Autor: |
Honmore VS; a Department of Chemistry, Post Graduate and Research Centre , MES Abasaheb Garware College , Pune , India., Rojatkar SR; b R & D Centre in Pharmaceutical Sciences and Applied Chemistry, Poona College of Pharmacy , Bharati Vidyapeeth Deemed University , Pune , India., Nawale LU; c Combichem-Bioresource Centre, OCD , National Chemical Laboratory , Pune , India., Arkile MA; c Combichem-Bioresource Centre, OCD , National Chemical Laboratory , Pune , India., Khedkar VM; c Combichem-Bioresource Centre, OCD , National Chemical Laboratory , Pune , India., Natu AD; a Department of Chemistry, Post Graduate and Research Centre , MES Abasaheb Garware College , Pune , India., Sarkar D; c Combichem-Bioresource Centre, OCD , National Chemical Laboratory , Pune , India. |
Abstrakt: |
Phytochemical investigation of methanol extract of the rhizomes of Alpinia officinarum Hance afforded four known diarylheptanoids 1,7-diphenylhept-4-en-3-one (1), 5-hydroxy-1,7-diphenyl-3-heptanone (2), 5-hydroxy-7-(4″-hydroxy-3″-methoxyphenyl)-1-phenyl-3-heptanone (3), and 7-(4″-hydroxy-3″-methoxyphenyl)-1-phenyl heptan-3-one (4).The acetate derivative of (4), 7-(4″-actetate-3″-methoxy phenyl)-1-phenyl heptan-3-one (5), was prepared. These diarylheptanoids exhibited promising in vitro and ex vivo antitubercular activity for the first time against dormant Mycobacterium tuberculosis H37Ra with the IC 50 values between 0.34-47.69 and 0.13-22.91 μM, respectively. All compounds showed comparable activity against Mycobacterium bovis BCG (dormant phage) and did not show any activity against two gram + ve and two gram -ve bacterial strains. These compounds were also weakly cytotoxic up to 300 μM against three human cancer cell lines THP-1, Panc-1 and A549. |