Wu Ling-Shang, Jia Min, Chen Ling, Zhu Bo, Dong Hong-Xiu, Si Jin-Ping, Peng Wei, Han Ting
Nurturing Station for the State Key Laboratory of Subtropical Silviculture, Zhejiang A & F University, Lin'an 311300, China.
Department of Pharmacognosy, School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
Molecules. 2015 Dec 22;21(1):E14. doi: 10.3390/molecules21010014.
Two novel cytotoxic and antifungal constituents, (4S,6S)-6-[(1S,2R)-1, 2-dihydroxybutyl]-4-hydroxy-4-methoxytetrahydro-2H-pyran-2-one (1), (6S,2E)-6-hydroxy-3-methoxy-5-oxodec-2-enoic acid (2), together with three known compounds, LL-P880γ (3), LL-P880α (4), and Ergosta-5,7,22-trien-3b-ol (5) were isolated from the metabolites of endophytic fungi from Dendrobium officinale. The chemical structures were determined based on spectroscopic methods. All the isolated compounds 1-5 were evaluated by cytotoxicity and antifungal effects. Our present results indicated that compounds 1-4 showed notable anti-fungal activities (minimal inhibitory concentration (MIC) ≤ 50 μg/mL) for all the tested pathogens including Candida albicans, Cryptococcus neoformans, Trichophyton rubrum, Aspergillus fumigatus. In addition, compounds 1-4 possessed notable cytotoxcities against human cancer cell lines of HL-60 cells with the IC50 values of below 100 μM. Besides, compounds 1, 2, 4 and 5 showed strong cytotoxities on the LOVO cell line with the IC50 values were lower than 100 μM. In conclusion, our study suggested that endophytic fungi of D. officinale are great potential resources to discover novel agents for preventing or treating pathogens and tumors.
从铁皮石斛内生真菌的代谢产物中分离出两种新型细胞毒性和抗真菌成分,即(4S,6S)-6-[(1S,2R)-1,2-二羟基丁基]-4-羟基-4-甲氧基四氢-2H-吡喃-2-酮(1)、(6S,2E)-6-羟基-3-甲氧基-5-氧代癸-2-烯酸(2),以及三种已知化合物LL-P880γ(3)、LL-P880α(4)和麦角甾-5,7,22-三烯-3β-醇(5)。通过光谱方法确定了化学结构。对所有分离得到的化合物1-5进行了细胞毒性和抗真菌作用评估。我们目前的结果表明,化合物1-4对包括白色念珠菌、新型隐球菌、红色毛癣菌、烟曲霉在内的所有测试病原体均表现出显著的抗真菌活性(最低抑菌浓度(MIC)≤50μg/mL)。此外,化合物1-4对HL-60人癌细胞系具有显著的细胞毒性,IC50值低于100μM。此外,化合物1、2、4和5对LOVO细胞系表现出较强的细胞毒性,IC50值低于100μM。总之,我们的研究表明,铁皮石斛内生真菌是发现预防或治疗病原体和肿瘤新型药物的巨大潜在资源。