BackgroundAntibacterial, immunomodulatory and antioxidant properties of aerial parts of Barleria lupulina Lindl were investigated in the present communication.MethodsThe antibacterial, antioxidant and immunomodulatory properties of B. lupulina (methanol soluble leaf and stem extracts) was analyzed by minimum inhibitory concentration, total phenolic contents, DPPH radical scavenging activity, determination of toxicity, hemagglutination antibody titre, delayed type hypersensitivity and neutrophil adhesion test, respectively.ResultsMethanol soluble leaf extract (MLE) contains more soluble bioactive compounds inhibiting the growth of five bacterial pathogens viz., Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, and Salmonella typhi even at MICs of 1.25 and 2.5 mg/mL. Aqueous stem extract (ASE) was least effective while MLE was highly effective in inhibiting the growth and survival of bacterial pathogens. While testing the effect of these extracts in animal model, no mortality of albino rats was recorded by using MLE and MSE at the concentrations from 200 to 600 mg/kg of their body weight. The MLE showed significant result in agglutination reaction and induced paw edema volumes when compared with untreated group (control). Both MLE and MSE extracts significantly increased neutrophil adhesion with increase in doses of extracts. MLE was found to have more potent immune-stimulant properties than the MSE. High phenolic contents were found in MSE while lowest IC50 values were found in MLE in term of DPPH radical scavenging activity.ConclusionsMethanol soluble leaf and stem extract of Barleria lupulina contains antibacterial, antioxidants and immunomodulating phytochemical compounds that was effective for antibacterial, antioxidant and immunomodulatory properties. These may be used as synthetic drug.

The present study was carried out for the evaluation of in-vitro antioxidant potential of alcoholic stem bark (ALSB) extract of Bauhinia variegata Linn. Dried stem bark extract of B. variegata Linn. was screened to evaluate its free radical scavenging effect. Various methods like DPPH assay, reducing power assay, percentage scavenging activity of hydrogen peroxide and superoxide radical scavenging activity were used for screening in-vitro antioxidant potential. Antioxidant potentials were concentration dependent which were compared with standard antioxidants such as butylated hydroxyanisole (BHA) and ascorbic acid. The maximum scavenging effect of B. variegata Linn. alcoholic stem bark extract on  DPPH free radical, superoxide radical and hydrogen peroxide was 72.19 + 0.20, 81.60 + 0.22 and 76.06 + 0.16 respectively at a concentration of 2500 ?g/mL.  It was clearly indicated that the alcoholic extract of the stem bark has significant in vitro antioxidant activity. Currently available synthetic antioxidants like butylated hydroxyanisole (BHA), butylated hydroxyl toluene (BHT), Ascorbic acid and gallic acid appear to be associated with hepatotoxicity and many others negative health effects. Therefore, natural antioxidants may be preferred over the synthetic antioxidants.

Cancer, the uncontrolled growth of cells, is not a single but a multifaceted disorder with malignant behavior, metastasis, and invasion, medically known as malignant neoplasm. The number of cases and morbidity due to cancer is rising alarmingly worldwide, causing around 21 % annually. Imidazoquinoxaline is a privileged scaffold with a wide range of pharmacological activities that is well explored for its anticancer potential. As a synthon, imidazoquinoxaline presents a large number of possibilities for structural modifications, which have attained the attention of many researchers for the development of new anticancer molecules with diverse improved target specificity and efficiency. Development of imiquimod followed by EAPB203 and EAPB503 derivatives further enhanced the popularity of this structural pharmacophore. In this report, we have focused on the anticancer potential of newly reported imidazoquinoxaline derivatives, along with their SAR studies and therapeutic potential. We have also enlisted the synthetic schemes reported for the synthesis of imidazoquinoxaline derivatives. The lead structural features described in this review will assist the researchers in designing and developing the novel imidazoquinoxaline pharmacophore containing anticancer compounds possessing the potential to interfere with various factors or mediators which are responsible for the progression of cancer. This report will also help in identifying the potent compounds which can be further evaluated in clinical trials for the development of new anticancer drugs with minimal to no side effects.

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The development of new pharmacologically active molecules targeting tubulin polymerization has recently attracted great interest in research groups. In efforts to develop new potent anticancer compounds, imidazole-tethered/fused pharmacologically active aryl derivatives possessing different substitution patterns targeting tubulin polymerization have been rationally designed and synthesized. The target molecules (P1-5 and KG1-5) were synthesized by multistep syntheses involving the reaction of intermediate 2-aminophenyl-tethered imidazoles with appropriate reactants in the presence of p-TsOH under different conditions. The synthesized compounds displayed moderate to good cytotoxicity, comparable to that of colchicine, against four cancer cell lines (MCF-7, MD-MBA-231, A549, and HCT-116). Compounds P2 and P5, with an imidazoloquinoxaline moiety, emerged as potential leads with cytotoxicity profiles against these cell lines similar to colchicine. Compounds P2 and P5 arrested cell division at the G2/M phase and prevented cancerous cell growth through induced apoptosis. These results favored the hypothesis that the compounds might act by binding to the colchicine binding site, which was further confirmed with the help of a tubulin polymerization inhibition assay. The results encourage the further exploration of imidazoloquinoxalines as promising leads that deserve advanced clinical investigation.

Computer-aided drug design is a powerful and promising tool for drug design and development, with a reduced cost and time. In the current study, we rationally selected a library of 34 fused imidazo[1,2-a]quinoxaline derivatives and performed virtual screening, molecular docking, and molecular mechanics for a lead identification against tubulin as an anticancer molecule. The computational analysis and pharmacophoric features were represented as 1A2; this was a potential lead against tubulin, with a maximized affinity and binding score at the colchicine-binding site of tubulin. The efficiency of this lead molecule was further identified using an in vitro assay on a tubulin enzyme and the anticancer potential was established using an MTT assay. Compound 1A2 (IC50 = 4.33–6.11 µM against MCF-7, MDA-MB-231, HCT-116, and A549 cell lines) displayed encouraging results similar to the standard drug colchicine in these in vitro studies, which further confirmed the effectiveness of CADD in new drug developments. Thus, we successfully applied the utility of in silico techniques to identify the best plausible leads from the fused azaheterocycles.

Malignant behavior and multiple abnormal cellular functions have rendered cancer a great challenge for scientists to treat. The rising death toll presents an alarming situation, and the side effects associated with marketed drugs has further increased the quest to develop new anticancer drug molecules. We herein report a rationally designed 2,4-disubstituted quinazoline-based bioactive pharmacophore possessing different substitution patterns to obtain potent anticancer active agents targeting tubulin polymerization. In this series, two compounds showed potent cytotoxicity against all four cancer cell lines (MCF-7, MD-MBA-231, A549, and HCT-116) comparable to that of colchicine. The compounds showed cell cycle arrest in the G2/M phase and induced apoptosis, which showed these compounds might act via binding to the colchicine binding site. These results were further confirmed via tubulin polymerization inhibition, which showed a similar profile to colchicine. Compounds with a propargyl moiety showed very low cytotoxicity as compared to colchicines, even in the presence of a trimethoxy substituent at the quinazoline ring, except for compound case. Two compounds are obtained as potential lead compounds for the development of active anticancer agents, with one having a similar profile to colchicine activity on tubulin polymerization inhibition. These compounds represent promising leads that deserve further investigation and optimization.

Albizzia procera belongs to family Fabaceae and has several phytoconstituents like flavonoids, terpenes, alkaloids, saponins etc. The plant is commonly used in traditional medicines. The objective of the present study was to assess the ameliorative effect of A. procera leaves extract against an experimentally induced gastric ulcer in albino rats. The antiulcer, antisecretory and cytoprotective properties of an ethanolic extract prepared from the leaves was evaluated. When given in a 200 mg/kg oral (per. os) dose, the extract produced 74% and 85% protection index in ethanol-induced ulcer model and pylorus ligation model, respectively.  Additionally, the extract also prohibited the formation of haemorrhage and edema, significantly lessened catalase activity (p<0.0001) and the lipid peroxidation level (p<0.0001) in the glandular tissue of Wistar albino rats. Furthermore, the extract also significantly diminished the total acidity(p<0.0001) of the gastric fluid by increasing its pH (p<0.0001). The occupancy of different phytoconstituents in the extract, such as flavonoids and tannins were identified that may be responsible for its gastro-protective activity. All these results provide a basis explaining the antiulcer ability of A. procera being useful in the management of gastric ulcers.