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Purpose: Long-term clinical usage of nonsteroidal anti-inflammatory drugs (NSAIDs) is associated with significant side effects -gastrointestinal lesions, bleeding and nephrotoxicity. Therefore, the discovery of new safer antiinflammatory drugs represents a challenging goal for this research area. (4d, e, h, j, k, q, p) Methods: Various derivatives of 3-(2-aminopyrimidin-4-yl) indoles viz. 4-(4-substitutedphenyl)-6-(2-(4-substitutedphenyl)-1H-indol-3-yl) pyrimidin-2-amine (4a-4r) were synthesized by cyclization of (3-(4-substitutedphenyl)-1-(2-(4-substitutedphenyl)-1H-indol-3-yl) prop-2-en-1-one) of indole with guanidine

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In this investigation, the fabrication of capsaicin loaded self nano emulsifying drug delivery system (SNEDDS) was attempted to improve the effectiveness of capsaicin through the oral route. A pseudoternary phase diagram was constructed at different km values (1:1, 2:1, & 3:1). Nine liquid formulations (LeCAP-1 to LeCAP-9) were prepared at km ¼ 3, evaluated & converted to solid free-flowing granules using neusilin® US2. LeCAP-3 comprising of 15% isopropyl myristate, 33.75% Labrafil, & 11.25% ethanol exhibited higher % transmittance (98.90 ± 1.24%) & lower self-emulsification time (18.19 ± 0.46 s). FT-IR spectra showed no incompatibility whereas virtual analysis confirmed hydrogen bond interaction between amino hydrogen in the capsaicin & oxygen of the neusilin. DSC & XRD study revealed the amorphization & molecular dispersion of capsaicin in S-SNEDDS. TEM analysis confirmed the nano-sized spherical globules. Within 15 min, L-SNEDDS, S-SNEDDS, & pure capsaicin showed 87.36 ± 3.25%, 85.19 ± 4.87%, & 16.61 ± 3.64% drug release respectively. S-CAP-3 significantly (P < 0.001) inhibited the proliferation of HT-29 colorectal cancer cells than capsaicin. Apoptosis assay involving Annexin V/PI staining for S-CAP-3 treated cells demonstrated a significant (P < 0.001) apoptotic rate. Remarkably, 3.6 fold increase in bioavailability was observed after oral administration of capsaicin-SNEDDS than plain capsaicin.

Background:Peptic ulcer is a digestive disorder most commonly found in clinical practice. Given the many side effects of modern medicine, the initial acquisition of fewer side effects, and medication of indigenous drugs, it should be considered as a better alternative for the treatment of peptic ulcer.Objective:To assess antiulcer and antioxidant activity of ethanol extract of Barleria gibsoni (EBG) Dalz. leaves in ulcer-induced rats and in vitro antioxidants method, respectively.Materials and Methods:Ethanol EBG was screened for antiulcer activity in pylorus ligation-induced ulcer models in Wistar rats. In vitro antioxidant activity of the extracts was tested using 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO) radical scavenging activity. Total phenol and flavonoid content in the extracts were determined spectrophotometrically.Results:Oral administration of ethanol extract of leaves at doses of 250, 500 mg/kg p.o. reduced significant gastric lesions induced by pylorus ligation-induced ulcer as compared to standard omeprazole (20 mg/kg p.o.). The IC50 values were found to be 150 μg/mL in leaves extract. The ethanol extracts showed good antioxidant capacity in DPPH radical scavenging assay and NO radical scavenging activity when compared to standard. The total phenolic content using Folin–Ciocalteu reagent estimated in 1 mg of leaves extracts was 368 μg and 481 μg with gallic acid equivalent and also the total flavonoid content found to be 240 and 410 μg, respectively, with quercetin equivalence.Conclusion:These findings suggest that the leaves of B. gibsoni possessed antiulcer potential and antioxidant compared to standard. This is the first ever report of antiulcer and antioxidant activities in B. gibsoni (Acanthaceae).SUMMARY In vivo antiulcer and in vitro antioxidant activity of Barleria gibsoni was evaluated.Soxhelt extraction was carried out and extracts were subjected to qualitative phytochemical analysis. Extract obtained by Soxhlation showed higher total phenolic and flavonoid contents.EBG showed DPPH and Nitric oxide scavenging activity indicating its strong antioxidant potential.On pylorus ligation-accumulated secretions and the related ulcers confirm gastric acid output to be the basic cause of gastric ulcers. Ethanol extract of leaves attenuated the gastric volume, free acidity, total acidity and ulcer index thus showing the anti-secretory mechanism.The results of the histopathological investigation of Barleria gibsoni leaves for antiulcer effects using pylorus ligation induced ulcer model in rats laid credence to traditional use of the plant leaves in ulcer treatment. The ethanol extract of leaves demonstrated increase in percentage preventive index compared to omeprazole respectively. From the present study results reveals the antiulcer activity of ethanol extract leaves which is comparable to that of Omeprazole. Abbreviations Used: EBG: Ethanol extract prepared from the leaves of B. gibsoni, ROS: Reactive Oxygen Species, DPPH: 2, 2-diphenyl-1-picrylhydrazyl, NO: Nitric Oxide, IC50: The ha...