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In the continuous search for new antiinflammatory agents from natural products, dichloromethane (DCM), ethyl acetate (EtOAc) and methanol (MeOH) extracts of Ipomea fistulosa leaves were evaluated for inhibition of production of nitric oxide (NO), interleukin 1beta (IL-1β) and tumor necrosis factor alpha (TNF-α) in lipopolysaccharide (LPS) stimulated J774A.1 cells. Among the tested extracts, the ethyl acetate (EtOAc) extract was found to be most active and activity based fractionation of this extract by column chromatography led to the identification of seven compounds for the first time from this plant. Furthermore, 3,4-dimethoxy cinnamic acid (1) exhibited two folds more potent inhibition of LPS-induced NO production (IC50 = 10.7 μg/mL) as compared with the standard, L-NAME (IC50 = 19.8 μg/mL). The present study supports the use of Ipomea fistulosa leaves for the treatment of inflammation.

The leaves of Aegle marmelos are reported to contain multi-bioactive classes of compounds including coumarins, furanocoumarins and alkaloids. HPLC analysis of the crude extract was challenging due to low concentrations of the compounds in the leaves. Five compounds visible in the HPLC chromatogram were separated and identified by HPLC and further elaborated for quantification as marker compounds of A. marmelos leaves using a C18 column with detection at 275 nm. A gradient mobile phase consisting of acetonitrile and water was used. The developed HPLC method showed good linearity (r2 > 0.994), high precision (RSD<5%), and good recovery (99.27-99.98%) of the compounds. The lowest detection limit was 5 ng and the method was found to be robust. All the validation parameters were within the permissible limits. Therefore, the developed method is accurate and reliable for the quality control of A. marmelos. This is the first report of extensive quantitative HPLC analysis of marker compounds in A. marmelos leaves and method validation.

The anti-inflammatory and cytotoxic activity of thirty-six extracts of nine Indian medicinal plants were determined by measuring the inhibition of production of nitric oxide (NO), interleukin 1beta (IL-1beta) and tumor necrosis factor alpha (TNF-alpha) in lipopolysaccharide (LPS) stimulated RAW 264.7 cells. Their cytotoxic activity against macrophages was determined by MTT assay. The ethyl acetate (EtOAc) extract of Cassia occidentalis L. (roots) (IC50 = 21.3 to 43.1 microg/mL) and Mimosa pudica (whole plant) (1C50= 31.7 to 47.2 microg/mL) and the dichloromethane (DCM) extract of Leucas cephalotes (whole plant) (IC50 = 46.8 to 49.3 microg/mL) exhibited significant anti-inflammatory activity by in vitro inhibition of the production of TNF-alpha, IL-1beta and NO in LPS stimulated RAW 264.7 cells. Furthermore, the five compounds isolated from the ethyl acetate extract of Cassia occidentalis roots were found to suppress LPS-induced IL-1beta, TNF-alpha and NO production in a concentration-dependent manner in these cells at 1C50 values ranging from 22.5 to 97.4 microM. Emodin and chrysophanol were also found active in inhibiting pro-inflammatory cytokines in vivo. These findings justify an ethnopharmacological use of C occidentalis roots as an effective herbal remedy for the treatment and prevention of inflammation and associated ailments.

In continuation towards the discovery of potential antiobesity lead(s) from natural products, we have screened n-hexane, dichloromethane (DCM), ethyl acetate (EtOAc) and methanol (MeOH) extracts of 33 Indian medicinal plants (200 extracts) for in vitro pancreatic lipase inhibitory activity. Of the screened extracts, the EtOAc extract of Cassia siamea roots showed 74.3 +/- 1.4% enzyme inhibition at 250 microg/mL concentration. Bioassay guided fractionation of the active extract afforded 6 known compounds viz. chrysophanol (1), physcion (2), emodin (3), cassiamin A (4), friedelin (5) and cycloart-25-en-3beta,24-diol (6). These compounds were further evaluated for pancreatic lipase inhibitory activity. Cassiamin A (4), a bianthraquinone, was found to be most active with an IC50 value of 41.8 +/- 1.2 microM and compounds 2 and 5 were found to be moderate enzyme inhibitors. Results indicate the antiobesity potential of C. siamea through pancreatic lipase inhibition.

Jirakadyarishta, an Ayurvedic formulation prepared by the fermentation of a decoction of Cuminum cyminum (seeds) is traditionally used for intestinal disorders. RP-HPLC analysis of the decoction and the final processed formulation revealed that apigenin-7-O-[galacturonide (1 --> 4)-O-glucoside] and luteolin-4'-O-glucoside-7-O-galacturonide) were the two major constituents of the decoction of C. cyminum. Selective hydrolysis of 7-O-glucosides of luteolin and apigenin during fermentation resulted in an increase in the amount of luteolin and apigenin. The 4'-O-glucoside-7-O-galacturonide of luteolin and galacturonide derivative of apigenin were not hydrolyzed during fermentation. Monomeric phenolics, together with 5-hydroxymethyl furfural (5-HMF), were also introduced into the formulation through the jaggery and other plant materials during fermentation. This communication highlights the importance of the ancient processing methods used in Ayurveda.

Abhayarishta is an Ayurvedic formulation prepared traditionally by the fermentation of the decoction of Terminalia chebula (pericarp), Vitis vinifera (fruits), Embelia ribes (fruits) and Madhuca indica (flowers). In the present communication, chemical changes occurring during fermentation in Abhayarishta have been studied for the purpose of its standardization. An HPLC-DAD method for quantitative estimation of selected marker constituents in the formulation has been developed and validated. A comparison of decoction and final processed formulation revealed that major polyphenolics (chebulagic and chebulinic acid) of T. chebula were hydrolyzed to their respective monomers and, consequently, there was an increase in the amount of chebulic acid, gallic acid, ellagic acid and ethyl gallate after fermentation. 5-Hydroxymethyl furfural (5-HMF) was also found in the formulation. Thus, emphasis is laid upon consideration of processing methods of formulation which has been lacking in the standardization of most of Ayurvedic formulations.

Various extracts of the aerial parts of Coleus forskohlii (Labiatae) were prepared and evaluated at their non cytotoxic concentration against HIV-1 NL4-3. Chloroform, ethyl acetate and n-butanol extracts showed 45.6, 66.5 and 37.7% inhibition of HIV, respectively in CEM-GFP cells infected with HIV-1(NL4-3) at 5 microg/mL. Four diterpenes, 1-deoxyforskolin, 1,9-dideoxyforskolin, forskolin and isoforskolin were isolated from the chloroform extract and tested against the virus. Six semi-synthetic derivatives of forskolin have been prepared to study SAR. 1-Deoxyforskolin and forskolin were found to be active against HIV(NL4-3). This is first report of anti HIV activity of this plant and its isolated constituents.

In the continuing search for newer pancreatic lipase inhibitors from plants, a total of 63 extracts from 21 different plants were screened to study their pancreatic lipase (PL) inhibitory activity in vitro. All three extracts (DCM, EtOAc and MeOH) of Murraya koenigii (L.) Spreng leaves (Rutaceae) exhibited antilipase activity greater than 80%. Further, bioactivity guided fractionation of the EtOAc extract led to the isolation of four alkaloids, namely mahanimbin, koenimbin, koenigicine and clausazoline-K, with IC50 values of 17.9 microM, 168.6 microM, 428.6 microM and <500 microM, respectively. This study reports for the first time the PL inhibitory potential of carbazole alkaloids from plants.