title: Bioactive glycosides from the roots of Ilex asprella.
abstract: Context The roots of Ilex asprella (Hook. et Arn.) Champ. ex Benth. (Aquifoliaceae) are widely used in Chinese medicine to treat influenza, amygdalitis, pertussis, etc. Their mechanism of action is still unknown, which raises the need to identify new bioactive compounds in this plant. Objective In this study, we isolated a novel saponin containing sulphonic groups, namely, asprellcoside A (1) and a known phenolic glycoside compound (2) from the roots of Ilex asprella and evaluated their bioactivities. Materials and methods Molecular structures were elucidated by analysing their spectral and chemical properties. The viability of A549 cells was tested using a MTT assay. Ability of the compounds to inhibit viruses was determined using the neuraminidase activity assay. Their anti-inflammatory effects were tested using the IP-10 activity assay using various concentrations (compound 1: 0.6, 0.2, 0.6, 1.70, 5.00 and 15.00 μM; compound 2: 0.4, 1.2, 3.6, 11.0, 33.0 and 100 μM). Their inhibitory effect on platelet aggregation induced by adenosine diphosphate (ADP) in rabbit plasma was determined at 60 and 80 μM. Results Both compounds inhibit influenza virus strain A/PuertoRico/8/1934 (H1N1) strongly with EC50 values of 4.1 and 1.7 μM, respectively. Both compounds inhibit the secretion of IP-10 with EC50 values of 6.6 and 2.5 μM, respectively. Compound 1 alone inhibited platelet aggregation significantly, with the rate of suppression being 47 ± 8 and 38 ± 3%, at 60 and 80 μM, respectively. Conclusions The results suggest that both compounds may be valid therapeutics against influenza virus infection and that compound 1 may be a novel agent for treating thrombosis.
authors.affiliation: a Department of Chinese Medicine , Guangzhou University of Chinese Medicine , Guangzhou , China ;
authors.forename: Min-Hua
authors.initials: MH
authors.lastname: Peng
authors.affiliation: a Department of Chinese Medicine , Guangzhou University of Chinese Medicine , Guangzhou , China ;
authors.forename: Wei-Ping
authors.initials: WP
authors.lastname: Dai
authors.affiliation: a Department of Chinese Medicine , Guangzhou University of Chinese Medicine , Guangzhou , China ;
authors.forename: Si-Jun
authors.initials: SJ
authors.lastname: Liu
authors.affiliation: a Department of Chinese Medicine , Guangzhou University of Chinese Medicine , Guangzhou , China ;
authors.forename: Liang-Wen
authors.initials: LW
authors.lastname: Yu
authors.affiliation: a Department of Chinese Medicine , Guangzhou University of Chinese Medicine , Guangzhou , China ;
authors.forename: Yi-Na
authors.initials: YN
authors.lastname: Wu
authors.affiliation: b Wuhan Institute of Virology, Chinese Academy of Sciences , Wuhan , China ;
authors.forename: Rui
authors.initials: R
authors.lastname: Liu
authors.affiliation: b Wuhan Institute of Virology, Chinese Academy of Sciences , Wuhan , China ;
authors.forename: Xu-Lin
authors.initials: XL
authors.lastname: Chen
authors.affiliation: a Department of Chinese Medicine , Guangzhou University of Chinese Medicine , Guangzhou , China ;
authors.forename: Xiao-Ping
authors.initials: XP
authors.lastname: Lai
authors.affiliation: c The Second Affiliated Hospital of Guangzhou University of Traditional Chinese Medicine , Guangzhou , China.
authors.forename: Xiong
authors.initials: X
authors.lastname: Li
authors.affiliation: a Department of Chinese Medicine , Guangzhou University of Chinese Medicine , Guangzhou , China ;
authors.forename: Zhong-Xiang
authors.initials: ZX
authors.lastname: Zhao
authors.affiliation: a Department of Chinese Medicine , Guangzhou University of Chinese Medicine , Guangzhou , China ;
authors.forename: Geng
authors.initials: G
authors.lastname: Li
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000998:Antiviral Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D016207:Cytokines / Q000378:metabolism; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D006027:Glycosides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D030017:Ilex / Q000737:chemistry; D018836:Inflammation Mediators / Q000378:metabolism; D053118:Influenza A Virus, H1N1 Subtype / Q000187:drug effects / Q000201:enzymology; D061985:Madin Darby Canine Kidney Cells; D015394:Molecular Structure; D009439:Neuraminidase / Q000037:antagonists & inhibitors / Q000378:metabolism; D008517:Phytotherapy; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018517:Plant Roots; D010946:Plants, Medicinal; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D011817:Rabbits; D013329:Structure-Activity Relationship
chemical_list: D000893:Anti-Inflammatory Agents; D000998:Antiviral Agents; D016207:Cytokines; D006027:Glycosides; D018836:Inflammation Mediators; D010936:Plant Extracts; D010975:Platelet Aggregation Inhibitors; D009439:Neuraminidase
keywords: IP-10; neuraminidases; phenolic glycoside; platelet aggregation; triterpenoid saponin