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来自海绵Spongosorites sp.的双(吲哚)生物碱的抗菌活性和细胞毒性

Antimicrobial activity and cytotoxicity of bis(indole) alkaloids from the sponge Spongosorites sp.

作者信息

Oh Ki-Bong, Mar Woongchon, Kim Sanghee, Kim Ji-Yun, Lee Tae-Hoon, Kim Jae-Gyu, Shin Daehyun, Sim Chung J, Shin Jongheon

机构信息

Seoul National University, School of Agricultural Biotechnology, Korea.

出版信息

Biol Pharm Bull. 2006 Mar;29(3):570-3. doi: 10.1248/bpb.29.570.

Abstract

Bis(indole) alkaloids, of the topsentin class (1-4) and hamacanthin class (5-9), isolated from the marine sponge Spongosorites sp. were investigated using several biological assays. In the evaluation of antimicrobial activity against various strains of bacteria and fungi, compounds of the hamacanthin class exhibited more potent antibacterial activity than those of the topsentin class. Deoxytopsentin (1) and hamacanthin A (5) also exhibited significant antibacterial activity against methicillin-resistant Staphylococcus aureus, with MIC values of less than 12.5 microg/ml. In the antifungal activity test, hamacanthins, especially hamacanthin A (5), showed potent inhibitory activity against medically important pathogenic fungi. In contrast, all of the topsentins (1-4) were inactive against fungal growth. These compounds (1-9) also exhibited moderate cytotoxicity against cancer cell lines at concentrations between 1.1 and >20 microg/ml.

摘要

从海洋海绵Spongosorites sp.中分离得到的托普西汀类(1 - 4)和哈马坎汀类(5 - 9)双(吲哚)生物碱,通过多种生物学试验进行了研究。在针对各种细菌和真菌菌株的抗菌活性评估中,哈马坎汀类化合物表现出比托普西汀类更强的抗菌活性。脱氧托普西汀(1)和哈马坎汀A(5)对耐甲氧西林金黄色葡萄球菌也表现出显著的抗菌活性,最低抑菌浓度(MIC)值小于12.5微克/毫升。在抗真菌活性测试中,哈马坎汀类,尤其是哈马坎汀A(5),对医学上重要的致病真菌显示出强效抑制活性。相比之下,所有托普西汀(1 - 4)对真菌生长均无活性。这些化合物(1 - 9)在浓度为1.1至>20微克/毫升之间时,对癌细胞系也表现出中等程度的细胞毒性。

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