title: Apoptotic effects of diosgeninlactoside on oral squamous carcinoma cells in vitro and in vivo.
abstract: Diosgenyl saponins possess a variety of biological functions. Herein, we demonstrate a new type of diosgenyl saponin derivatives that inhibit cellular proliferation of oral squamous cell carcinoma (OSCC) cell lines. Thereafter, we analyzed these cells' expression of apoptosis-related proteins. Crucial proteins that participate in apoptosis regulation including caspases 8, 9, and 3, and cleaved Bid were activated and upregulated accompanied by increased concentrations of diosgenyl saponins. Meanwhile, Bcl-2 was downregulated and mitochondrial membrane potential decreased. In our mice model of OSCC, compound 1 showed potent inhibition of solid tumor growth and salient antitumor activity. Diosgenyl β-D-galactopyranosyl-(1→4)-β-D-glucopyranoside might induce OSCC cell line apoptosis through extrinsic and intrinsic pathways, and might provide a mechanistic background for the development of this new type of diosgenylsaponin derivatives into anti-oral cancer agents against OSCC.
authors.affiliation: State Key Laboratory of Oral Diseases, West China Hospital of Stomatology, Sichuan University.
authors.forename: Xu
authors.initials: X
authors.lastname: Wang
authors.forename: Chongkui
authors.initials: C
authors.lastname: Sun
authors.forename: Shiliang
authors.initials: S
authors.lastname: He
authors.forename: Xiurong
authors.initials: X
authors.lastname: Guo
authors.forename: Hao
authors.initials: H
authors.lastname: Xu
authors.forename: Xin
authors.initials: X
authors.lastname: Zeng
authors.forename: Lu
authors.initials: L
authors.lastname: Jiang
authors.forename: Yu
authors.initials: Y
authors.lastname: Zhou
authors.forename: Yunfeng
authors.initials: Y
authors.lastname: Lin
authors.forename: Ling
authors.initials: L
authors.lastname: Ye
authors.forename: Ning
authors.initials: N
authors.lastname: Ji
authors.forename: Jing
authors.initials: J
authors.lastname: Li
authors.forename: Qianming
authors.initials: Q
authors.lastname: Chen
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D017209:Apoptosis / Q000187:drug effects; D051023:BH3 Interacting Domain Death Agonist Protein / Q000378:metabolism; D002294:Carcinoma, Squamous Cell / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D020169:Caspases / Q000378:metabolism; D002460:Cell Line; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004144:Diosgenin / Q000031:analogs & derivatives* / Q000494:pharmacology* / Q000627:therapeutic use; D005260:Female; D006027:Glycosides / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects; D008807:Mice, Inbred BALB C; D009062:Mouth Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000378:metabolism; D047368:Tumor Burden / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D051023:BH3 Interacting Domain Death Agonist Protein; C494814:BID protein, human; D006027:Glycosides; D019253:Proto-Oncogene Proteins c-bcl-2; C008245:lactosides; D020169:Caspases; D004144:Diosgenin