title: Natural phosphodiesterase-4 inhibitors from the leaf skin of Aloe barbadensis Miller.
abstract: The ethanolic extract of Aloe barbadensis Miller leaf skin showed inhibitory activity against phosphodiesterase-4D (PDE4D), which is a therapeutic target of inflammatory disease. Subsequent bioassay-guided fractionation led to the isolation of two new anthrones, 6'-O-acetyl-aloin B (9) and 6'-O-acetyl-aloin A (11), one new chromone, aloeresin K (8), together with thirteen known compounds. Their chemical structures were elucidated by spectroscopic methods including UV, IR, 1D and 2D NMR, and HRMS. All of the isolates were screened for their inhibitory activity against PDE4D using tritium-labeled adenosine 3',5'-cyclic monophosphate ((3)H-cAMP) as substrate. Compounds 13 and 14 were identified as PDE4D inhibitors, with their IC50 values of 9.25 and 4.42 μM, respectively. These achievements can provide evidences for the use of A. barbadensis leaf skin as functional feed additives for anti-inflammatory purpose.
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China.
authors.forename: Jia-Sheng
authors.initials: JS
authors.lastname: Zhong
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China.
authors.forename: Yi-You
authors.initials: YY
authors.lastname: Huang
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China.
authors.forename: Tian-Hua
authors.initials: TH
authors.lastname: Zhang
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China.
authors.forename: Yu-Peng
authors.initials: YP
authors.lastname: Liu
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China.
authors.forename: Wen-Jing
authors.initials: WJ
authors.lastname: Ding
authors.affiliation: Analysis and Testing Center, Chinese Academy of Tropical Agricultural Sciences, Haikou 571101, PR China; Hainan Provincial Key Laboratory of Quality and Safety for Tropical Fruits and Vegetables, Haikou 571101, PR China.
authors.forename: Xiao-Fang
authors.initials: XF
authors.lastname: Wu
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China.
authors.forename: Zhi-Yong
authors.initials: ZY
authors.lastname: Xie
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China. Electronic address: luohb77@mail.sysu.edu.cn.
authors.forename: Hai-Bin
authors.initials: HB
authors.lastname: Luo
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China. Electronic address: jinzhiwan2004@aliyun.com.
authors.forename: Jin-Zhi
authors.initials: JZ
authors.lastname: Wan
mesh_terms: D000504:Aloe / Q000737:chemistry*; D000818:Animals; D000873:Anthracenes / Q000737:chemistry / Q000302:isolation & purification; D002460:Cell Line; D002867:Chromones / Q000737:chemistry / Q000302:isolation & purification; D020128:Inhibitory Concentration 50; D051379:Mice; D015394:Molecular Structure; D058988:Phosphodiesterase 4 Inhibitors / Q000737:chemistry* / Q000302:isolation & purification; D010936:Plant Extracts / Q000737:chemistry*; D018515:Plant Leaves / Q000737:chemistry*
chemical_list: D000873:Anthracenes; D002867:Chromones; D058988:Phosphodiesterase 4 Inhibitors; D010936:Plant Extracts
keywords: Aloe barbadensis Miller; Aloe-emodin (PubChem CID: 10207); Aloin A (PubChem CID: 5458893); Aloin B (PubChem CID: 5458894); Aloinoside A (PubChem CID: 46173997); Aloinoside B (PubChem CID: 46173998); Anthrone; Chromone; Cytotoxicity; Isoaloeresin D (PubChem CID: 76332505); PDE4