title: Cytotoxic metabolites from the cultures of endophytic fungi from Panax ginseng.
abstract: Two strains of endophytic fungi, Penicillium melinii Yuan-25 and Penicillium janthinellum Yuan-27, with strong anti-Pyricularia oryzae activity, were obtained from the roots of Panax ginseng. Based on bioactivity-oriented isolation, a new benzaldehyde derivative, ginsenocin (1), together with six known compounds, methyl 2,4-dihydroxy-3,5,6-trimethylbenzoate (2), 3,4,5-trimethyl-1,2-benzenediol (3), penicillic acid (4), mannitol (5), ergosterol (6), and ergosterol peroxide (7), were separated from the EtOAc extract of Yuan-25 culture, while brefeldin A (8) was isolated as the major constituent from the EtOAc extract of Yuan-27 culture. The chemical structures were determined based on spectroscopic methods. All the isolated compounds 1-8 were evaluated for their cytotoxicity against six human cancer cell lines. Brefeldin A (8) was the most cytotoxic constituent against all the tested cell lines with IC50 values <0.12 μg/ml, while ginsenocin (1) and penicillic acid (4) also exhibited potent cytotoxicity with IC50 values ranging from 0.49 to 7.46 μg/ml. Our results suggest that endophytic fungi isolated from P. ginseng are a promising natural source of potential anticancer agents.
authors.affiliation: Department of Pharmacognosy, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai, 200433, People's Republic of China.
authors.forename: Cheng-Jian
authors.initials: CJ
authors.lastname: Zheng
authors.forename: Li-Li
authors.initials: LL
authors.lastname: Xu
authors.forename: Yuan-Yuan
authors.initials: YY
authors.lastname: Li
authors.forename: Ting
authors.initials: T
authors.lastname: Han
authors.forename: Qiao-Yan
authors.initials: QY
authors.lastname: Zhang
authors.forename: Qian-Liang
authors.initials: QL
authors.lastname: Ming
authors.forename: Khalid
authors.initials: K
authors.lastname: Rahman
authors.forename: Lu-Ping
authors.initials: LP
authors.lastname: Qin
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000378:metabolism* / Q000633:toxicity*; D045744:Cell Line, Tumor; D060026:Endophytes / Q000737:chemistry / Q000235:genetics / Q000302:isolation & purification / Q000378:metabolism*; D006801:Humans; D008969:Molecular Sequence Data; D015394:Molecular Structure; D005894:Panax / Q000382:microbiology*; D010407:Penicillium / Q000737:chemistry / Q000235:genetics / Q000302:isolation & purification / Q000378:metabolism*; D010802:Phylogeny; D018517:Plant Roots / Q000382:microbiology
chemical_list: D000970:Antineoplastic Agents