title: Bioactive metabolites from an endophytic Cryptosporiopsis sp. inhabiting Clidemia hirta.
abstract: An endophytic Cryptosporiopsis sp. was isolated from Clidemia hirta and analyzed for its secondary metabolites that lead to the isolation of three bioactive molecules. The compounds were purified from the culture broth of the fungus and their structures were determined by spectroscopic methods as (R)-5-hydroxy-2-methylchroman-4-one (1), 1-(2,6-dihydroxyphenyl)pentan-1-one (2) and (Z)-1-(2-(2-butyryl-3-hydroxyphenoxy)-6-hydroxyphenyl)-3-hydroxybut-2-en-1-one (3). Compound 1 exhibited significant cytotoxic activity against the human leukemia cell line, HL-60 with an IC50 of 4 μg/ml. This compound induced G2 arrest of the HL-60 cell cycle significantly. In addition, out of these compounds, 2 and 3 were active against several bacterial pathogens. Compound 2 was active against Bacillus cereus, Escherichia coli and Staphylococcus aureus with IC50 values varying from 18 to 30 μg/ml, and compound 3 displayed activity against Pseudomonas fluorescens with an IC50 value of 6 μg/ml. Compounds 2 and 3 are novel whereas compound 1 was reported earlier but the stereochemistry of its C-2 methyl is established for the first time.
authors.affiliation: Natural Product Division, CSIR-Indian Institute of Integrative Medicine, Jammu 180 001, India.
authors.forename: Mahesh K
authors.initials: MK
authors.lastname: Zilla
authors.forename: Masroor
authors.initials: M
authors.lastname: Qadri
authors.forename: Anup S
authors.initials: AS
authors.lastname: Pathania
authors.forename: Gary A
authors.initials: GA
authors.lastname: Strobel
authors.forename: Yedukondalu
authors.initials: Y
authors.lastname: Nalli
authors.forename: Sunil
authors.initials: S
authors.lastname: Kumar
authors.forename: Santosh K
authors.initials: SK
authors.lastname: Guru
authors.forename: Shashi
authors.initials: S
authors.lastname: Bhushan
authors.forename: Sanjay K
authors.initials: SK
authors.lastname: Singh
authors.forename: Ram A
authors.initials: RA
authors.lastname: Vishwakarma
authors.forename: Syed
authors.initials: S
authors.lastname: Riyaz-Ul-Hassan
authors.forename: Asif
authors.initials: A
authors.lastname: Ali
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use; D001203:Ascomycota / Q000737:chemistry*; D001407:Bacillus / Q000187:drug effects; D001419:Bacteria / Q000187:drug effects*; D001688:Biological Products / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D002090:Butyrophenones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D002867:Chromones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D060026:Endophytes / Q000737:chemistry; D004926:Escherichia coli / Q000187:drug effects; D018922:HL-60 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D007938:Leukemia / Q000188:drug therapy*; D035322:Melastomataceae / Q000382:microbiology*; D015394:Molecular Structure; D010422:Pentanones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D011551:Pseudomonas fluorescens / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects
chemical_list: C588384:1-(2,6-dihydroxyphenyl)pentan-1-one; C588385:1-(2-(2-butyryl-3-hydroxyphenoxy)-6-hydroxyphenyl)-3-hydroxybut-2-en-1-one; C588383:5-hydroxy-2-methylchroman-4-one; D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D001688:Biological Products; D002090:Butyrophenones; D002867:Chromones; D010422:Pentanones
keywords: Antimicrobial activity; Clidemia hirta; Cryptosporiopsis; Cytotoxicity; Endophytes; Natural products