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20 pages, 5265 KiB

Open AccessArticle

Isolation and Characterization of L-Asparaginase-Producing Bacteria from the Arabian–Persian Gulf Region: First Report on Bacillus xiamenensis ASP-J1-4 as a Producer and Its Potential Application

by Ghofran M. Al-Harbi, Essam Kotb, Abeer A. Almiman, Mahmoud M. Berekaa, Salwa Alhamad, Nada F. Alahmady, Meneerah A. Aljafary, Nadiyah M. Alqazlan, Reem I. Alyami, Joud M. Alqarni and Ebtesam Abdullah Al-Suhaimi

Mar. Drugs 2025, 23(5), 194; https://doi.org/10.3390/md23050194 - 29 Apr 2025

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Abstract

L-asparaginase (L-ASNase) functions as a chemotherapeutic enzyme with antitumor properties. It facilitates the degradation of L-asparagine (L-ASN), a vital amino acid required for the proliferation of tumor cells. In this study, we have isolated 177 L-ASNase-producing strains from the aquatic environment of the [...] Read more.

L-asparaginase (L-ASNase) functions as a chemotherapeutic enzyme with antitumor properties. It facilitates the degradation of L-asparagine (L-ASN), a vital amino acid required for the proliferation of tumor cells. In this study, we have isolated 177 L-ASNase-producing strains from the aquatic environment of the Arabian–Persian Gulf. The most potent isolate, ASP-J1-4, was an endophyte recovered from the seablite Suaeda maritima and was molecularly identified as B. xiamenensis (accession number PQ593941). The enzyme purified through DEAE-Sepharose displayed a molecular weight of 37 kDa based on the SDS-PAGE profile and lacked detectable L-glutaminase (L-GTNase) activity. Optimal enzyme activity was at 40 °C and pH 9.0, with stability at pH 7–9. The maximum stimulation effect was found in the presence of Fe³⁺, Mn²⁺, and Na⁺ ions, respectively. The enzyme demonstrated a V_max of 35.71 U/mL and a K_m of 0.15 mM. Interestingly, ASP-J1-4 L-ASNase showed a dose-dependent inhibition against human colon carcinoma (HCT-116) and cervical Henrietta Lacks (HeLa) cell lines, with IC₅₀ values of 15.42 µg/mL and 12.13 µg/mL, respectively. These findings collectively suggest a biocompatible, efficient, and robust enzyme for potential applications in tumor therapy after validation of in vivo studies and clinical trials. This study introduces the first deep screening program for L-ASNase-producing bacteria harboring in the Arabian–Persian Gulf region. In addition, it launches B. xiamenensis and other species as new sources of L-ASNase. Full article

(This article belongs to the Special Issue Pharmacological Potential of Marine Natural Products, 2nd Edition)

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14 pages, 6471 KiB

Open AccessArticle

Marine-Derived Yaequinolone Derivative CHNQD-02792 Suppresses Colorectal Cancer Cell Proliferation and Induces Apoptosis via MAPK Pathway Modulation

by Jia-Qi Kang, Tian-Yi Zhou, Wen-Hui Wang, Mei-Yan Wei and Chang-Lun Shao

Mar. Drugs 2025, 23(4), 136; https://doi.org/10.3390/md23040136 - 21 Mar 2025

Viewed by 466

Abstract

Colorectal cancer is currently the third most common malignancy, and the toxic side effects of clinical therapeutic drugs often influence treatment outcomes. Marine-derived quinolone alkaloids exhibit various biological activities and are particularly notable for their antitumor properties. Compounds 1–13 were semi-synthesized [...] Read more.

Colorectal cancer is currently the third most common malignancy, and the toxic side effects of clinical therapeutic drugs often influence treatment outcomes. Marine-derived quinolone alkaloids exhibit various biological activities and are particularly notable for their antitumor properties. Compounds 1–13 were semi-synthesized based on 4′-desmethoxyyaequinolone J1, which is a 4-phenyl derivative of the natural quinolone alkaloid yaequinolone J1 and was isolated from Penicillium sp. FKI-2140. This study is the first to investigate the antitumor activity of 1–13 in colorectal cancer cells through proliferation, clonality, apoptosis, cell cycle, and MAPK signaling pathway. Cytotoxicity screening against seven colorectal cancer cell lines revealed that CHNQD-02792 (13) had the most sensitivity to HT-29 cells (IC₅₀ = 4.5 μM), far exceeding positive control 5-fluorouracil (IC₅₀ = 15.58 μM). The plate cloning assay revealed that CHNQD-02792 completely inhibited the growth of HT-29 cells at the concentration of 9 μM. CHNQD-02792 (4.5 μM) inhibited CDK1 expression and triggered G2/M phase arrest in HT-29 cells. Mechanistic analysis revealed that CHNQD-02792 induced apoptosis by suppressing the anti-apoptotic protein Bcl-2 and upregulating the pro-apoptotic proteins Caspase-3 and Bax. Furthermore, CHNQD-02792 inhibited ERK and JNK phosphorylation and thus highlighted its regulatory role in MAPK signaling. These findings suggest that CHNQD-02792 exerts cytotoxic effects on HT-29 cells via dual mechanisms: inducing G2/M arrest and apoptosis while regulating MAPK signaling through ERK/JNK dephosphorylation. This study demonstrates the dual targeting of CHNQD-02792 against tumor cell proliferation and survival pathways, providing a foundation for further development of anti-colorectal cancer drugs. Full article

(This article belongs to the Special Issue Pharmacological Potential of Marine Natural Products, 2nd Edition)

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32 pages, 4710 KiB

Open AccessArticle

The Benthic Dinoflagellate Coolia malayensis (Dinophyceae) Produces an Array of Compounds with Antineoplastic Activity in Cells of Tumor Origin

by Itzel B. Morales-Montesinos, Maria Yolanda Rios, Yordin D. Ocampo-Acuña, Baldomero Esquivel-Rodríguez, Celia Bustos-Brito, María del Carmen Osorio-Ramírez, Lorena M. Durán-Riveroll and Leticia González-Maya

Mar. Drugs 2025, 23(3), 127; https://doi.org/10.3390/md23030127 - 14 Mar 2025

Viewed by 1366

Abstract

Among aquatic organisms, marine dinoflagellates are essential sources of bioactive metabolites. The benthic dinoflagellate Coolia malayensis produces metabolites that have exhibited substantial and specific cytotoxicity on cancer cells; however, isolation and identification of the purified compounds remain a challenge. This study reports C. [...] Read more.

Among aquatic organisms, marine dinoflagellates are essential sources of bioactive metabolites. The benthic dinoflagellate Coolia malayensis produces metabolites that have exhibited substantial and specific cytotoxicity on cancer cells; however, isolation and identification of the purified compounds remain a challenge. This study reports C. malayensis biomass multi-step extraction plus chemical analyses for identifying compounds with antineoplastic activity. Through bio-directed fractionation, the cytotoxicity of extracts and fractions was tested on H1299 (lung), PC-3 (prostate), HeLa (cervical), and MCF-7 (breast) cancer cell lines. Dichloromethane (DCM) phase, hydroalcoholic (HYD) secondary extract, and methanolic (MET) extract showed cytotoxic effects on all cell lines. Active extracts and fractions were analyzed by HPLC-QTOF-MS, ¹H, and ¹³C NMR. Cell lines H1299 and PC-3 treated with fractions F4, F7, and DCM2-AQ-Ch sub-extract showed morphological changes resembling those observed in the apoptosis control, and no signs of necrosis were observed. The selectivity of fraction F7 was above 100 μg mL⁻¹ for healthy cells, while cytotoxic activity was observed in cancer cells. This fraction was identified as mostly fatty acids (FA) by NMR. Seventeen compounds with reported biological activities, such as antioxidant, analgesic, antiviral, and anticancer, were identified from C. malayensis extracts and fractions. Among them, the phycotoxins gambieric acid A and B, okadaic acid, and dinophysistoxin-1 were detected. Further studies are needed to reveal more significant anti-cancer potential from C. malayensis. Full article

(This article belongs to the Special Issue Pharmacological Potential of Marine Natural Products, 2nd Edition)

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20 pages, 7039 KiB

Open AccessArticle

Characterization of Flexusin A, a Novel Circular Bacteriocin Produced by Marine Bacterium Bacillus flexus R29-2

by Xiaoni Qiao, Xiaowen Sun, Shuting Wang, Chen Zhai, Wei Tang, Tao Tang, Jun Zhang and Zengguo He

Mar. Drugs 2025, 23(3), 95; https://doi.org/10.3390/md23030095 - 21 Feb 2025

Viewed by 695

Abstract

Circular bacteriocins are potent antimicrobials against pathogenic Gram-positives. In searching for marine bacteriocins, an antibacterial peptide (flexusin A) was purified from the fermentation broth of marine bacterium Bacillus flexus R29-2. Genome sequencing and gene annotation revealed the chromosome contained an unknown circular bacteriocin [...] Read more.

Circular bacteriocins are potent antimicrobials against pathogenic Gram-positives. In searching for marine bacteriocins, an antibacterial peptide (flexusin A) was purified from the fermentation broth of marine bacterium Bacillus flexus R29-2. Genome sequencing and gene annotation revealed the chromosome contained an unknown circular bacteriocin gene cluster. Approaches including shot-gun proteomics analysis, AntiSMASH and BAGEL4 predication as well as the comprehensive sequence alignment, were then conducted, respectively, to verify the correlation of flexusin A with the gene-encoded precursor peptide. The results confirmed that flexusin A was the mature circular bacteriocin of the predicated precursor peptide with six amino acids as leader peptide. Flexusin A was 6098.4 Da in size, with a net charge of +3 and PI of 9.60. It shared the typical saposin-like fold spatial conformation features as commonly found in other circular bacteriocins. Flexusin A was pH, thermal, and protease tolerant. It exhibited a narrow antimicrobial spectrum against Gram-positives, and it can strongly inhibit Staphylococcus aureus by causing cell destruction via membrane destabilization. Taken together, a novel circular bacteriocin flexusin A was identified in this work. The characterization of flexusin A has extended circular bacteriocins family to 26 members. This is also the first report on bacteriocin production by B. flexus. Full article

(This article belongs to the Special Issue Pharmacological Potential of Marine Natural Products, 2nd Edition)

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15 pages, 6024 KiB

Open AccessArticle

Identification of Filovirus Entry Inhibitors from Marine Fungus-Derived Indole Alkaloids

by Leah Liu Wang, Javier Seravalli, Brett Eaton, Yi Liu, Michael R. Holbrook, Wen-Jian Lan and Shi-Hua Xiang

Mar. Drugs 2025, 23(1), 23; https://doi.org/10.3390/md23010023 - 3 Jan 2025

Cited by 1 | Viewed by 1265

Abstract

Filoviruses, mainly consisting of the two genera of Ebolavirus and Marburgvirus, are enveloped negative-strand RNA viruses that can infect humans to cause severe hemorrhagic fevers and outbreaks with high mortality rates. However, we still do not have effective medicines for treating these [...] Read more.

Filoviruses, mainly consisting of the two genera of Ebolavirus and Marburgvirus, are enveloped negative-strand RNA viruses that can infect humans to cause severe hemorrhagic fevers and outbreaks with high mortality rates. However, we still do not have effective medicines for treating these diseases. To search for effective drugs, we have identified three marine indole alkaloids that exhibit potent activities against filovirus infection. Thus, it is suggested that marine indole alkaloids can be a valuable compound source for filovirus drug screening and development. Since marine indole alkaloids comprise a large diverse group of secondary metabolites, their biological properties would be helpful for pharmaceutical drug development to treat various filovirus infections. Full article

(This article belongs to the Special Issue Pharmacological Potential of Marine Natural Products, 2nd Edition)

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13 pages, 2160 KiB

Open AccessArticle

Heterocycles and a Sorbicillinoid from the Coral-Derived Fungus Penicillium chrysogenum

by Junjie Yang, Yuan Zong, Cili Wang, Kai Li, Yue Zhang and Pinglin Li

Mar. Drugs 2024, 22(11), 517; https://doi.org/10.3390/md22110517 - 15 Nov 2024

Viewed by 1291

Abstract

A detailed chemical study of the culture of a coral-derived fungus Penicillium chrysogenum resulted in the isolation and identification of four new aromatic heterocycles chrysoquinazolinones A–B (1–2) and chrysobenzothiazoles A–B (3–4), along with a new [...] Read more.

A detailed chemical study of the culture of a coral-derived fungus Penicillium chrysogenum resulted in the isolation and identification of four new aromatic heterocycles chrysoquinazolinones A–B (1–2) and chrysobenzothiazoles A–B (3–4), along with a new sorbicillinoid 4-carboxylsorbicillin (5). Chrysoquinazolinones A–B (1–2) combine a quinazolinone fragment with a bicyclo[2.2.2]octane or a pyrrolidone moiety, respectively, demonstrating the unexpected structures of marine natural products. Chrysobenzothiazoles A–B (3–4) possess a benzothiazole system and are the second isolation of this class of skeleton compounds from marine organisms. The existence of the pair of enantiomers (±3) was deduced by chiral HPLC analysis. Their structures and absolute configurations were elucidated by detailed spectroscopic analysis, comparison with the literature data, single-crystal X-ray crystallographic analysis and TDDFT-ECD calculations. Compound 5 exhibited moderate cytotoxicity against K562 and NCI-H446 cell lines, with IC₅₀ values of 15.00 μM and 16.87 μM, respectively. Full article

(This article belongs to the Special Issue Pharmacological Potential of Marine Natural Products, 2nd Edition)

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14 pages, 3526 KiB

Open AccessArticle

Talaroterpenoids A–F: Six New Seco-Terpenoids from the Marine-Derived Fungus Talaromyces aurantiacus

by Zi-Hong Peng, Hui Jia, Yan-Liang Luo, Li-Jun Zhang, Jia-Tong Zhou, Yuan-Han Xie, Li-Jun Wang, Jiang-Ke Qin, Jun Li, Guo-Hai Zhang, Rui-Yun Yang and Wei-Feng Xu

Mar. Drugs 2024, 22(10), 475; https://doi.org/10.3390/md22100475 - 18 Oct 2024

Cited by 1 | Viewed by 1435

Abstract

Six new highly oxidized seco-terpenoids, including three 3-nor-labdane type diterpenes, talaroterpenoids A–C (1–3), and three meroterpenoids containing an orthoester group, talaroterpenoids D–F (6–8), together with five known compounds (4–5 [...] Read more.

Six new highly oxidized seco-terpenoids, including three 3-nor-labdane type diterpenes, talaroterpenoids A–C (1–3), and three meroterpenoids containing an orthoester group, talaroterpenoids D–F (6–8), together with five known compounds (4–5 and 9–11), were isolated from the marine-derived fungus Talaromyces aurantiacus. Their chemical structures were elucidated through 1D, 2D NMR, HRESIMS, J-based configuration analysis (JBCA), computational ECD calculations, and single-crystal X-ray diffraction analysis. Compounds 1 and 2 contain an unusual 6,20-γ-lactone-bridged scaffold. Compounds 10 and 11 presented inhibitory effects on NO release in lipopolysaccharide (LPS)-induced BV-2 cells with IC₅₀ values of 11.47 and 11.32 μM, respectively. Talaroterpenoid C (3) showed moderate antifungal activity against A. alternata and P. theae Steyaert. Full article

(This article belongs to the Special Issue Pharmacological Potential of Marine Natural Products, 2nd Edition)

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18 pages, 2458 KiB

Open AccessArticle

Semisynthesis, Structure Elucidation and Anti-Mycobacterium marinum Activity of a Series of Marine-Derived 14-Membered Resorcylic Acid Lactones with Interesting Ketal Groups

by Jun-Na Yin, Cui-Fang Wang, Xiu-Li Zhang, Ya-Jie Cheng, Yan-Wei Wu, Qun Zhang, Chang-Lun Shao, Mei-Yan Wei and Yu-Cheng Gu

Mar. Drugs 2024, 22(10), 431; https://doi.org/10.3390/md22100431 - 25 Sep 2024

Cited by 1 | Viewed by 1302

Abstract

The incidence of Mycobacterium marinum infection is on the rise; however, the existing drug treatment cycle is lengthy and often requires multi-drug combination. Therefore, there is a need to develop new and effective anti-M. marinum drugs. Cochliomycin A, a 14-membered resorcylic acid [...] Read more.

The incidence of Mycobacterium marinum infection is on the rise; however, the existing drug treatment cycle is lengthy and often requires multi-drug combination. Therefore, there is a need to develop new and effective anti-M. marinum drugs. Cochliomycin A, a 14-membered resorcylic acid lactone with an acetonide group at C-5′ and C-6′, exhibits a wide range of antimicrobial, antimalarial, and antifouling activities. To further explore the effect of this structural change at C-5′ and C-6′ on this compound’s activity, we synthesized a series of compounds with a structure similar to that of cochliomycin A, bearing ketal groups at C-5′ and C-6′. The R/S configuration of the diastereoisomer at C-13′ was further determined through an NOE correlation analysis of CH₃ or CH₂ at the derivative C-13′ position and the H-5′ and H-6′ by means of a 1D NOE experiment. Further comparative ¹H NMR analysis of diastereoisomers showed the difference in the chemical shift (δ) value of the diastereoisomers. The synthetic compounds were screened for their anti-microbial activities in vitro. Compounds 15–24 and 28–35 demonstrated promising activity against M. marinum, with MIC₉₀ values ranging from 70 to 90 μM, closely approaching the MIC₉₀ of isoniazid. The preliminary structure–activity relationships showed that the ketal groups with aromatic rings at C-5′ and C-6′ could enhance the inhibition of M. marinum. Further study demonstrated that compounds 23, 24, 29, and 30 had significant inhibitory effects on M. marinum and addictive effects with isoniazid and rifampicin. Its effective properties make it an important clue for future drug development toward combatting M. marinum resistance. Full article

(This article belongs to the Special Issue Pharmacological Potential of Marine Natural Products, 2nd Edition)

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16 pages, 4560 KiB

Open AccessArticle

The Cytochalasins and Polyketides from a Mangrove Endophytic Fungus Xylaria arbuscula QYF

by Qi Tan, Xinyu Ye, Siqi Fu, Yihao Yin, Yufeng Liu, Jianying Wu, Fei Cao, Bo Wang, Tingshun Zhu, Wencong Yang and Zhigang She

Mar. Drugs 2024, 22(9), 407; https://doi.org/10.3390/md22090407 - 5 Sep 2024

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Abstract

Twelve compounds, including four undescribed cytochalasins, xylariachalasins A–D (1–4), four undescribed polyketides (5–8), and four known cytochalasins (9–12), were isolated from the mangrove endophytic fungus Xylaria arbuscula QYF. Their structures and [...] Read more.

Twelve compounds, including four undescribed cytochalasins, xylariachalasins A–D (1–4), four undescribed polyketides (5–8), and four known cytochalasins (9–12), were isolated from the mangrove endophytic fungus Xylaria arbuscula QYF. Their structures and absolute configurations were established by extensive spectroscopic analyses (1D and 2D NMR, HRESIMS), electronic circular dichroism (ECD) calculations, ¹³C NMR calculation and DP4+ analysis, single-crystal X-ray diffraction, and the modified Mosher ester method. Compounds 1 and 2 are rare cytochalasin hydroperoxides. In bioactivity assays, Compound 2 exhibited moderate antimicrobial activities against Staphylococcus aureus and Candida albicans with MIC values of 12.5 μM for both Compound 10 exhibited significant cytotoxic activity against MDA-MB-435 with an IC₅₀ value of 3.61 ± 1.60 μM. Full article

(This article belongs to the Special Issue Pharmacological Potential of Marine Natural Products, 2nd Edition)

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16 pages, 13502 KiB

Open AccessArticle

Identification of Penexanthone A as a Novel Chemosensitizer to Induce Ferroptosis by Targeting Nrf2 in Human Colorectal Cancer Cells

by Genshi Zhao, Yanying Liu, Xia Wei, Chunxia Yang, Junfei Lu, Shihuan Yan, Xiaolin Ma, Xue Cheng, Zhengliang You, Yue Ding, Hongwei Guo, Zhiheng Su, Shangping Xing and Dan Zhu

Mar. Drugs 2024, 22(8), 357; https://doi.org/10.3390/md22080357 - 6 Aug 2024

Cited by 4 | Viewed by 1799

Abstract

Ferroptosis has emerged as a potential mechanism for enhancing the efficacy of chemotherapy in cancer treatment. By suppressing nuclear factor erythroid 2-related factor 2 (Nrf2), cancer cells may lose their ability to counteract the oxidative stress induced by chemotherapy, thereby becoming more susceptible [...] Read more.

Ferroptosis has emerged as a potential mechanism for enhancing the efficacy of chemotherapy in cancer treatment. By suppressing nuclear factor erythroid 2-related factor 2 (Nrf2), cancer cells may lose their ability to counteract the oxidative stress induced by chemotherapy, thereby becoming more susceptible to ferroptosis. In this study, we investigate the potential of penexanthone A (PXA), a xanthone dimer component derived from the endophytic fungus Diaporthe goulteri, obtained from mangrove plant Acanthus ilicifolius, to enhance the therapeutic effect of cisplatin (CDDP) on colorectal cancer (CRC) by inhibiting Nrf2. The present study reported that PXA significantly improved the ability of CDDP to inhibit the activity of and induce apoptosis in CRC cells. Moreover, PXA was found to increase the level of oxidative stress and DNA damage caused by CDDP. In addition, the overexpression of Nrf2 reversed the DNA damage and ferroptosis induced by the combination of PXA and CDDP. In vivo experiments using zebrafish xenograft models demonstrated that PXA enhanced the therapeutic effect of CDDP on CRC. These studies suggest that PXA enhanced the sensitivity of CRC to CDDP and induce ferroptosis by targeting Nrf2 inhibition, indicating that PXA might serve as a novel anticancer drug in combination chemotherapy. Full article

(This article belongs to the Special Issue Pharmacological Potential of Marine Natural Products, 2nd Edition)

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Review

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45 pages, 6883 KiB

Open AccessReview

Natural Products from Marine-Derived Fungi with Anti-Inflammatory Activity

by Yikang Qiu, Shiji Chen, Miao Yu, Jueying Shi, Jiayu Liu, Xiaoyang Li, Jiaxing Chen, Xueping Sun, Guolei Huang and Caijuan Zheng

Mar. Drugs 2024, 22(10), 433; https://doi.org/10.3390/md22100433 - 25 Sep 2024

Cited by 5 | Viewed by 5306

Abstract

Inflammation is considered as one of the most primary protective innate immunity responses, closely related to the body’s defense mechanism for responding to chemical, biological infections, or physical injuries. Furthermore, prolonged inflammation is undesirable, playing an important role in the development of various [...] Read more.

Inflammation is considered as one of the most primary protective innate immunity responses, closely related to the body’s defense mechanism for responding to chemical, biological infections, or physical injuries. Furthermore, prolonged inflammation is undesirable, playing an important role in the development of various diseases, such as heart disease, diabetes, Alzheimer’s disease, atherosclerosis, rheumatoid arthritis, and even certain cancers. Marine-derived fungi represent promising sources of structurally novel bioactive natural products, and have been a focus of research for the development of anti-inflammatory drugs. This review covers secondary metabolites with anti-inflammatory activities from marine-derived fungi, over the period spanning August 2018 to July 2024. A total of 285 anti-inflammatory metabolites, including 156 novel compounds and 11 with novel skeleton structures, are described. Their structures are categorized into five categories: terpenoids, polyketides, nitrogen-containing compounds, steroids, and other classes. The biological targets, as well as the in vitro and in vivo screening models, were surveyed and statistically summarized. This paper aims to offer valuable insights to researchers in the exploration of natural products and the discovery of anti-inflammatory drugs. Full article

(This article belongs to the Special Issue Pharmacological Potential of Marine Natural Products, 2nd Edition)

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22 pages, 2173 KiB

Open AccessReview

Recent Advances in Marine-Derived Compounds as Potent Antibacterial and Antifungal Agents: A Comprehensive Review

by Devaraj Bharathi and Jintae Lee

Mar. Drugs 2024, 22(8), 348; https://doi.org/10.3390/md22080348 - 29 Jul 2024

Cited by 4 | Viewed by 6728

Abstract

The increase in antimicrobial resistance (AMR) in microorganisms is a significant global health concern. Various factors contribute to AMR, including alterations in cell membrane permeability, increased efflux pump activity, enzymatic modification or inactivation of antibiotics, target site changes, alternative metabolic pathways, and biofilm [...] Read more.

The increase in antimicrobial resistance (AMR) in microorganisms is a significant global health concern. Various factors contribute to AMR, including alterations in cell membrane permeability, increased efflux pump activity, enzymatic modification or inactivation of antibiotics, target site changes, alternative metabolic pathways, and biofilm formation. Marine environments, with their extensive biodiversity, provide a valuable source of natural products with a wide range of biological activities. Marine-derived antimicrobial compounds show significant potential against drug-resistant bacteria and fungi. This review discusses the current knowledge on marine natural products such as microorganisms, sponges, tunicates and mollusks with antibacterial and antifungal properties effective against drug-resistant microorganisms and their ecological roles. These natural products are classified based on their chemical structures, such as alkaloids, amino acids, peptides, polyketides, naphthoquinones, terpenoids, and polysaccharides. Although still in preclinical studies, these agents demonstrate promising in vivo efficacy, suggesting that marine sources could be pivotal in developing new drugs to combat AMR, thereby fulfilling an essential medical need. This review highlights the ongoing importance of marine biodiversity exploration for discovering potential antimicrobial agents. Full article

(This article belongs to the Special Issue Pharmacological Potential of Marine Natural Products, 2nd Edition)

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44 pages, 3898 KiB

Open AccessReview

Recent Discovery of Nitrogen Heterocycles from Marine-Derived Aspergillus Species

by Jueying Shi, Miao Yu, Weikang Chen, Shiji Chen, Yikang Qiu, Zhenyang Xu, Yi Wang, Guolei Huang and Caijuan Zheng

Mar. Drugs 2024, 22(7), 321; https://doi.org/10.3390/md22070321 - 18 Jul 2024

Cited by 2 | Viewed by 3775

Abstract

Nitrogen heterocycles have drawn considerable attention because of their structurally novel and significant biological activities. Marine-derived fungi, especially the Aspergillus species, possess unique metabolic pathways to produce secondary metabolites with novel structures and potent biological activities. This review prioritizes the structural diversity and [...] Read more.

Nitrogen heterocycles have drawn considerable attention because of their structurally novel and significant biological activities. Marine-derived fungi, especially the Aspergillus species, possess unique metabolic pathways to produce secondary metabolites with novel structures and potent biological activities. This review prioritizes the structural diversity and biological activities of nitrogen heterocycles that are produced by marine-derived Aspergillus species from January 2019 to January 2024, and their relevant biological activities. A total of 306 new nitrogen heterocycles, including seven major categories—indole alkaloids, diketopiperazine alkaloids, quinazoline alkaloids, isoquinoline alkaloids pyrrolidine alkaloids, cyclopeptide alkaloids, and other heterocyclic alkaloids—are presented in this review. Among these nitrogen heterocycles, 52 compounds had novel skeleton structures. Remarkably, 103 compounds showed various biological activities, such as cytotoxic, antimicrobial, anti-inflammatory, antifungal, anti-virus, and enzyme-inhibitory activities, and 21 compounds showed potent activities. This paper will guide further investigations into the structural diversity and biological activities of nitrogen heterocycles derived from the Aspergillus species and their potential contributions to the future development of new natural drug products in the medicinal and agricultural fields. Full article

(This article belongs to the Special Issue Pharmacological Potential of Marine Natural Products, 2nd Edition)

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