Flow Update for a Cossy Photocyclization.

A Cossy 5-exo-dig photocyclization of organohalides (X = Br, I) onto a C-C triple bond was studied using a flow photomicroreactor, which proceeded in a minute order of residence time. A deuterium labeling study supported the nonchain radical mechanism proposed by the Cossy group, in which a hydrogen source originates from a triethylamine cation radical. Scalable flow synthesis using a larger volume of flow reactor was also successful, providing 4 g of the product in high yield.

Chemical composition, antioxidant, antitumor, anticancer and cytotoxic effects of Psidium guajava leaf extracts.

Context Psidium guajava L. (Myrtaceae) leaves are used in traditional medicines for the treatment of cancer, inflammation and other ailments. Objective The current study explores scientific validation for this traditional medication. Materials and methods We used ferric-reducing antioxidant power (FRAP) and 2,2-diphenyl-1-picryl hydrazil (DPPH) assays to estimate antioxidant activity of P. guajava leaf extracts (methanol, hexane and chloroform). Antitumour and in vivo cytotoxic activities were determined using potato disc assay (PDA) and brine shrimp lethality assay, respectively. Three human carcinoma cell lines (KBM5, SCC4 and U266) were incubated with different doses (10-100 µg/mL) of extracts and the anticancer activity was estimated by MTT assay. NF-κB suppressing activity was determined using electrophoretic mobility shift assay (EMSA). Chemical composition of the three extracts was identified by GC-MS. Total phenolic and flavonoid contents were measured by colorimetric assays. Results and discussions The order of antioxidant activity of three extracts was methanol > chloroform > hexane. The IC50 values ranged from 22.73 to 51.65 µg/mL for KBM5; 22.82 to 70.25 µg/mL for SCC4 and 20.97 to 89.55 µg/mL for U266 cells. The hexane extract exhibited potent antitumour (IC50 value = 65.02 µg/mL) and cytotoxic (LC50 value = 32.18 µg/mL) activities. This extract also completely inhibited the TNF-α induced NF-κB activation in KBM5 cells. GC-MS results showed that pyrogallol, palmitic acid and vitamin E were the major components of methanol, chloroform and hexane extracts. We observed significant (p < 0.05) difference in total phenolic and flavonoid contents of different solvent extracts. Conclusion The present study demonstrates that P. guajava leaf extracts play a substantial role against cancer and down-modulate inflammatory nuclear factor kB.

Antioxidant, antimicrobial, antitumor, and cytotoxic activities of an important medicinal plant (Euphorbia royleana) from Pakistan.

The aim of present study was to evaluate antioxidant, antimicrobial, and antitumor activities of methanol, hexane, and aqueous extracts of fresh Euphorbia royleana. Total phenolic and flavonoid contents were estimated as gallic acid and querectin equivalents, respectively. Antioxidant activity was assessed by scavenging of free 2,2'- diphenyl-1-picrylhydrazyl radicals and reduction of ferric ions, and it was observed that inhibition values increase linearly with increase in concentration of extract. The results of ferric reducing antioxidant power assay showed that hexane extract has maximum ferric reducing power (12.70 ± 0.49 mg gallic acid equivalents/g of plant extract). Maximum phenolic (47.47 ± 0.71 µg gallic acid equivalents/mg of plant extract) and flavonoid (63.68 ± 0.43 µg querectin equivalents/mg of plant extract) contents were also found in the hexane extract. Furthermore, we examined antimicrobial activity of the three extracts (methanol, hexane, aqueous) against a panel of microorganisms (Escherichia coli, Bacillus subtillis, Pasteurella multocida, Aspergillus niger, and Fusarium solani) by disc-diffusion assay, and found the hexane extract to be the best antimicrobial agent. Hexane extract was also observed as to be most effective in a potato disc assay. As hexane extract showed potent activity in all the investigated assays, it was targeted for cytotoxic assessment. Maximum cytotoxicity (61.66%) by hexane extract was found at 800 µg/mL. It is concluded that investigated extracts have potential for isolation of antioxidant and antimicrobial compounds for the pharmaceutical industry.

New ceramides from Platytaenia multicaule.

Phytochemical investigation of Platytaenia multicaule resulted in the isolation of two new ceramides, N-triacontylpentadecanamide and 1,3,4-trihydroxy-2,dodecanoylamino-(24E)-unacotenene, along with two known compounds, beta-sitosterol and beta-sitosterol glycoside. The structure elucidation of the isolated compounds was based primarily on 1D and 2D NMR analyses, including COSY, NOESY, HMQC, and HMBC correlations.