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体外和计算机模拟评估药用蘑菇Ganoderma neo-japonicum Imazeki 对人结肠癌细胞的抗癌作用。

In vitro and in silico anticancer evaluation of a medicinal mushroom, Ganoderma neo-japonicum Imazeki, against human colonic carcinoma cells.

机构信息

Department of Biomedical Science, Faculty of Medicine, University of Malaya, Kuala Lumpur, 50603, Malaysia.

Mushroom Research Centre, University of Malaya, Kuala Lumpur, 50603, Malaysia.

出版信息

Biotechnol Appl Biochem. 2021 Aug;68(4):902-917. doi: 10.1002/bab.2013. Epub 2020 Sep 13.

Abstract

Ganoderma neo-japonicum is a well-known medicinal mushroom in Asian countries. However, scientific validations on its curative activities are confined to cirrhosis and diabetes. In this study, the anticancer properties of G. neo-japonicum were evaluated using cellular and computational models. The ethanolic extract (EtOH) with a promising inhibitory effect was fractionated into four different fractions: hexane (Hex), chloroform (Chl), butanol (Btn), and aqueous (Aq). The active fractions were then subjected to cell apoptosis assessment and phytochemical profiling. Molecular docking was conducted to elucidate the affinity of selected constituents towards antiapoptotic Bcl-2 protein. The butanol fraction showed the highest antioxidant activities as well as total phenolic content. Both hexane and chloroform fractions exerted a potent cytotoxic effect on colonic carcinoma cells through the induction of apoptosis. Phytochemical analysis revealed that the chloroform fraction is terpenoid enriched whereas the hexane fraction comprises predominantly sterol constituents. Stellasterol and 1,25-dihydroxyvitamin D3 3-glycoside were demonstrated to have a high affinity towards Bcl-2 protein. Overall, G. neo-japonicum can be considered as a compelling therapeutic candidate for cancer treatment.

摘要

灵芝是亚洲国家广为人知的药用蘑菇。然而,其治疗活动的科学验证仅限于肝硬化和糖尿病。在这项研究中,使用细胞和计算模型评估了灵芝的抗癌特性。具有良好抑制作用的乙醇提取物(EtOH)被分为四个不同的馏分:正己烷(Hex)、氯仿(Chl)、正丁醇(Btn)和水(Aq)。然后对活性馏分进行细胞凋亡评估和植物化学分析。进行分子对接以阐明所选成分对抗细胞凋亡 Bcl-2 蛋白的亲和力。正丁醇馏分显示出最高的抗氧化活性和总酚含量。正己烷和氯仿馏分均通过诱导细胞凋亡对结肠癌细胞产生强烈的细胞毒性作用。植物化学分析表明,氯仿馏分富含萜类化合物,而正己烷馏分主要含有固醇成分。Stellasterol 和 1,25-二羟基维生素 D3 3-糖苷被证明与 Bcl-2 蛋白具有高亲和力。总的来说,灵芝可以被认为是癌症治疗的一种有吸引力的治疗候选物。

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