title: Antioxidant value and antiproliferative efficacy of mitragynine and a silane reduced analogue.
abstract: BACKGROUND
  To investigate the antioxidant value and anticancer functions of mitragynine (MTG) and its silane-reduced analogues (SRM) in vitro.
  
  
  METHODS
  MTG and SRM was analyzed for their reducing power ability, ABTS radical inhibition and 1,1-diphenyl-2-picryl hydrazylfree radicals scavenging activities. Furthermore, the antiproliferation efficacy was evaluated using MTT assay on K 562 and HCT116 cancer cell lines versus NIH/3T3 and CCD18-Co normal cell lines respectively.
  
  
  RESULTS
  SRM and MTG demonstrate moderate antioxidant value with ABTS assay (Trolox equivalent antioxidant capacity (TEAC): 2.25±0.02 mmol trolox / mmol and 1.96±0.04 mmol trolox / mmol respectively) and DPPH (IC50=3.75±0.04 mg/mL and IC50=2.28±0.02 mg/mL respectively). Both MTG and SRM demonstrate equal potency (IC50=25.20±1.53 and IC50= 22.19±1.06 respectively) towards K 562 cell lines, comparable to control, betulinic acid (BA) (IC5024.40±1.26). Both compounds showed concentration-dependent cytototoxicity effects and exert profound antiproliferative efficacy at concentration > 100 μM towards HCT 116 and K 562 cancer cell lines, comparable to those of BA and 5-FU (5-Fluorouracil). Furthermore, both MTG and SRM exhibit high selectivity towards HCT 116 cell lines with selective indexes of 3.14 and 2.93 respectively compared to 5-FU (SI=0.60).
  
  
  CONCLUSIONS
  These findings revealed that the medicinal and nutitional values of mitragynine obtained from ketum leaves that growth in tropical forest of Southeast Asia and its analogues does not limited to analgesic properties but could be promising antioxidant and anticancer or chemopreventive compounds.
authors: Centre for Drug Research, Universiti Sains Malaysia, Penang, Malaysia E-mail : smahsufi@usm.my, gohteikbeng@yahoo.com.
authors: Teik Beng
authors: TB
authors: Goh
authors: R Y
authors: RY
authors: Koh
authors: Mohd Nizam
authors: MN
authors: Mordi
authors: Sharif Mahsuf
authors: SM
authors: Mansor
mesh_terms: D016475:3T3 Cells; D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000494:pharmacology; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology; D000975:Antioxidants / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D018890:Chemoprevention; D003110:Colonic Neoplasms / Q000188:drug therapy*; D005472:Fluorouracil / Q000494:pharmacology; D045325:HCT116 Cells; D006801:Humans; D051379:Mice; D018384:Oxidative Stress / Q000187:drug effects; D053978:Pentacyclic Triterpenes; D028321:Plant Preparations / Q000494:pharmacology; D046948:Secologanin Tryptamine Alkaloids / Q000494:pharmacology*; D012821:Silanes / Q000378:metabolism*; D014315:Triterpenes / Q000494:pharmacology; D000094062:Betulinic Acid
chemical_list: D000964:Antimetabolites, Antineoplastic; D000972:Antineoplastic Agents, Phytogenic; D000975:Antioxidants; D053978:Pentacyclic Triterpenes; D028321:Plant Preparations; D046948:Secologanin Tryptamine Alkaloids; D012821:Silanes; D014315:Triterpenes; C001801:mitragynine; D005472:Fluorouracil; D000094062:Betulinic Acid