01732nas a2200205   4500008004100000245011600041210006900157260000800226300001400234490000700248520098800255100002401243700002501267700002301292700002401315700002301339700001901362700001901381856012601400       2016                        eng d00aIn vitro and ex vivo antitubercular activity of diarylheptanoids from the rhizomes of alpinia officinarum hance0 aIn vitro and ex vivo antitubercular activity of diarylheptanoids  cMAR  a2825-28300 v303 a<p>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 IC50 values between 0.3447.69 and 0.1322.91 mu M, 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 mu M against three human cancer cell lines THP-1, Panc-1 and A549.</p>1 aHonmore, Varsha, S.1 aRojatkar, Supada, R.1 aNawale, Laxman, U.1 aArkile, Manisha, A.1 aKhedkar, Vijay, M.1 aNatu, Arun, D.1 aSarkar, Dhiman  uhttp://library.ncl.res.in/content/vitro-and-ex-vivo-antitubercular-activity-diarylheptanoids-rhizomes-alpinia-officinarum03544nas a2200313   4500008004100000022001400041245013800055210006900193260007300262300000900335490000700344520238000351653007102731653002402802653002202826653001602848653002102864653001302885100002402898700002302922700002102945700002302966700001902989700002703008700002203035700002503057700001903082856012903101       2016                        eng d  a1567-576900aIsolates of alpinia officinarum hance as COX-2 inhibitors: evidence from anti-inflammatory, antioxidant and molecular docking studies0 aIsolates of alpinia officinarum hance as COX2 inhibitors evidenc  aPO BOX 211, 1000 AE AMSTERDAM, NETHERLANDSbELSEVIER SCIENCE BVcAPR  a8-170 v333 a<p>Background: Inflammation triggered by oxidative stress can cause various ailments, such as cancer, rheumatoid arthritis, asthma, diabetes etc. In the last few years, there has been a renewed interest in studying the antioxidant and anti-inflammatory action of plant constituents such as flavonoids and diarylheptanoids. Aim: To evaluate the antioxidant, anti-inflammatory activity and the total phenolic content of isolated compounds from Alpinia officinarum rhizomes. Furthermore, molecular docking was performed to study the binding mode of these compounds into the active site of cyclooxygenase-2 (COX -2). Methods: A. officinarum rhizomes were extracted by maceration, using methanol. This extract was further fractionated by partitioning with hexane, chloroform and ethyl acetate and these fractions on further purification resulted in isolation of five pure compounds. Characterization was carried out by using H-1 NMR, C-13 NMR and MS. They were further evaluated for antioxidant and anti-inflammatory activity using carrageenan-induced paw edema model in rats. Molecular docking study was performed using Glide module integrated in Schrodinger molecular modeling software. Results: The compounds were identified as 1,7-diphenylhept-4-en-3-one (1), 5-hydroxy-1,7-diphenyl-3-heptanone (2), 3,5,7-trihydroxyflavone (Galangin, 3), 3,5,7-trihydroxy-4'-methoxyflavone (Kaempferide, 4) and 5-hydroxy-7-(4 `'-hydroxy-3 `'-methoxyphenyl)-1-phenyl-3-heptanone (5). The compound-3 and compound-5 (10 mg/kg) showed significant (p &lt; 0.001) antioxidant and anti-inflammatory potential. Moreover, total phenolic content was detected as 72.96 mg and 51.18 mg gallic acid equivalent respectively. All the five isolates were found to be good binders with COX-2 (average docking score -9.03). Conclusions: Galangin and 5-hydroxy-7-(4 `'-hydroxy-3 `'-methoxyphenyl)-1-phenyl-3-heptanone exhibited anti-inflammatory and in-vitro antioxidant activity which may be due to presence of phenolic content in it. The molecular docking study revealed that these compounds have affinity towards COX-2 active site which can further be explored as selective COX-2 inhibitors. The results obtained in this work justify the use of A. officinarum in the treatment of inflammatory disorders like rheumatoid arthritis and inflammatory bowel diseases. (C) 2016 Elsevier B.V. All rights reserved.</p>10a5-Hydroxy-7-(4 `'-hydroxy-3 `'-methoxyphenyl)-1-phenyl-3-heptanone10aAlpinia officinarum10aAnti-inflammatory10aAntioxidant10aCOX-2 inhibitors10aGalangin1 aHonmore, Varsha, S.1 aKandhare, Amit, D.1 aKadam, Parag, P.1 aKhedkar, Vijay, M.1 aSarkar, Dhiman1 aBodhankar, Subhash, L.1 aZanwar, Anand, A.1 aRojatkar, Supada, R.1 aNatu, Arun, D.  uhttp://library.ncl.res.in/content/isolates-alpinia-officinarum-hance-cox-2-inhibitors-evidence-anti-inflammatory-antioxidant