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与菌丝体相关的灵芝羊毛甾烷型三萜类化合物的抗结核活性。

Antitubercular Activity of Mycelium-Associated Ganoderma Lanostanoids.

作者信息

Isaka Masahiko, Chinthanom Panida, Sappan Malipan, Supothina Sumalee, Vichai Vanicha, Danwisetkanjana Kannawat, Boonpratuang Thitiya, Hyde Kevin D, Choeyklin Rattaket

机构信息

National Center for Genetic Engineering and Biotechnology (BIOTEC) , 113 Thailand Science Park, Phaholyothin Road, Klong Luang, Pathumthani 12120, Thailand.

Center of Excellence in Fungal Research, Mae Fah Luang University , Chiang Rai 57100, Thailand.

出版信息

J Nat Prod. 2017 May 26;80(5):1361-1369. doi: 10.1021/acs.jnatprod.6b00973. Epub 2017 May 15.

Abstract

In a continuation of our research into antitubercular lanostane triterpenoids from submerged cultures of Ganoderma species, three strains, Ganoderma orbiforme BCC 22325, Ganoderma sp. BCC 60695, and Ganoderma australe BCC 22314, have been investigated. Fourteen new lanostane triterpenoids, together with 35 known compounds, were isolated. Antitubercular activities of these mycelium-associated Ganoderma lanostanoids against Mycobacterium tuberculosis H37Ra were evaluated. Taken together with the assay data of previously isolated compounds, structure-activity relationships of the antitubercular activity are proposed. Most importantly, 3β- and 15α-acetoxy groups were shown to be critical for antimycobacterial activity. The most potent compound was (24E)-3β,15α-diacetoxylanosta-7,9(11),24-trien-26-oic acid (35).

摘要

在我们对灵芝属 submerged 培养物中抗结核羊毛甾烷三萜类化合物的研究延续中,对三株菌株进行了研究,分别是圆灵芝 BCC 22325、灵芝属 BCC 60695 和南方灵芝 BCC 22314。共分离出 14 种新的羊毛甾烷三萜类化合物以及 35 种已知化合物。评估了这些与菌丝体相关的灵芝羊毛甾烷类化合物对结核分枝杆菌 H37Ra 的抗结核活性。结合先前分离化合物的测定数据,提出了抗结核活性的构效关系。最重要的是,3β-和 15α-乙酰氧基被证明对抗分枝杆菌活性至关重要。最有效的化合物是(24E)-3β,15α-二乙酰氧基羊毛甾-7,9(11),24-三烯-26-酸(35)。

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