Methanolic fraction of Cassia fistula L. bark exhibits potential to combat oxidative stress and possess antiproliferative activity.

Cassia fistula L. is well known for its traditional medicinal properties as an anti-inflammatory, hepatoprotective, antifungal, antibacterial, antimutagenic, and wound healing agent. The aim of the present study was to determine antioxidant, genoprotective, and cytotoxic potential of different fractions of C. fistula bark including hexane (CaMH), chloroform (CaMC), ethyl acetate (CaME), and methanol (CaMM). Among all the fractions studied, CaMM exhibited maximal radical scavenging activity in antioxidant DPPH assay, Superoxide anion radical scavenging assay and nitric oxide radical scavenging assay displayed an IC50 value of 18.95, 29.41, and 13.38 µg/ml, respectively. CaMM fraction possessed the highest phenolic (130.37 mg gallic acid equivalent/g dry weight of extract) and flavonoid (36.96 mg rutin equivalent/g dry weight of fraction) content. Data demonstrated significant positive correlation between polyphenol levels and radical scavenging activity. Single cell gel electrophoresis (Comet assay) exhibited genoprotective potential of C. fistula bark fractions against DNA damage induced by hydrogen peroxide (H2O2) in human lymphocytes. CaMM fraction displayed highest protective ability against H2O2 induced-toxicity as evidenced by significant decrease in % tail DNA content from 30 to 7% at highest concentration (200 µg/ml). CaMM was found to be rich in catechin, gallic acid, chlorogenic acid, and kaempferol. The phenolic content and antioxidant ability of the fractions was markedly negatively correlated with H2O2- induced DNA damage in human lymphocytes. Cytotoxic potential was evaluated against dermal epidermoid carcinoma (A431), pancreatic (MIA PaCa-2) and brain glioblastoma (LN-18) cancer cell lines using MTT assay. Results showed that C. fistula bark fractions possessed highest toxicity against the skin carcinoma cells. CaMM fraction reduced over 50% cell growth at the concentration of 76.72 µg/ml in A431 cells. These findings suggest that fractions of C. fistula bark exhibit potential to be considered as therapeutic agents in various carcinomas.

Synthesis and Cytotoxicity on Human Lung Cancer Cell Lines of 2-Arylidene and Related Analogues of Malabaricol.

Malabaricol is a unique plant natural product, 3-keto tricarbocyclic triterpenoid, isolated from Ailanthus malabarica. Malabaricol underwent reaction with aromatic aldehydes under alkaline conditions to form 2-arylidene analogs. Indoles and pyrazine ring system fused to the 2,3-position of malabaricol were synthesized. In this ring system of tricarbocyclic triterpenoid, the conformation is such that there is no steric hindrance due to C4 and C10 axial methyl groups and other skeletons. Malabaricol and its synthetic analogues show cytotoxic activity toward lung cancer, which was compared to that of standard doxorubicin.

Palladium(ii)-catalyzed direct O-alkenylation of 2-arylquinazolinones with N-tosylhydrazones: an efficient route to O-alkenylquinazolines.

An efficient Pd(ii)-catalyzed direct O-alkenylation of 2-arylquinazolinones with simple ketone-derived N-tosylhydrazones is reported. In this reaction, O-alkenylquinazolines were obtained in good yields, with excellent functional group tolerance. Pd-carbene migratory insertion is proposed as the key step in the reaction mechanism.

Synthesis of novel chromeno-annulated cis-fused pyrano[3,4-c]benzopyran and naphtho pyran derivatives via domino aldol-type/hetero Diels-Alder reaction and their cytotoxicity evaluation.

New chromeno-annulated cis-fused pyrano[3,4-c]benzopyran and naphtho pyran derivatives have been synthesized by domino aldol-type reaction/hetero Diels-Alder reaction generated from o-quinone methide in situ from 7-O-prenyl derivatives of 8-formyl-2,3-disubstituted chromenones with resorcinols/naphthols in the presence of 20 mol% ethylenediamine diacetate (EDDA), triethylamine (2 mL) as co-catalyst in CH3CN under reflux conditions in good yields. The structures were established based on spectroscopic data, and further confirmed by X-ray diffraction analysis. The results showed that compounds 4h and 4j exhibited very potent cytotoxicity against human cervical cancer cell line (HeLa). Compound 4h displayed good inhibitory activity against both breast cancer cell lines, MDA-MB-231 and MCF-7. Further, the compound 4i exhibited good cytotoxicity against only MDA-MB-231, and compound 4j showed promising activity against human lung cancer cell line, A549 with IC50 value of 2.53±0.07 µM, which was comparable to the standard doxorubicin (IC50=1.21±0.1 µM).

Standardization of the Unani drug - Myristica fragrans Houtt. (Javetri) - with modern analytical techniques.

Today, there is a tremendous demand of herbal medicine in the global market and the scarcity of data regarding the parameters and methods employed for assessing the quality of medicines. Aril (Mace) of Myristica fragrans Houtt., known as "Javetri," belonging to the Myristicaceae family, plays a foremost role in the Unani system of medicine. It contains Myristicin, an active principle of drug isolated by column chromatography, and its structure was established by spectroscopic methods. Different solvent drug extracts posses pharmacological properties like hypocholesteremic, anti-inflammatory, anti-diarrheal, chemopreventive action, etc. and hence there is a great need to determine the amount of myristicin present in the different extracts. The proposed method employed the High Performance Thin Layer Chromatography (HPTLC) DESAGA Sarstedt Gruppe and pre-coated aluminum sheets of silica gel developed with 100% chloroform to quantitatively determine the myristicin concentrations present in various extracts that are responsible for their different pharmacological actions. An attempt was made through instrumental analysis for quantitative estimations that are widely accepted for the quality assessment of herbal drugs such as TLC and HPTLC studies, etc. Physicochemical parameters, microbial load, aflatoxin and heavy metals and fluorescence studies were also carried out to lay down the standard for genuine drug. HPTLC studies were carried out in petroleum ether, chloroform, ethyl acetate, ethanol and methanol extracts and detected at 254 nm. Estimated high amount of myristicin in the petroleum ether extract w.r.t. the other extracts was confirmed by spectroscopy. The present paper describes the isolation, characterization and quantification of myristicin along with chemical standardization in order to develop standard parameters for the genuine drug.