helvamide(helvamide) - 药物靶点：SOAT1 x SOAT2_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

SOAT1 x SOAT2

作用机制

SOAT1抑制剂(酰基辅酶A：胆固醇酰基转移酶-1抑制剂)、SOAT2 抑制剂(sterol O-acyltransferase 2 inhibitors)

治疗领域-

在研适应症-

非在研适应症-

原研机构

Kitasato University

在研机构

Kitasato University

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 helvamide 相关的临床结果

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100 项与 helvamide 相关的转化医学

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100 项与 helvamide 相关的专利（医药）

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1

项与 helvamide 相关的文献（医药）

2024-12-01·Natural Products and Bioprospecting

New piperazine derivatives helvamides B–C from the marine-derived fungus Penicillium velutinum ZK-14 uncovered by OSMAC (One Strain Many Compounds) strategy

Article

作者: Khudyakova, Yuliya V ; Gerasimenko, Andrey V ; Chingizov, Artur R ; Chausova, Viktoria E ; Kalinovsky, Anatoly I ; Kirichuk, Natalya N ; Leshchenko, Elena V ; Chingizova, Ekaterina A ; Shlyk, Nadezhda P ; Isaeva, Marina P ; Berdyshev, Dmitrii V ; Borkunov, Gleb V ; Yurchenko, Ekaterina A ; Popov, Roman S ; Antonov, Alexandr S ; Yurchenko, Anton N

AbstractFour extracts of the marine-derived fungus Penicillium velutinum J.F.H. Beyma were obtained via metal ions stress conditions based on the OSMAC (One Strain Many Compounds) strategy. Using a combination of modern approaches such as LC/UV, LC/MS and bioactivity data analysis, as well as in silico calculations, influence metal stress factors to change metabolite profiles Penicillium velutinum were analyzed. From the ethyl acetate extract of the P. velutinum were isolated two new piperazine derivatives helvamides B (1) and C (2) together with known saroclazin A (3) (4S,5R,7S)-4,11-dihydroxy-guaia-1(2),9(10)-dien (4). Their structures were established based on spectroscopic methods. The absolute configuration of helvamide B (1) as 2R,5R was determined by a combination of the X-ray analysis and by time-dependent density functional theory (TD-DFT) calculations of electronic circular dichroism (ECD) spectra. The cytotoxic activity of the isolated compounds against human prostate cancer PC-3 and human embryonic kidney HEK-293 cells and growth inhibition activity against yeast-like fungi Candida albicans were assayed.Graphical Abstract

100 项与 helvamide 相关的药物交易

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