Humboldtia unijuga Bedd., endemic to Agasthyamala in Western Ghats in India, is traditionally used by local Kani tribes for chicken pox, head ache and snake bite. This study reports the isolation of erythrodiol-3-acetate (HU-1) and 2,4-di-tert-butylphenol (HU-2) from H. unijuga roots and their anti-inflammatory and anticancer activities in macrophage, skin and breast cancer cell lines. Effects of HU-1 and HU-2 treatments (50, 100 µg/mL) on gene expression profiles of pro-inflammatory cytokines TNFα, IL-6 and IL-1β, and apoptosis genes p53 and caspase 7 were studied. HU-2 exerted a significantly superior anti-inflammatory effect compared to HU-1 in all three proinflammatory genes. HU-2 showed a superior dose dependent anticancer effect through activation of p53 gene over HU-1 in MCF-7 cells. HU-1 exhibited a dose dependent effect on caspase 7 gene in both cell lines while HU-2 was more effective in A431. HU-2 has potential for development as a novel anti-inflammatory and anticancer agent.

Ficus krishnae stem bark and leaves are used for diabetes treatment in traditional medicines. Stem bark of F. krishnae was sequentially extracted with hexane, methanol and water, and these extracts were tested for their antihyperglyceamic activity by oral glucose tolerance test (OGTT) in overnight fasted glucose loaded normal rats. Hexane extract showed significant glucose lowering activity in OGTT, and the triterpene alcohols (cycloar-tenol+24-methylenecycloartanol) (CA+24-MCA) were isolated together from it by activity guided isolation and characterized by NMR and mass spectroscopy. The ratio of the chemical constituents CA and 24-MCA in (CA+24-MCA) was determined as 2.27:1.00 by chemical derivatization and gas chromatographic quantification. (CA+24-MCA) in high fat diet-streptozotocin induced type II diabetic rats showed significant antidiabetes activity at 1 mg/kg and ameliorated derailed blood glucose and other serum biochemical parameters. Cytoprotective activity of (CA+24-MCA) from glucose toxicity was evaluated in cultured RIN-5F cells by MTT assay and fluorescent microscopy. (CA+24-MCA) in in vitro studies showed enhanced cell viability in RIN-5F cells and significant protection of beta cells from glucose toxicity. Both in in vivo and in vitro studies (CA+24-MCA) showed enhancement in insulin release from the beta cells. In short term toxicity studies in mice (CA+24-MCA) did not show any conspicuous toxic symptoms. The combination of the phytosterols (CA+24-MCA) obtained through activity guided isolation of the stem bark of F. krishnae showed significant activity, and therefore is a promising candidate for new generation antidiabetes drug development.

In this study, an innovative bioavailable gingerol formulation, Ginactiv, was prepared by using polar−nonpolar sandwich (PNS) technology with a full spectrum of ginger matrix (FSGM). SEM images showed that Ginactiv was almost spherical, was well dispersed, had a smooth morphology with a particle size range of 50−60 μm, and was divided by three layers of PNS formulation. IR, DSC, a stability study, an enhanced and sustained release profile, and the good antioxidant potential of Ginactiv furthermore confirmed the existence of gingerols with great stability in a bioavailable form in the PNS formulation. Ginactiv registered a higher moisture content (3.98 ± 1.17%), hygroscopicity (0.94 ± 0.23 g/g), and water solubility index (43.71 ± 3.42%) in comparison to the ginger oleoresin values of 1.96 ± 0.72%, 0.36 ± 0.13 g/g, and 9.62 ± 1.21%, respectively, due to the good encapsulation of gingerols by the PNS technology. The existence of the synergistic effects of FSGM in Ginactiv can be utilized as a natural dietary supplement for supporting gastrointestinal and gut health improvement and to maintain the gut−brain axis.

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