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Mar. Drugs, Volume 22, Issue 9 (September 2024) – 28 articles

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35 pages, 1776 KiB  
Review
Marine Microorganism Molecules as Potential Anti-Inflammatory Therapeutics
by Malia Lasalo, Thierry Jauffrais, Philippe Georgel and Mariko Matsui
Mar. Drugs 2024, 22(9), 405; https://doi.org/10.3390/md22090405 (registering DOI) - 3 Sep 2024
Abstract
The marine environment represents a formidable source of biodiversity, is still largely unexplored, and has high pharmacological potential. Indeed, several bioactive marine natural products (MNPs), including immunomodulators, have been identified in the past decades. Here, we review how this reservoir of bioactive molecules [...] Read more.
The marine environment represents a formidable source of biodiversity, is still largely unexplored, and has high pharmacological potential. Indeed, several bioactive marine natural products (MNPs), including immunomodulators, have been identified in the past decades. Here, we review how this reservoir of bioactive molecules could be mobilized to develop novel anti-inflammatory compounds specially produced by or derived from marine microorganisms. After a detailed description of the MNPs exerting immunomodulatory potential and their biological target, we will briefly discuss the challenges associated with discovering anti-inflammatory compounds from marine microorganisms. Full article
(This article belongs to the Special Issue Pharmacological Potential of Marine Natural Products)
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16 pages, 3145 KiB  
Article
Light Spectra, a Promising Tool to Modulate Ulva lacinulata Productivity and Composition
by Helena M. Amaro, Fernando Pagels, Rosa Melo, Antoine Fort, Ronan Sulpice, Graciliana Lopes, Isabel Costa and Isabel Sousa-Pinto
Mar. Drugs 2024, 22(9), 404; https://doi.org/10.3390/md22090404 (registering DOI) - 3 Sep 2024
Abstract
Light quality is a key factor affecting algal growth and biomass composition, particularly pigments such as carotenoids, known for their antioxidant properties. Light-emitting diodes (LEDs) are becoming a cost-effective solution for indoor seaweed production when compared to fluorescent bulbs, allowing full control of [...] Read more.
Light quality is a key factor affecting algal growth and biomass composition, particularly pigments such as carotenoids, known for their antioxidant properties. Light-emitting diodes (LEDs) are becoming a cost-effective solution for indoor seaweed production when compared to fluorescent bulbs, allowing full control of the light spectra. However, knowledge of its effects on Ulva biomass production is still scarce. In this study, we investigated the effects of LEDs on the phenotype of an Ulva lacinulata strain, collected on the Northern Portuguese coast. Effects of white (W), green (G), red (R), and blue (B) LEDs were evaluated for growth (fresh weight and area), photosynthetic activity, sporulation, and content of pigments and antioxidant compounds. The results showed that there were no significant differences in terms of fresh weight accumulation and reduced sporulation among the tested LEDs, while W light induced the highest expansion rate. Under G, U. lacinulata attained a quicker photoacclimation, and the highest content of pigments and total antioxidant activity; but with R and W, antioxidant compounds against the specific radicals O2•− and NO were produced in a higher content when compared to other LEDs. Altogether, this study demonstrated that it is possible to modulate the bioactive properties of U. lacinulata by using W, R, and G light, opening the path to the production of biomass tailored for specific nutraceutical applications. Full article
(This article belongs to the Special Issue Biotechnology of Algae)
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11 pages, 2819 KiB  
Article
New Sesquiterpenoids from the Mangrove-Derived Fungus Talaromyces sp. as Modulators of Nuclear Receptors
by Tanwei Gu, Jian Cai, Danni Xie, Jianglian She, Yonghong Liu, Xuefeng Zhou and Lan Tang
Mar. Drugs 2024, 22(9), 403; https://doi.org/10.3390/md22090403 (registering DOI) - 3 Sep 2024
Viewed by 109
Abstract
Four new sesquiterpenoids, talaroterpenes A–D (14), were isolated from the mangrove-derived fungus Talaromyces sp. SCSIO 41412. The structures of compounds 14 were elucidated through comprehensive NMR and MS spectroscopic analyses. The absolute configurations of 14 [...] Read more.
Four new sesquiterpenoids, talaroterpenes A–D (14), were isolated from the mangrove-derived fungus Talaromyces sp. SCSIO 41412. The structures of compounds 14 were elucidated through comprehensive NMR and MS spectroscopic analyses. The absolute configurations of 14 were assigned based on single-crystal X-ray diffraction and calculated electronic circular dichroism analysis. Talaroterpenes A–D (14) were evaluated with their regulatory activities on nuclear receptors in HepG2 cells. Under the concentrations of 200 μM, 1, 3 and 4 exhibited varying degrees of activation on ABCA1 and PPARα, while 4 showed the strongest activities. Furthermore, 4 induced significant alterations in the expression of downstream target genes CLOCK and BMAL1 of RORα, and the in silico molecular docking analysis supported the direct binding interactions of 4 with RORα protein. This study revealed that talaroterpene D (4) was a new potential non-toxic modulator of nuclear receptors. Full article
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48 pages, 5981 KiB  
Review
An Overview of Secondary Metabolites from Soft Corals of the Genus Capnella over the Five Decades: Chemical Structures, Pharmacological Activities, NMR Data, and Chemical Synthesis
by Can-Qi Liu, Qi-Bin Yang, Ling Zhang and Lin-Fu Liang
Mar. Drugs 2024, 22(9), 402; https://doi.org/10.3390/md22090402 - 2 Sep 2024
Viewed by 219
Abstract
There has been no specific review on the secondary metabolites from soft corals of the genus Capnella till now. In this work, all secondary metabolites from different species of the title genus were described. It covered the first work from 1974 to May [...] Read more.
There has been no specific review on the secondary metabolites from soft corals of the genus Capnella till now. In this work, all secondary metabolites from different species of the title genus were described. It covered the first work from 1974 to May 2024, spanning five decades. In the viewpoint of the general structural features, these chemical constituents were classified into four groups: sesquiterpenes, diterpenes, steroids, and lipids. Additionally, the 1H and 13C NMR data of these metabolites were provided when available in the literature. Among them, sesquiterpenes were the most abundant chemical compositions from soft corals of the genus Capnella. A variety of pharmacological activities of these compounds were evaluated, such as cytotoxic, antibacterial, antifungal, and anti-inflammatory activities. In addition, the chemical synthesis works of several representative sesquiterpenes were provided. This review aims to provide an up-to-date knowledge of the chemical structures, pharmacological activities, and chemical synthesis of the chemical constituents from soft corals of the genus Capnella. Full article
(This article belongs to the Special Issue Bioactive Compounds from Soft Corals and Their Derived Microorganisms)
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13 pages, 3073 KiB  
Article
Anti-Inflammatory Effect of Fucoidan from Costaria costata Inhibited Lipopolysaccharide-Induced Inflammation in Mice
by Wei Zhang, Peter C. W. Lee and Jun-O Jin
Mar. Drugs 2024, 22(9), 401; https://doi.org/10.3390/md22090401 - 2 Sep 2024
Viewed by 208
Abstract
Seaweed extracts, especially fucoidan, are well known for their immune-modulating abilities. In this current study, we extracted fucoidan from Costaria costata, a seaweed commonly found in coastal Asia, and examined its anti-inflammatory effect. Fucoidan was extracted from dried C. costata (FCC) using [...] Read more.
Seaweed extracts, especially fucoidan, are well known for their immune-modulating abilities. In this current study, we extracted fucoidan from Costaria costata, a seaweed commonly found in coastal Asia, and examined its anti-inflammatory effect. Fucoidan was extracted from dried C. costata (FCC) using an alcohol extraction method at an extraction rate of 4.5 ± 0.21%. The extracted FCC comprised the highest proportion of carbohydrates, along with sulfate and uronic acid. The immune regulatory effect of FCC was examined using bone marrow-derived dendritic cells (BMDCs). Pretreatment with FCC dose-dependently decreased the lipopolysaccharide (LPS)-induced upregulation of co-stimulatory molecules and major histocompatibility complex. In addition, FCC prevented morphological changes in LPS-induced BMDCs. Moreover, treatment of LPS-induced BMDCs with FCC suppressed the secretion of pro-inflammatory cytokines. In C57BL/6 mice, oral administration of FCC suppressed LPS-induced lung inflammation, reducing the secretion of pro-inflammatory cytokines in the bronchoalveolar lavage fluid. Finally, the administration of FCC suppressed LPS-induced sepsis. Therefore, FCC could be developed as a health supplement based on the observed anti-inflammatory effects. Full article
(This article belongs to the Special Issue Polysaccharides from Marine Environment)
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16 pages, 3122 KiB  
Article
Novel Galectins Purified from the Sponge Chondrilla australiensis: Unique Structural Features and Cytotoxic Effects on Colorectal Cancer Cells Mediated by TF-Antigen Binding
by Ryuhei Hayashi, Kenichi Kamata, Marco Gerdol, Yuki Fujii, Takashi Hayashi, Yuto Onoda, Nanae Kobayashi, Satoshi Furushima, Ryuya Ishiwata, Mayuka Ohkawa, Naoko Masuda, Yuka Niimi, Masao Yamada, Daisuke Adachi, Sarkar M. A. Kawsar, Sultana Rajia, Imtiaj Hasan, Somrita Padma, Bishnu Pada Chatterjee, Yuji Ise, Riku Chida, Kayo Hasehira, Nobumitsu Miyanishi, Tatsuya Kawasaki, Yukiko Ogawa, Hideaki Fujita, Alberto Pallavicini and Yasuhiro Ozekiadd Show full author list remove Hide full author list
Mar. Drugs 2024, 22(9), 400; https://doi.org/10.3390/md22090400 (registering DOI) - 31 Aug 2024
Viewed by 353
Abstract
We here report the purification of a novel member of the galectin family, the β-galactoside-binding lectin hRTL, from the marine sponge Chondrilla australiensis. The hRTL lectin is a tetrameric proto-type galectin with a subunit molecular weight of 15.5 kDa, consisting of 141 [...] Read more.
We here report the purification of a novel member of the galectin family, the β-galactoside-binding lectin hRTL, from the marine sponge Chondrilla australiensis. The hRTL lectin is a tetrameric proto-type galectin with a subunit molecular weight of 15.5 kDa, consisting of 141 amino acids and sharing 92% primary sequence identity with the galectin CCL from the congeneric species C. caribensis. Transcriptome analysis allowed for the identification of additional sequences belonging to the same family, bringing the total number of hRTLs to six. Unlike most other galectins, hRTLs display a 23 amino acid-long signal peptide that, according to Erdman degradation, is post-translationally cleaved, leaving an N-terminal end devoid of acetylated modifications, unlike most other galectins. Moreover, two hRTLs display an internal insertion, which determines the presence of an unusual loop region that may have important functional implications. The characterization of the glycan-binding properties of hRTL revealed that it had high affinity towards TF-antigen, sialyl TF, and type-1 N-acetyl lactosamine with a Galβ1-3 structure. When administered to DLD-1 cells, a colorectal carcinoma cell line expressing mucin-associated TF-antigen, hRTL could induce glycan-dependent cytotoxicity. Full article
(This article belongs to the Section Marine Pharmacology)
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17 pages, 6491 KiB  
Article
Identification and Characterization of a Highly Active Hyaluronan Lyase from Enterobacter asburiae
by Linjing Zhang, Jiayu Jiang, Wei Liu, Lianlong Wang, Zhiyuan Yao, Heng Li, Jinsong Gong, Chuanli Kang, Lei Liu, Zhenghong Xu and Jinsong Shi
Mar. Drugs 2024, 22(9), 399; https://doi.org/10.3390/md22090399 - 31 Aug 2024
Viewed by 351
Abstract
Hyaluronic acid (HA) is a well-known functional marine polysaccharide. The utilization and derivative development of HA are of great interest. Hyaluronan lyase has wide application prospects in the production of HA oligosaccharides and lower molecular weight HA. In this study, a strain of [...] Read more.
Hyaluronic acid (HA) is a well-known functional marine polysaccharide. The utilization and derivative development of HA are of great interest. Hyaluronan lyase has wide application prospects in the production of HA oligosaccharides and lower molecular weight HA. In this study, a strain of Enterobacter asburiae CGJ001 with high hyaluronan lyase activity was screened from industrial wastewater. This strain exhibited an impressive enzyme activity of 40,576 U/mL after being incubated for 14 h. Whole genome sequencing analysis revealed that E. asburiae CGJ001 contained a cluster of genes involved in HA degradation, transport, and metabolism. A newly identified enzyme responsible for glycosaminoglycan degradation was designated as HylEP0006. A strain of E. coli BL21(DE3)/pET-22b(+)-hylEP0006 was successfully constructed. HylEP0006 exhibited optimal degradation at 40 °C and pH 7.0, showing a high activity of 950,168.3 U/mg. HylEP0006 showed specific activity against HA. The minimum degradation fragment of HylEP0006 was hyaluronan tetrasaccharides, and HylEP0006 could efficiently degrade HA into unsaturated disaccharides (HA2), with HA2 as the final product. These characteristics indicate that HylEP0006 has a potential application prospect for the extraction and utilization of hyaluronic acid. Full article
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13 pages, 2732 KiB  
Article
Preparation and Vasodilation Mechanism of Angiotensin-I-Converting Enzyme Inhibitory Peptide from Ulva prolifera Protein
by Zhiyong Li, Hongyan He, Jiasi Liu, Huiyue Gu, Caiwei Fu, Aurang Zeb, Tuanjie Che and Songdong Shen
Mar. Drugs 2024, 22(9), 398; https://doi.org/10.3390/md22090398 - 31 Aug 2024
Viewed by 257
Abstract
Ulva prolifera, a type of green algae that can be consumed, was utilized in the production of an angiotensin-I converting enzyme (ACE) inhibitory peptide. The protein from the algae was isolated and subsequently hydrolyzed using a neutral protease. The resulting hydrolysate underwent [...] Read more.
Ulva prolifera, a type of green algae that can be consumed, was utilized in the production of an angiotensin-I converting enzyme (ACE) inhibitory peptide. The protein from the algae was isolated and subsequently hydrolyzed using a neutral protease. The resulting hydrolysate underwent several processes including Sephadex-G100 filtration chromatography, ultrafiltration, HPLC-Q-TOF-MS analysis, ADMET screening, UV spectrum detection test, molecular docking, and molecular dynamic simulation. Then, the ACE inhibitory peptide named KAF (IC50, 0.63 ± 0.26 µM) was identified. The effectiveness of this peptide in inhibiting ACE can be primarily attributed to two conventional hydrogen bonds. Additionally, it could activate endothelial nitric oxide synthase (eNOS) activity to promote the generation of nitric oxide (NO). Additionally, KAF primarily increased the intracellular calcium (Ca2+) level by acting on L-type Ca2+ channel (LTCC) and the ryanodine receptor (RyR) in the endoplasmic reticulum, and completed the activation of eNOS under the mediation of protein kinase B (Akt) signaling pathway. Our study has confirmed that KAF has the potential to be processed into pharmaceutical candidate functions on vasoconstriction. Full article
(This article belongs to the Special Issue Marine Bioactive Peptides—Structure, Function, and Application 2.0)
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15 pages, 4297 KiB  
Article
Antiviral Activity of Chlorophyll Extracts from Tetraselmis sp., a Marine Microalga, Against Zika Virus Infection
by Nalae Kang, Eun-A Kim, Areumi Park, Seong-Yeong Heo, Jun-Ho Heo, Won-Kyu Lee, Yong-Kyun Ryu and Soo-Jin Heo
Mar. Drugs 2024, 22(9), 397; https://doi.org/10.3390/md22090397 - 31 Aug 2024
Viewed by 279
Abstract
Recent advancements in the large-scale cultivation of Tetraselmis sp. in Korea have enabled year-round production of this marine microalgae. This study explores the potential industrial applications of Tetraselmis sp. biomass by investigating the antiviral properties of its extracts and primary components. The antiviral [...] Read more.
Recent advancements in the large-scale cultivation of Tetraselmis sp. in Korea have enabled year-round production of this marine microalgae. This study explores the potential industrial applications of Tetraselmis sp. biomass by investigating the antiviral properties of its extracts and primary components. The antiviral effects of Tetraselmis sp. extracts were evaluated in Zika virus (ZIKV)-infected cells. Following extensive isolation and purification, the main compounds were characterized using liquid chromatography–mass spectrometry (LC-MS) and nuclear magnetic resonance (NMR) analyses. Their antiviral activities were confirmed using in vitro and in silico tests. Tetraselmis sp. extracts reduced infectious viral particles and non-structural protein 1 messenger RNA levels in ZIKV-infected cells without inducing cytotoxicity. Additionally, they modulated the interferon-mediated immune system responses. Tetraselmis sp. extracts are composed of four main chlorophylls: chlorophyll a, chlorin e6-131-152-dimethyl-173-phytyl ester, hydroxychlorophyll a, and hydroxypheophytin a. Among them, chlorophyll a, chlorin e6-131-152-dimethyl-173-phytyl ester, and hydroxypheophytin showed the antiviral activities in ZIKV-infected cells and molecular docking simulations predicted interactions between these chlorophylls and ZIKV. Our findings suggest that Tetraselmis sp. chlorophyll extracts exert antiviral effects against ZIKV and could serve as potential therapeutic candidates against ZIKV infection. Full article
(This article belongs to the Special Issue Biotechnological Applications of Marine Microalgae)
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17 pages, 2939 KiB  
Article
Stonikacidin A, an Antimicrobial 4-Bromopyrrole Alkaloid Containing L-Idonic Acid Core from the Northwestern Pacific Marine Sponge Lissodendoryx papillosa
by Kseniya M. Tabakmakher, Tatyana N. Makarieva, Yuri E. Sabutski, Maxim S. Kokoulin, Alexander S. Menshov, Roman S. Popov, Alla G. Guzii, Larisa K. Shubina, Ekaterina A. Chingizova, Artur R. Chingizov, Ekaterina A. Yurchenko, Sergey N. Fedorov, Boris B. Grebnev, Gunhild von Amsberg, Sergey A. Dyshlovoy, Natalia V. Ivanchina and Pavel S. Dmitrenok
Mar. Drugs 2024, 22(9), 396; https://doi.org/10.3390/md22090396 - 30 Aug 2024
Viewed by 400
Abstract
Stonikacidin A (1), the first representative of a new class of 4-bromopyrrole alkaloids containing an aldonic acid core, was isolated from the marine sponge Lissodendoryx papillosa. The compound is named in honor of Prof. Valentin A. Stonik, who is one [...] Read more.
Stonikacidin A (1), the first representative of a new class of 4-bromopyrrole alkaloids containing an aldonic acid core, was isolated from the marine sponge Lissodendoryx papillosa. The compound is named in honor of Prof. Valentin A. Stonik, who is one of the outstanding investigators in the field of marine natural chemistry. The structure of 1 was determined using NMR, MS analysis, and chemical correlations. The L-idonic acid core was established by the comparison of GC, NMR, MS, and optical rotation data of methyl-pentaacetyl-aldonates obtained from the hydrolysis products of 1 and standard hexoses. The L-form of the idonic acid residue in 1 was confirmed by GC analysis of pentaacetate of (S)-2-butyl ester of the hydrolysis product from 1 and compared with corresponding derivatives of L- and D-idonic acids. The biosynthetic pathway for stonikacidin A (1) was proposed. The alkaloid 1 inhibited the growth of Staphylococcus aureus and Escherichia coli test strains, as well as affected the formation of S. aureus and E. coli biofilms. Compound 1 inhibited the activity of sortase A. Molecular docking data showed that stonikacidin A (1) can bind with sortase A due to the interactions between its bromine atoms and some amino acid residues of the enzyme. Full article
(This article belongs to the Special Issue Bio-Active Components from Marine Sponges)
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27 pages, 8736 KiB  
Article
Ameliorative Effect of Chitosan/Spirulina platensis Ethanolic Extract Nanoformulation against Cyclophosphamide-Induced Ovarian Toxicity: Role of PPAR-γ/Nrf-2/HO-1 and NF-kB/TNF-α Signaling Pathways
by May Almukainzi, Thanaa A. El-Masry, Hanaa A. Ibrahim, Hebatallah M. Saad, Enas I. El Zahaby, Asmaa Saleh and Maysa M. F. El-Nagar
Mar. Drugs 2024, 22(9), 395; https://doi.org/10.3390/md22090395 - 30 Aug 2024
Viewed by 456
Abstract
Cyclophosphamide (CP) is an anticancer drug that causes infertility disorders. This study was designed to evaluate a nanoformulation of chitosan with an ethanolic extract from Spirulina platensis in terms of its protection against cyclophosphamide-induced ovarian toxicity. Nine groups of female Wistar rats were [...] Read more.
Cyclophosphamide (CP) is an anticancer drug that causes infertility disorders. This study was designed to evaluate a nanoformulation of chitosan with an ethanolic extract from Spirulina platensis in terms of its protection against cyclophosphamide-induced ovarian toxicity. Nine groups of female Wistar rats were randomly assigned as follows: 1: control vehicle, 2: chitosan polymer, 3: telmisartan, 4: Spirulina platensis extract, 5: nanoformulation of the Spirulina platensis, and 6: single injection of CP; groups 7, 8, and 9 received the same treatments as those used in groups 3, 4, and 5, respectively, with a single dose of CP (200 mg/kg, I.P). The results displayed that the CP treatment decreased estradiol, progesterone, anti-mullerian hormone, and GSH content, and it downregulated PPAR-γ, Nrf-2, and HO-1 gene expression. In addition, the CP treatment caused an increase in the FSH, LH, and MDA levels. In the same manner, the protein expression of caspase-3, NF-kB, and TNF-α was upregulated in response to the CP treatment, while PPAR-γ was downregulated in comparison with the control. The rats treated with SPNPs exhibited a substantial reduction in the detrimental effects of oxidative stress and inflammation of the ovarian tissue. This study’s conclusions showed that SPNPs counteracted the effects of CP, preventing the death of ovarian follicles and restoring the gonadotropin hormone balance and normal ovarian histological appearance. Full article
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28 pages, 5832 KiB  
Article
Bioactive Glial-Derived Neurotrophic Factor from a Safe Injectable Collagen–Alginate Composite Gel Rescues Retinal Photoreceptors from Retinal Degeneration in Rabbits
by Tingyu Hu, Ting Zhou, Rajesh Kumar Goit, Ka Cheung Tam, Yau Kei Chan, Wai-Ching Lam and Amy Cheuk Yin Lo
Mar. Drugs 2024, 22(9), 394; https://doi.org/10.3390/md22090394 - 30 Aug 2024
Viewed by 392
Abstract
The management of vision-threatening retinal diseases remains challenging due to the lack of an effective drug delivery system. Encapsulated cell therapy (ECT) offers a promising approach for the continuous delivery of therapeutic agents without the need for immunosuppressants. In this context, an injectable [...] Read more.
The management of vision-threatening retinal diseases remains challenging due to the lack of an effective drug delivery system. Encapsulated cell therapy (ECT) offers a promising approach for the continuous delivery of therapeutic agents without the need for immunosuppressants. In this context, an injectable and terminable collagen–alginate composite (CAC) ECT gel, designed with a Tet-on pro-caspase-8 system, was developed as a safe intraocular drug delivery platform for the sustained release of glial-cell-line-derived neurotrophic factor (GDNF) to treat retinal degenerative diseases. This study examined the potential clinical application of the CAC ECT gel, focusing on its safety, performance, and termination through doxycycline (Dox) administration in the eyes of healthy New Zealand White rabbits, as well as its therapeutic efficacy in rabbits with sodium-iodate (SI)-induced retinal degeneration. The findings indicated that the CAC ECT gel can be safely implanted without harming the retina or lens, displaying resistance to degradation, facilitating cell attachment, and secreting bioactive GDNF. Furthermore, the GDNF levels could be modulated by the number of implants. Moreover, Dox administration was effective in terminating gel function without causing retinal damage. Notably, rabbits with retinal degeneration treated with the gels exhibited significant functional recovery in both a-wave and b-wave amplitudes and showed remarkable efficacy in reducing photoreceptor apoptosis. Given its biocompatibility, mechanical stability, controlled drug release, terminability, and therapeutic effectiveness, our CAC ECT gel presents a promising therapeutic strategy for various retinal diseases in a clinical setting, eliminating the need for immunosuppressants. Full article
(This article belongs to the Special Issue Marine-Derived Biomaterials for Tissue Regeneration)
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12 pages, 2493 KiB  
Article
Two C23-Steroids and a New Isocoumarin Metabolite from Mangrove Sediment-Derived Fungus Penicillium sp. SCSIO 41429
by Lishan Huang, Chunmei Chen, Jian Cai, Yixin Chen, Yongyan Zhu, Bin Yang, Xuefeng Zhou, Yonghong Liu and Huaming Tao
Mar. Drugs 2024, 22(9), 393; https://doi.org/10.3390/md22090393 - 30 Aug 2024
Viewed by 284
Abstract
Two new C23-steroids derivatives, cyclocitrinoic acid A (1) and cyclocitrinoic acid B (2), and a new isocoumarin metabolite, (3R,4S)-6,8-dihydroxy-3,4,5-trimethyl-7-carboxamidelisocoumarin (10), together with 12 known compounds (39, 11 [...] Read more.
Two new C23-steroids derivatives, cyclocitrinoic acid A (1) and cyclocitrinoic acid B (2), and a new isocoumarin metabolite, (3R,4S)-6,8-dihydroxy-3,4,5-trimethyl-7-carboxamidelisocoumarin (10), together with 12 known compounds (39, 1115) were isolated from the mangrove-sediment fungus Penicillium sp. SCSIO 41429. The structures of the new compounds were comprehensively characterized by 1D and 2D NMR, HRESIMS and ECD calculation. All isolates were evaluated for pancreatic lipase (PL) inhibitory and antioxidant activities. The biological evaluation results revealed that compounds 2, 14 and 15 displayed weak or moderate inhibition against PL, with IC50 values of 32.77, 5.15 and 2.42 µM, respectively. In addition, compounds 7, 12 and 13 showed radical scavenging activities against DPPH, with IC50 values of 64.70, 48.13, and 75.54 µM, respectively. In addition, molecular docking results indicated that these compounds had potential for PL inhibitory and antioxidant activities, which provided screening candidates for antioxidants and a reduction in obesity. Full article
(This article belongs to the Section Marine Pharmacology)
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8 pages, 761 KiB  
Communication
New Meroterpenes from South China Sea Soft Coral Litophyton brassicum
by Xiaoyi Chen, Jiahui Zhang, Jiayu Yang, Bing Li, Te Li, Han Ouyang, Wenhan Lin, Hongyu Hu, Xia Yan and Shan He
Mar. Drugs 2024, 22(9), 392; https://doi.org/10.3390/md22090392 - 30 Aug 2024
Viewed by 398
Abstract
A chemical investigation of the extracts from the soft coral Litophyton brassicum led to the isolation and identification of four new meroterpenes, brassihydroxybenzoquinone A and B (1 and 2) and brassinaphthoquinone A and B (3 and 4), along with [...] Read more.
A chemical investigation of the extracts from the soft coral Litophyton brassicum led to the isolation and identification of four new meroterpenes, brassihydroxybenzoquinone A and B (1 and 2) and brassinaphthoquinone A and B (3 and 4), along with two known related meroterpenes (5 and 6). Their structures were elucidated using high-resolution electrospray ionization mass spectrometry (HRESIMS), nuclear magnetic resonance (NMR) spectroscopy, and a comparison with the literature data. All compounds were evaluated for antibacterial activity against six pathogenic bacterial strains and for cytotoxic activity against three cancer cell lines. In the cytotoxic assay, all compounds were inactive at 10 μM against the A549, HeLa, and MDA-MB-231 cell lines. In the antibacterial assay, compounds 1 and 2 exhibited moderate inhibitory activity with minimum inhibitory concentrations (MIC) ranging from 8 to 64 μg/mL. Full article
(This article belongs to the Special Issue Bioactive Compounds from Soft Corals and Their Derived Microorganisms)
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20 pages, 5769 KiB  
Article
Chrysomycin A Reshapes Metabolism and Increases Oxidative Stress to Hinder Glioblastoma Progression
by Dong-Ni Liu, Wen-Fang Zhang, Wan-Di Feng, Shuang Xu, Dan-Hong Feng, Fu-Hang Song, Hua-Wei Zhang, Lian-Hua Fang, Guan-Hua Du and Yue-Hua Wang
Mar. Drugs 2024, 22(9), 391; https://doi.org/10.3390/md22090391 (registering DOI) - 29 Aug 2024
Viewed by 274
Abstract
Glioblastoma represents the predominant and a highly aggressive primary neoplasm of the central nervous system that has an abnormal metabolism. Our previous study showed that chrysomycin A (Chr-A) curbed glioblastoma progression in vitro and in vivo. However, whether Chr-A could inhibit orthotopic glioblastoma [...] Read more.
Glioblastoma represents the predominant and a highly aggressive primary neoplasm of the central nervous system that has an abnormal metabolism. Our previous study showed that chrysomycin A (Chr-A) curbed glioblastoma progression in vitro and in vivo. However, whether Chr-A could inhibit orthotopic glioblastoma and how it reshapes metabolism are still unclear. In this study, Chr-A markedly suppressed the development of intracranial U87 gliomas. The results from airflow-assisted desorption electrospray ionization mass spectrometry imaging (AFADESI-MSI) indicated that Chr-A improved the abnormal metabolism of mice with glioblastoma. Key enzymes including glutaminase (GLS), glutamate dehydrogenases 1 (GDH1), hexokinase 2 (HK2) and glucose-6-phosphate dehydrogenase (G6PD) were regulated by Chr-A. Chr-A further altered the level of nicotinamide adenine dinucleotide phosphate (NADPH), thus causing oxidative stress with the downregulation of Nrf-2 to inhibit glioblastoma. Our study offers a novel perspective for comprehending the anti-glioma mechanism of Chr-A, highlighting its potential as a promising chemotherapeutic agent for glioblastoma. Full article
(This article belongs to the Collection Marine Compounds and Cancer)
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16 pages, 5332 KiB  
Article
Single Amino Acid Substitution in Loop1 Switches the Selectivity of α-Conotoxin RegIIA towards the α7 Nicotinic Acetylcholine Receptor
by Jinpeng Yu, Junjie Xie, Yuting Ma, Pengcheng Wei, Panpan Zhang, Zepei Tang, Xiaopeng Zhu, Dongting Zhangsun and Sulan Luo
Mar. Drugs 2024, 22(9), 390; https://doi.org/10.3390/md22090390 - 29 Aug 2024
Viewed by 362
Abstract
α-Conotoxins are disulfide-rich peptides obtained from the venom of cone snails, which are considered potential molecular probes and drug leads for nAChR-related disorders. However, low specificity towards different nAChR subtypes restricts the further application of many α-conotoxins. In this work, a series of [...] Read more.
α-Conotoxins are disulfide-rich peptides obtained from the venom of cone snails, which are considered potential molecular probes and drug leads for nAChR-related disorders. However, low specificity towards different nAChR subtypes restricts the further application of many α-conotoxins. In this work, a series of loop1 amino acid-substituted mutants of α-conotoxin RegIIA were synthesized, whose potency and selectivity were evaluated by an electrophysiological approach. The results showed that loop1 alanine scanning mutants [H5A]RegIIA and [P6A]RegIIA blocked rα7 nAChR with IC50s of 446 nM and 459 nM, respectively, while their inhibition against rα3β2 and rα3β4 subtypes was negligible, indicating the importance of the fifth and sixth amino acid residues for RegIIA’s potency and selectivity. Then, second-generation mutants were designed and synthesized, among which the analogues [H5V]RegIIA and [H5S]RegIIA showed significantly improved selectivity and comparable potency towards rα7 nAChR compared with the native RegIIA. Overall, these findings provide deep insights into the structure–activity relationship of RegIIA, as well as revealing a unique perspective for the further modification and optimization of α-conotoxins and other active peptides. Full article
(This article belongs to the Special Issue Toxins as Marine-Based Drug Discovery, 2nd Edition)
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11 pages, 723 KiB  
Article
Sulfated Aeruginosins from Lake Kinneret: Microcystis Bloom, Isolation, Structure Elucidation, and Biological Activity
by Shira Weisthal Algor, Assaf Sukenik and Shmuel Carmeli
Mar. Drugs 2024, 22(9), 389; https://doi.org/10.3390/md22090389 - 28 Aug 2024
Viewed by 339
Abstract
Aeruginosins are common metabolites of cyanobacteria. In the course of re-isolation of the known aeruginosins KT608A and KT608B for bioassay studies, we isolated three new sulfated aeruginosins, named aeruginosins KT688 (1), KT718 (2), and KT575 (3), from [...] Read more.
Aeruginosins are common metabolites of cyanobacteria. In the course of re-isolation of the known aeruginosins KT608A and KT608B for bioassay studies, we isolated three new sulfated aeruginosins, named aeruginosins KT688 (1), KT718 (2), and KT575 (3), from the extract of a Microcystis cell mass collected during the 2016 spring bloom event in Lake Kinneret, Israel. The structures of the new compounds were established on the basis of analyses of the 1D and 2D NMR, as well as HRESIMS data. Marfey’s method, coupled with HR ESI LCMS and chiral HPLC, was used to establish the absolute configuration of the amino acid and hydroxyphenyl lactic acid residues, respectively. Compounds 13 were tested for inhibition of the serine protease trypsin, and compounds 1 and 2 were found to exhibit IC50 values of 2.38 and 1.43 µM, respectively. Full article
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15 pages, 2075 KiB  
Review
Marine Bacteriocins: An Evolutionary Gold Mine to Payoff Antibiotic Resistance
by Piyush Baindara, Roy Dinata and Santi M. Mandal
Mar. Drugs 2024, 22(9), 388; https://doi.org/10.3390/md22090388 - 28 Aug 2024
Viewed by 335
Abstract
The rapid evolution of drug resistance is one of the greatest health issues of the 21st century. There is an alarming situation to find new therapeutic strategies or candidate drugs to tackle ongoing multi-drug resistance development. The marine environment is one of the [...] Read more.
The rapid evolution of drug resistance is one of the greatest health issues of the 21st century. There is an alarming situation to find new therapeutic strategies or candidate drugs to tackle ongoing multi-drug resistance development. The marine environment is one of the prime natural ecosystems on Earth, the majority of which is still unexplored, especially when it comes to the microbes. A wide variety of bioactive compounds have been obtained from a varied range of marine organisms; however, marine bacteria-produced bacteriocins are still undermined. Owing to the distinct environmental stresses that marine bacterial communities encounter, their bioactive compounds frequently undergo distinct adaptations that confer on them a variety of shapes and functions, setting them apart from their terrestrial counterparts. Bacterially produced ribosomally synthesized and posttranslationally modified peptides (RiPPs), known as bacteriocins, are one of the special interests to be considered as an alternative to conventional antibiotics because of their variety in structure and diverse potential biological activities. Additionally, the gut microbiome of marine creatures are a largely unexplored source of new bacteriocins with promising activities. There is a huge possibility of novel bacteriocins from marine bacterial communities that might come out as efficient candidates to fight against antibiotic resistance, especially in light of the growing pressure from antibiotic-resistant diseases and industrial desire for innovative treatments. The present review summarizes known and fully characterized marine bacteriocins, their evolutionary aspects, challenges, and the huge possibilities of unexplored novel bacteriocins from marine bacterial communities present in diverse marine ecosystems. Full article
(This article belongs to the Special Issue Bioactive Natural Products from the Deep-Sea-Sourced Microbes)
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18 pages, 8210 KiB  
Article
Comprehensive Assessment of Herbicide Toxicity on Navicula sp. Algae: Effects on Growth, Chlorophyll Content, Antioxidant System, and Lipid Metabolism
by Chunyan Zheng, Jie Yang, Yunting Wang, Waqas Ahmed, Amir Khan, Jiannan Li, Jiechang Weng, Sajid Mehmood and Weidong Li
Mar. Drugs 2024, 22(9), 387; https://doi.org/10.3390/md22090387 - 28 Aug 2024
Viewed by 321
Abstract
This study investigated the effects of herbicide exposure on Navicula sp. (MASCC-0035) algae, focusing on growth density, chlorophyll content, antioxidant system, and lipid metabolism. Navicula cultures were exposed to different concentrations of atrazine (ATZ), glyphosate (Gly), and acetochlor (ACT) for 96 h. Results [...] Read more.
This study investigated the effects of herbicide exposure on Navicula sp. (MASCC-0035) algae, focusing on growth density, chlorophyll content, antioxidant system, and lipid metabolism. Navicula cultures were exposed to different concentrations of atrazine (ATZ), glyphosate (Gly), and acetochlor (ACT) for 96 h. Results showed a significant decrease in cell numbers, with higher herbicide concentrations having the most noticeable impacts. For instance, Gly-G2 had reduced cell populations by 21.00% at 96 h. Chlorophyll content varied, with Gly having a greater impact on chlorophyll a compared to ATZ and ACT. Herbicide exposure also affected the antioxidant system, altering levels of soluble sugar, soluble protein, and reactive oxygen species (ROS). Higher herbicide rates increased soluble sugar content (e.g., ATZ, Gly, and ACT-G2 had increased by 14.03%, 19.88%, and 19.83%, respectively, at 72 h) but decreased soluble protein content, notably in Gly-G2 by 11.40%, indicating cellular stress. Lipid metabolism analysis revealed complex responses, with changes in free proline, fatty acids, and lipase content, each herbicide exerting distinct effects. These findings highlight the multifaceted impacts of herbicide exposure on Navicula algae, emphasizing the need for further research to understand ecological implications and develop mitigation strategies for aquatic ecosystems. Full article
(This article belongs to the Special Issue Marine Microalgal Biorefinery for Bioactive Compound Production 2024)
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13 pages, 1314 KiB  
Article
Nutritional Value and Productivity Potential of the Marine Microalgae Nitzschia laevis, Phaeodactylum tricornutum and Isochrysis galbana
by Xue Lu, Shufang Yang, Yongjin He, Weixuan Zhao, Man Nie and Han Sun
Mar. Drugs 2024, 22(9), 386; https://doi.org/10.3390/md22090386 - 27 Aug 2024
Viewed by 383
Abstract
Microalgae are considered promising sustainable feedstocks for the production of food, food additives, feeds, chemicals and various high-value products. Marine microalgae Phaeodactylum tricornutum, Isochrysis galbana and Nitzschia laevis are rich in fucoxanthin, which is effective for weight loss and metabolic diseases. The [...] Read more.
Microalgae are considered promising sustainable feedstocks for the production of food, food additives, feeds, chemicals and various high-value products. Marine microalgae Phaeodactylum tricornutum, Isochrysis galbana and Nitzschia laevis are rich in fucoxanthin, which is effective for weight loss and metabolic diseases. The selection of microalgae species with outstanding nutritional profiles is fundamental for novel foods development, and the nutritional value of P. tricornutum, I. galbana and N. laevis are not yet fully understood. Hence, this study investigates and analyzes the nutritional components of the microalgae by chromatography and mass spectrometry, to explore their nutritional and industrial application potential. The results indicate that the three microalgae possess high nutritional value. Among them, P. tricornutum shows significantly higher levels of proteins (43.29%) and amino acids, while I. galbana has the highest content of carbohydrates (25.40%) and lipids (10.95%). Notwithstanding that P. tricornutum and I. galbana have higher fucoxanthin contents, N. laevis achieves the highest fucoxanthin productivity (6.21 mg/L/day) and polyunsaturated fatty acids (PUFAs) productivity (26.13 mg/L/day) because of the competitive cell density (2.89 g/L) and the advantageous specific growth rate (0.42/day). Thus, compared with P. tricornutum and I. galbana, N. laevis is a more promising candidate for co-production of fucoxanthin and PUFAs. Full article
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14 pages, 11931 KiB  
Article
Machine Learning-Driven Discovery and Evaluation of Antimicrobial Peptides from Crassostrea gigas Mucus Proteome
by Jingchen Song, Kelin Liu, Xiaoyang Jin, Ke Huang, Shiwei Fu, Wenjie Yi, Yijie Cai, Ziniu Yu, Fan Mao and Yang Zhang
Mar. Drugs 2024, 22(9), 385; https://doi.org/10.3390/md22090385 - 26 Aug 2024
Viewed by 573
Abstract
Marine antimicrobial peptides (AMPs) represent a promising source for combating infections, especially against antibiotic-resistant pathogens and traditionally challenging infections. However, traditional drug discovery methods face challenges such as time-consuming processes and high costs. Therefore, leveraging machine learning techniques to expedite the discovery of [...] Read more.
Marine antimicrobial peptides (AMPs) represent a promising source for combating infections, especially against antibiotic-resistant pathogens and traditionally challenging infections. However, traditional drug discovery methods face challenges such as time-consuming processes and high costs. Therefore, leveraging machine learning techniques to expedite the discovery of marine AMPs holds significant promise. Our study applies machine learning to develop marine AMPs, focusing on Crassostrea gigas mucus rich in antimicrobial components. We conducted proteome sequencing of C. gigas mucous proteins, used the iAMPCN model for peptide activity prediction, and evaluated the antimicrobial, hemolytic, and cytotoxic capabilities of six peptides. Proteomic analysis identified 4490 proteins, yielding about 43,000 peptides (8–50 amino acids). Peptide ranking based on length, hydrophobicity, and charge assessed antimicrobial potential, predicting 23 biological activities. Six peptides, distinguished by their high relative scores and promising biological activities, were chosen for bactericidal assay. Peptides P1 to P4 showed antimicrobial activity against E. coli, with P2 and P4 being particularly effective. All peptides inhibited S. aureus growth. P2 and P4 also exhibited significant anti-V. parahaemolyticus effects, while P1 and P3 were non-cytotoxic to HEK293T cells at detectable concentrations. Minimal hemolytic activity was observed for all peptides even at high concentrations. This study highlights the potent antimicrobial properties of naturally occurring oyster mucus peptides, emphasizing their low cytotoxicity and lack of hemolytic effects. Machine learning accurately predicted biological activity, showcasing its potential in peptide drug discovery. Full article
(This article belongs to the Special Issue Bioactive Proteins and Peptides from Marine Mollusks)
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14 pages, 3593 KiB  
Article
New Bioactive Polyketides from the Mangrove-Derived Fungus Penicillium sp. SCSIO 41411
by Yi Chen, Jian Cai, Ziwei Xia, Chunmei Chen, Yonghong Liu, Lalith Jayasinghe, Xueni Wang and Xuefeng Zhou
Mar. Drugs 2024, 22(9), 384; https://doi.org/10.3390/md22090384 - 26 Aug 2024
Viewed by 444
Abstract
Three new polyketides, including three ester derivatives (1, 3, and 5) and a new natural product, which was a benzoquinone derivative, embelin A (4), together with nine known ones (2 and 613), were [...] Read more.
Three new polyketides, including three ester derivatives (1, 3, and 5) and a new natural product, which was a benzoquinone derivative, embelin A (4), together with nine known ones (2 and 613), were isolated from the mangrove-derived fungus Penicillium sp. SCSIO 41411. Their structures were determined by detailed NMR and MS spectroscopic analyses. The X-ray single-crystal diffraction analysis of 4 was described for the first time. Compound 9 displayed obvious inhibition against PDE4 with an inhibitory ratio of 40.78% at 10 μM. Compound 12 showed DPPH radical scavenging activity, with an EC50 of 16.21 µg/mL, compared to the positive control (ascorbic acid, EC50, 11.22 µg/mL). Furthermore, compound 4 exhibited cytotoxicity against PC-3 and LNCaP with IC50 values of 18.69 and 31.62 µM, respectively. Full article
(This article belongs to the Special Issue Bio-Active Products from Mangrove Ecosystems 2.0)
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15 pages, 3632 KiB  
Article
Glutamic-Alanine Rich Glycoprotein from Undaria pinnatifida: A Promising Natural Anti-Inflammatory Agent
by Md Saifur Rahman, Md Badrul Alam, Marufa Naznin, Mst Hur Madina and S. M. Rafiquzzaman
Mar. Drugs 2024, 22(9), 383; https://doi.org/10.3390/md22090383 - 26 Aug 2024
Viewed by 400
Abstract
This study aimed to assess the anti-inflammatory properties of a bioactive glutamic-alanine rich glycoprotein (GP) derived from Undaria pinnatifida on both LPS-stimulated RAW264.7 cells, peritoneal macrophages, and mouse models of carrageenan- and xylene-induced inflammation, investigating the underlying molecular mechanisms. In both in-vitro and [...] Read more.
This study aimed to assess the anti-inflammatory properties of a bioactive glutamic-alanine rich glycoprotein (GP) derived from Undaria pinnatifida on both LPS-stimulated RAW264.7 cells, peritoneal macrophages, and mouse models of carrageenan- and xylene-induced inflammation, investigating the underlying molecular mechanisms. In both in-vitro and in-vivo settings, GP was found to reduce the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) while also inhibiting the production of nitric oxide (NO) and prostaglandin E2 (PGE2) in response to lipopolysaccharide (LPS) stimulation. GP treatment significantly impeded the nuclear translocation of the nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway by blocking the phosphorylation of IKKα and IκBα, leading to a reduction in proinflammatory cytokines such as tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and interleukin-6 (IL-6). Additionally, GP effectively inhibited the activation of mitogen-activated protein kinases (MAPKs), with specific inhibitors of p38 and extra-cellular signal regulated kinase (ERK) enhancing GP’s anti-inflammatory efficacy. Notably, GP administration at 10 mg/kg/day (p.o.) markedly reduced carrageenan-induced paw inflammation and xylene-induced ear edema by preventing the infiltration of inflammatory cells into targeted tissues. GP treatment also downregulated key inflammatory markers, including iNOS, COX-2, IκBα, and NF-κB, by suppressing the phosphorylation of p38 and ERK, thereby improving the inflammatory index in both carrageenan- and xylene-induced mouse models. These findings suggest that marine resources, particularly seaweeds like U. pinnatifida, could serve as valuable sources of natural anti-inflammatory proteins for the effective treatment of inflammation and related conditions. Full article
(This article belongs to the Special Issue The Bioactive Potential of Marine-Derived Peptides and Proteins)
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17 pages, 4712 KiB  
Article
Mutagenesis of the Peptide Inhibitor of ASIC3 Channel Introduces Binding to Thumb Domain of ASIC1a but Reduces Analgesic Activity
by Timur A. Khasanov, Ekaterina E. Maleeva, Sergey G. Koshelev, Victor A. Palikov, Yulia A. Palikova, Igor A. Dyachenko, Sergey A. Kozlov, Yaroslav A. Andreev and Dmitry I. Osmakov
Mar. Drugs 2024, 22(9), 382; https://doi.org/10.3390/md22090382 - 24 Aug 2024
Viewed by 584
Abstract
Acid-sensing ion channels (ASICs), which act as proton-gating sodium channels, have garnered attention as pharmacological targets. ASIC1a isoform, notably prevalent in the central nervous system, plays an important role in synaptic plasticity, anxiety, neurodegeneration, etc. In the peripheral nervous system, ASIC1a shares prominence [...] Read more.
Acid-sensing ion channels (ASICs), which act as proton-gating sodium channels, have garnered attention as pharmacological targets. ASIC1a isoform, notably prevalent in the central nervous system, plays an important role in synaptic plasticity, anxiety, neurodegeneration, etc. In the peripheral nervous system, ASIC1a shares prominence with ASIC3, the latter well established for its involvement in pain signaling, mechanical sensitivity, and inflammatory hyperalgesia. However, the precise contributions of ASIC1a in peripheral functions necessitate thorough investigation. To dissect the specific roles of ASICs, peptide ligands capable of modulating these channels serve as indispensable tools. Employing molecular modeling, we designed the peptide targeting ASIC1a channel from the sea anemone peptide Ugr9-1, originally targeting ASIC3. This peptide (A23K) retained an inhibitory effect on ASIC3 (IC50 9.39 µM) and exhibited an additional inhibitory effect on ASIC1a (IC50 6.72 µM) in electrophysiological experiments. A crucial interaction between the Lys23 residue of the A23K peptide and the Asp355 residue in the thumb domain of the ASIC1a channel predicted by molecular modeling was confirmed by site-directed mutagenesis of the channel. However, A23K peptide revealed a significant decrease in or loss of analgesic properties when compared to the wild-type Ugr9-1. In summary, using A23K, we show that negative modulation of the ASIC1a channel in the peripheral nervous system can compromise the efficacy of an analgesic drug. These results provide a compelling illustration of the complex balance required when developing peripheral pain treatments targeting ASICs. Full article
(This article belongs to the Special Issue Marine Drug Discovery through Molecular Docking)
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18 pages, 1810 KiB  
Article
Mixotrophic Cultivation of Arthrospira platensis (Spirulina) under Salt Stress: Effect on Biomass Composition, FAME Profile and Phycocyanin Content
by Nicola Pio Russo, Marika Ballotta, Luca Usai, Serenella Torre, Maurizio Giordano, Giacomo Fais, Mattia Casula, Debora Dessì, Paola Nieri, Eya Damergi, Giovanni Antonio Lutzu and Alessandro Concas
Mar. Drugs 2024, 22(9), 381; https://doi.org/10.3390/md22090381 - 24 Aug 2024
Viewed by 828
Abstract
Arthrospira platensis holds promise for biotechnological applications due to its rapid growth and ability to produce valuable bioactive compounds like phycocyanin (PC). This study explores the impact of salinity and brewery wastewater (BWW) on the mixotrophic cultivation of A. platensis. Utilizing BWW [...] Read more.
Arthrospira platensis holds promise for biotechnological applications due to its rapid growth and ability to produce valuable bioactive compounds like phycocyanin (PC). This study explores the impact of salinity and brewery wastewater (BWW) on the mixotrophic cultivation of A. platensis. Utilizing BWW as an organic carbon source and seawater (SW) for salt stress, we aim to optimize PC production and biomass composition. Under mixotrophic conditions with 2% BWW and SW, A. platensis showed enhanced biomass productivity, reaching a maximum of 3.70 g L−1 and significant increases in PC concentration. This study also observed changes in biochemical composition, with elevated protein and carbohydrate levels under salt stress that mimics the use of seawater. Mixotrophic cultivation with BWW and SW also influenced the FAME profile, enhancing the content of C16:0 and C18:1 FAMES. The purity (EP of 1.15) and yield (100 mg g−1) of PC were notably higher in mixotrophic cultures, indicating the potential for commercial applications in food, cosmetics, and pharmaceuticals. This research underscores the benefits of integrating the use of saline water with waste valorization in microalgae cultivation, promoting sustainability and economic efficiency in biotechnological processes. Full article
(This article belongs to the Special Issue Algal Cultivation for Obtaining High-Value Products)
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17 pages, 9124 KiB  
Article
Exploring the Antimicrobial Potential of Hallachrome, a Defensive Anthraquinone from the Marine Worm Halla parthenopeia (Polychaeta)
by Anita Ferri, Roberto Simonini, Carla Sabia and Ramona Iseppi
Mar. Drugs 2024, 22(9), 380; https://doi.org/10.3390/md22090380 - 24 Aug 2024
Viewed by 402
Abstract
Antimicrobial resistance is a critical global health issue, with rising resistance among bacteria and fungi. Marine organisms have emerged as promising, but underexplored, sources of new antimicrobial agents. Among them, marine polychaetes, such as Halla parthenopeia, which possess chemical defenses, could attract [...] Read more.
Antimicrobial resistance is a critical global health issue, with rising resistance among bacteria and fungi. Marine organisms have emerged as promising, but underexplored, sources of new antimicrobial agents. Among them, marine polychaetes, such as Halla parthenopeia, which possess chemical defenses, could attract significant research interest. This study explores the antimicrobial properties of hallachrome, a unique anthraquinone found in the purple mucus of H. parthenopeia, against Gram-negative bacteria (Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 9027), Gram-positive bacteria (Enterococcus faecalis ATCC 29212, Staphylococcus aureus ATCC 6538, Staphylococcus epidermidis ATCC 12228), and the most common human fungal pathogen Candida albicans ATCC 10231. Antibacterial susceptibility testing revealed that Gram-negative bacteria were not inhibited by hallachrome at concentrations ≤2 mM. However, Gram-positive bacteria showed significant growth inhibition at 0.12–0.25 mM, while C. albicans was inhibited at 0.06 mM. Time-kill studies demonstrated dose-dependent growth inhibition of susceptible strains by hallachrome, which exerted its effect by altering the membrane permeability of C. albicans, E. faecalis, and S. epidermidis after 6 h and S. aureus after 24 h. Additionally, hallachrome significantly reduced biofilm formation and mature biofilm in S. aureus, E. faecalis, and C. albicans. Additionally, it inhibited hyphal growth in C. albicans. These findings highlight hallachrome’s potential as a novel antimicrobial agent, deserving further exploration for clinical experimentation. Full article
(This article belongs to the Special Issue Marine Drug Research in Italy)
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7 pages, 7698 KiB  
Editorial
Marine Collagen and Chitin: Promising Applications in Interdisciplinary Fields
by Azizur Rahman
Mar. Drugs 2024, 22(9), 379; https://doi.org/10.3390/md22090379 - 23 Aug 2024
Viewed by 402
Abstract
Marine collagen and chitin derived from marine organisms are gaining significant attention for their diverse applications across various fields [...] Full article
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21 pages, 11710 KiB  
Article
Enhanced Production of High-Value Porphyrin Compound Heme by Metabolic Engineering Modification and Mixotrophic Cultivation of Synechocystis sp. PCC6803
by Kai Cao, Fengjie Sun, Zechen Xin, Yujiao Cao, Xiangyu Zhu, Huan Tian, Tong Cao, Jinju Ma, Weidong Mu, Jiankun Sun, Runlong Zhou, Zhengquan Gao and Chunxiao Meng
Mar. Drugs 2024, 22(9), 378; https://doi.org/10.3390/md22090378 - 23 Aug 2024
Viewed by 444
Abstract
Heme, as an essential cofactor and source of iron for cells, holds great promise in various areas, e.g., food and medicine. In this study, the model cyanobacteria Synechocystis sp. PCC6803 was used as a host for heme synthesis. The heme synthesis pathway and [...] Read more.
Heme, as an essential cofactor and source of iron for cells, holds great promise in various areas, e.g., food and medicine. In this study, the model cyanobacteria Synechocystis sp. PCC6803 was used as a host for heme synthesis. The heme synthesis pathway and its competitive pathway were modified to obtain an engineered cyanobacteria with high heme production, and the total heme production of Synechocystis sp. PCC6803 was further enhanced by the optimization of the culture conditions and the enhancement of mixotrophic ability. The co-expression of hemC, hemF, hemH, and the knockout of pcyA, a key gene in the heme catabolic pathway, resulted in a 3.83-fold increase in the heme production of the wild type, while the knockout of chlH, a gene encoding a Mg-chelatase subunit and the key enzyme of the chlorophyll synthesis pathway, resulted in a 7.96-fold increase in the heme production of the wild type; further increased to 2.05 mg/L, its heme production was 10.25-fold that of the wild type under optimized mixotrophic culture conditions. Synechocystis sp. PCC6803 has shown great potential as a cell factory for photosynthetic carbon sequestration for heme production. This study provides novel engineering targets and research directions for constructing microbial cell factories for efficient heme production. Full article
(This article belongs to the Special Issue Algal Cultivation for Obtaining High-Value Products)
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