title: Daphnane-type diterpene esters with cytotoxic and anti-HIV-1 activities from Daphne acutiloba Rehd.
abstract: Seven previously unreported daphnane-type diterpene esters named acutilobins A-G, together with 12 known ones, were isolated from EtOAc extract of Daphne acutiloba Rehd. Their structures were elucidated based on the spectroscopic data. The cytotoxic and anti-HIV-1 activities of these daphnane-type diterpene esters were evaluated through bioassays. Fourteen of these isolates exhibited definite cytotoxic activities against the five human tumor cell lines HL-60, SMMC-7721, A-549, MCF-7, and SW480. Additionally, anti-HIV-1 activities were observed in 13 daphnane-type diterpene esters, among which acutilobins A-G exhibited significant anti-HIV-1 activities with EC₅₀ below 1.5 nM and SI over 10,000. Particularly, genkwanineVIII showed the strongest activity with EC₅₀ 0.17 nM and SI 187,010.
authors.affiliation: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, People's Republic of China.
authors.forename: Sheng Zhuo
authors.initials: SZ
authors.lastname: Huang
authors.forename: Xing Jie
authors.initials: XJ
authors.lastname: Zhang
authors.forename: Xing Yao
authors.initials: XY
authors.lastname: Li
authors.forename: Ling Mei
authors.initials: LM
authors.lastname: Kong
authors.forename: He Zhong
authors.initials: HZ
authors.lastname: Jiang
authors.forename: Qing Yun
authors.initials: QY
authors.lastname: Ma
authors.forename: Yu Qing
authors.initials: YQ
authors.lastname: Liu
authors.forename: Jiang Miao
authors.initials: JM
authors.lastname: Hu
authors.forename: Yong Tang
authors.initials: YT
authors.lastname: Zheng
authors.forename: Yan
authors.initials: Y
authors.lastname: Li
authors.forename: Jun
authors.initials: J
authors.lastname: Zhou
authors.forename: You Xing
authors.initials: YX
authors.lastname: Zhao
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D032364:Daphne / Q000737:chemistry*; D004224:Diterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D004952:Esters / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects*; D018922:HL-60 Cells; D006801:Humans; D008968:Molecular Conformation; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D000970:Antineoplastic Agents; D004224:Diterpenes; D004952:Esters; D010936:Plant Extracts; C011309:mezerein