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Dysamide U,a new trichlorinated Diketopiperazine from the sponge Dysidea sp.

Chinese Journal of Chemistry 2000年第6期18卷 882-885页

作者：符雄苏镜娱曾陇梅 Department of Chemistry Zhongshan University Guangzhou Guangdong 510275 China

Dysamide U, a new trichlorinated Diketopiperazine (1) along with seven known ones (2–8) were isolated from the sponge of Dysidea sp. collected from the Pacific ocean. The structure of dysamide U (l) was elucidated by... 详细信息

关键词： Sponges Dysidea dipeptide Diketopiperazine

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Antibacterial sorbicillin and Diketopiperazines from the endogenous fungus Penicillium sp. GD6 associated Chinese mangrove Bruguiera gymnorrhiza

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Chinese Journal of Natural Medicines 2018年第5期16卷 358-365页

作者： JIANG Cheng-Shi ZHOU Zhen-Fang YANG Xiao-Hong LAN Le-Fu GU Yu-Cheng YE Bo-Ping GUO Yue-Wei China State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai 201203 China School of Biological Science and Technology University of Jinan Jinan 250022 China School of Life Science & Technology China Pharmaceutical University Nanjing 210009 China Syngenta Jealott's Hill International Research Centre Berkshire RG42 6EY United Kingdom

One new sorbicillin derivative, 2-deoxy-sohirnone C(1), one new Diketopiperazine alkaloid, 5 S-hydroxynorvalineS-Ile(2), and two naturally occurring Diketopiperazines, 3 S-hydroxylcyclo(S-Pro-S-Phe)(3) and cyclo(S-Phe-S-Gln)(4), together with three known compounds were isolated from the Chinese mangrove endophytic fungus Penicillium sp. GD6. Their structures were determined on the basis of extensive spectroscopic analyses and by comparison with literature data. The absolute configuration of 3-hydroxyl moiety in 3 was determined by Mosher's method, while the absolute stereochemistry of 2 and 4 was established by comparison with the CD spectra of natural and synthesized Diketopiperazines. Compound 1 showed moderate antibacterial activity against Methicillin-resistant Staphylococcus aureus with a MIC value of 80 μg·m L^(-1).

关键词： Mangrove Penicillium sp. Sorbicillin derivative Diketopiperazine alkaloids

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Three nitrogen-containing metabolites from an algicolous isolate of Trichoderma asperellum

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Marine Life Science & Technology 2020年第2期2卷 155-160页

作者： Yinping Song Fengping Miao Xiuli Yin Naiyun Ji Yantai Institute of Coastal Zone Research Chinese Academy of SciencesYantai 264003China

As one of the most productive species,Trichoderma asperellum,especially isolated from marine algae,has contributed a number of new terpenes and nitrogen-bearing compounds,encouraging our continuous efforts to further explore them.Consequently,three new nitrogen-containing secondary metabolites,including cyclo(L-5-MeO-Pro-L-5-MeO-Pro)(1),5'-acetoxy-deoxycyclonerin B(2),and 5'-acetoxy-deoxycyclonerin D(3)were isolated from the marine alga-derived endophytic fungus Trichoderma asperellum A-YMD-9-2.Their structures and relative configurations were fully elucidated through spectroscopic techniques,mainly including 1D/2D NMR and MS.The absolute configurations of 1 and 2 were ascertained on the basis of X-ray diffraction(Cu Kα radiation)and ECD data,respectively.The isolation of these new nitrogen-bearing compounds adds to the structural diversity of marine algicolous Trichoderma spp.,and they display potent inhibition against some marine phytoplankton species.

关键词： Trichoderma Diketopiperazine Sesquiterpene Cyclonerane

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Synthesis and Pharmacokinetic Property Improvement of Deuterated Plinabulin 9

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Journal of Ocean University of China 2017年第2期16卷 305-310页

作者： ZHAO Jianchun CHENG Hejuan SUN Tianwen WANG Shixiao DING Zhongpeng DOU Guifang MENG Zhiyun GUAN Huashi LI Wenbao Key Laboratory of Marine Drugs of Ministry of Education of China School of Medicine and PharmacyOcean University of ChinaQingdao 266003P.R.China Marine Biomedical Research Institute of Qingdao Qingdao 266073P.R.China Institute of Transfusion Medicine Academy of Military Medical ScienceBeijing 100850P.R.China

Plinabulin,a potent microtubule-targeting agent,is derived from marine natural Diketopiperazine ‘phenylahistin'.To develop novel plinabulin analogue that could display better pharmacokinetic properties and less side effects,deuterated plinabulin 9 was synthesized and evaluated in vitro and in vivo.In comparison with plinabulin,in vivo pharmacokinetic studies indicated that the deuterated derivative 9 could alter blood circulation behavior obviously,which was proved by increased area under the plasma concentration-time curve(AUC_(0–∞)),reduced clearance(CL),and prolonged total body mean residence time(MRT).The derivative 9 also has higher inhibition rates against Bx PC-3,Jurkat and A-431 tumor cell lines as compared with its prototype plinabulin.Therefore,the deuterated compound 9 might be developed as a potential agent for different cancer treatments.

关键词： plinabulin Diketopiperazine antitumor deuteration pharmacokinetics

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