Two new alkaloids, polycarpine (1) and N,N-didesmethylgrossularine-1 (4), have been isolated from extracts of the ascidian Polycarpa aurata collected in Chuuk, Federated States of Micronesia. Three degradation products of 1 were also isolated. The structures of 1, 2, and 4 were determined by X-ray crystallography. The dimeric disulfide 1 inhibited the enzyme inosine monophosphate dehydrogenase, but the inhibition could be reversed by addition of excess dithiothreitol suggesting that 1 reacts with sulfhydryl groups on the enzyme.
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Bioorg Med Chem Lett
May 2024
Key Laboratory of Marine Drugs of Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China; Center for Innovation Marine Drug Screening & Evaluation of Pilot National Laboratory for Marine Science and Technology (Qingdao), Qingdao 266237, China; Marine Biomedical Research Institute of Qingdao, Qingdao 266003, China. Electronic address:
Coronaviruses (CoVs) are responsible for a wide range of illnesses in both animals and human. The main protease (M) of CoVs is an attractive drug target, owing its critical and highly conserved role in viral replication. Here, we developed and refined an enzymatic technique to identify putative M inhibitors from 189 marine chemicals and 46 terrestrial natural products.
View Article and Find Full Text PDFMar Drugs
December 2023
Department of Pharmacy, School of Medicine and Surgery, University of Naples Federico II, Via D. Montesano 49, 80131 Naples, Italy.
Hydrogen sulfide (HS) is a signaling molecule endogenously produced within mammals' cells that plays an important role in inflammation, exerting anti-inflammatory effects. In this view, the research has shown a growing interest in identifying natural HS donors. Herein, for the first time, the potential of marine extract as a source of HS-releasing agents has been explored.
View Article and Find Full Text PDFMar Drugs
March 2020
Griffith Institute for Drug Discovery, Griffith University, Brisbane, Queensland 4111, Australia.
In recent years, there has been a revival of interest in phenotypic-based drug discovery (PDD) due to target-based drug discovery (TDD) falling below expectations. Both PDD and TDD have their unique advantages and should be used as complementary methods in drug discovery. The PhenoTarget approach combines the strengths of the PDD and TDD approaches.
View Article and Find Full Text PDFMar Drugs
May 2019
The NeaNat Group, Department of Pharmacy, University of Naples "Federico II", Via D. Montesano 49, 80131 Napoli, Italy.
A deep study of the metabolic content of the tunicate , collected from Indonesian coast, afforded the isolation of two novel alkaloids, polyaurines A () and B (), along with two new -substituted benzoyl derivatives ( and ) and four known compounds (-). The structural elucidation of the new secondary metabolites was assigned by 1D, 2D NMR, and HRESIMS techniques. Computational studies resulted a useful tool to unambiguously determine in polyaurine B the presence of rarely found 1,2,4-thiadiazole ring.
View Article and Find Full Text PDFJ Biomed Sci
January 2016
Department of Pharmacology, College of Medicine, National Cheng Kung University, Tainan, Taiwan.
Background: Glioblastoma multiforme (GBM) is the most lethal primary brain tumors which remains difficult to cure despite advances in surgery, radiotherapy and chemotherapy. Therefore, the development of new drug is urgently needed. α-carboline derivatives were usually isolated from marine animals such as Britannia marine tunicate Dendrodoa grossularia and Indonesian ascidian Polycarpa aurata.
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