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A study on the anti-viral properties of Azadirachta indica (A.Juss, Neem) against HBV, HIV, HSV-I, Vaccinia and Varicella zoster viruses and Coscinium fenestratum (Gaertn.) Colebr, Tree turmeric against HBV and HIV
Abstract
Background and Objectives: Extracts of parts of three plants - Azadirachta indica (A.Juss) and Coscinium fenestratum (Gaertn.) Colebr. were prepared using various solvents namely hexane, petroleum ether, chloroform, methanol, and ethanol to identify their antiviral properties. Methods: These crude extracts were subjected to physico-chemical and anti-viral properties. Anti-HBs Ag, anti-HBV DNA polymerase and RT inhibition assays were performed for the plant extracts and methanolic extracts of C.fenestratum and A.indica were subjected to GC-MS. while docking studies were performed for HBV and HIV receptors for both the plants and docking studies were performed against receptors of HSV-Type I, Varicella Zoster and Vaccinia viruses for A.indica alone. Results: The ethanolic and methanolic extracts of A.indica inhibited HBsAg but the hit compound didn't bind to both HBV and HIV receptors. However GC MS hit compound of methanolic extract of A.indica docked with receptors of HSV-I, Vaccinia and Varicella zoster receptors. On the other hand methanolic and ethanolic extracts of C.fenestratum inhibited only HIV -RT but not HBsAg. However GCMS extracts of C.fenestratum methanolic extract docked with receptors of both HIV and HBV. Conclusion: The present findings revealed the potential anti-viral properties of A.indica against HSV-I, Vaccinia and Varicella zoster Viruses and C.fenestratum against HIV and HBV.
... Neem leaves extract possess a wide range of antibacterial effect against gram positive and gram negative as well as against Mycobacterium tuberculosis(Chorpra et al., 1952). In-vitro studies showsgrowth inhibition of Vibrio cholerae, Klebsiella pneumoniae, and M. pyogenes(Satyavati et al., 1976).Azadirachta indica leaf extract also suggest in vitro antiviral activity against Vaccinia virus(Anushka et al., 2011), Chikungemya and measles virus, group B coxsackieviruses(Satyavati et al., 1999) and herpes simplex virus type-1(Tiwari et al., 2010). Azadirachta indica leaves have quercetin and beta-sitosterol polyphenolic flavonoids which also shows antifungul activity(Govindachari et al., 1998). ...
Background: Herbal drugs are used in treatment of diseases since decades. Major contributing factor for their use is easy availability, less expensive and more belief of common population because of relatively less side effects compared to allopathic medicines. Medicines of natural origin or functional foods in the prevention of disease are the need of hour. Hence, the present review focused on activity of four drugs viz. Withania somnifera,Allium sativum,Curcuma longa andAzadirachta indica and role in different clinical complications. Methods: A thorough review of all the articles, research as well as reviews available regarding the concerned topic was performed. MEDLINE database was searched and English language articles were preferably selected. Results: Withania somnifera, Allium sativum, Curcuma longa andAzadirachta indicahave shown alleviation in inflammation, diabetes and cancer states. The herbal drugs have shown beneficial effects in the prevention and treatment of these disorders. Conclusion from these facts:Utilizing this concept, it can be assumed that herbal drugs play an intricate role in safeguarding the health of individuals from life-threatening complications. However, validation and reproducibility of results in clinical trails should be there in order to confirm the safety and efficacy of these herbal drugs.
Quantitative structure-activity relationships (QSAR) and Comparative Molecular Field Analysis (CoMFA) have been applied in order to explain the structural requirements of HIV-1 reverse transcriptase (HIV-1 RT) inhibitory activity of TIBO derivatives on the MT-4 cells. The best QSAR model is satisfactory in both statistical significance and predictive ability. The derived structural descriptors indicate the importance of electronic contributions toward the HIV-1 RT inhibition of this class of compounds. However, it could not reveal any hydrophobic influence because of high collinearity between C2 and logP variables. In order to cope with steric interaction in the correlation, 3D-QSAR was performed using CoMFA. The obtained CoMFA model shows high predictive ability, r2
cv=0.771, and clearly demonstrates its potential in the steric feature of the molecules through contour maps, explaining a majority (81.8%) of the variance in the data. Consequently, these results can be useful in identifying the structural requirements of TIBO derivatives and helpful for better understanding the HIV-1 RT inhibition. Eventually, they provide a beneficial basis to design new and more potent inhibitors of HIV-1 RT.
It has been suggested that Phyllanthus amarus may be helpful in the treatment of hepatitis B virus infection. We studied the effect of an aqueous extract of P. amarus on the cultured hepatoma cell line HepA2. This cell line had been transfected with tandemly arranged HBV DNA and continued to synthesize and secrete both HBsAg and HBeAg. Extract of P. amarus reversibly inhibited cellular proliferation and suppressed HBsAg production but not HBeAg production in HepA2 cells. We also found that P. amarus suppressed HBsAg gene expression at mRNA level in a time-dependent manner, and selectively abolished the HBsAg gene promoter driven CAT activity. Our results demonstrate that P. amarus contains some active components which can suppress the HBsAg gene expression in human hepatoma cells. Such suppression may contribute the antiviral activity of P. amarus in vivo.
A rapid extraction procedure for fingerprint chromatogram of different types of Mentha piperita L. (Labiatae family) is presented. The extracts were analysed by gas chromatography and gas chromatography-mass spectrometry (GC/MS). The main volatile compounds identified by the gas chromatography-mass spectrometric analysis of M. piperita L. were menthol, menthone, isomenthone, 1,8-cineole, menthyl acetate, limonene, beta-myrcene, carvone. M. piperita L. oil had the active principles: menthol, menthone, isomenthone, menthyl acetate, alpha-pinene, beta-pinene, champhor, limonene, linalool, piperitone. M. crispa L. showed carvone as major component.
Inhibitors of HIV reverse transcriptase (RT) are important drugs for the treatment of acquired immuno-deficiency syndrome (AIDS). One approach to identify novel inhibitors of HIV-1-RT is the screening of natural compounds. Many natural products have been shown to be active as RT inhibitors. These compounds belong to a wide range of different structural classes, e.g., coumarins, flavonoids, tannins, alkaloids, lignans, terpenes, naphtho- and anthraquinones, and polysaccharides. The life forms from which the bioactive compounds were isolated are as equally diverse and comprise terrestrial and marine plants, micro-organisms, and marine animals. From the most extensive screening effort, carried out by the NCl, calanolide A, isolated from the terrestrial plant Calophyllum lanigerum (Guttiferae), has been discovered as the most interesting natural RT inhibitor. The promise of this natural product probably relates to a novel mechanism of action. The current review describes natural products from various sources that are able to inhibit HIV-RT.
Methanolic-aqueous extracts of 70 plants were investigated for their ability to inhibit HIV-1 reverse transcriptase activity in vitro. Two thirds of the extracts screened showed more than 50% inhibition. Two extracts inhibited the enzyme completely while four exhibited more than 90% inhibition. Tannins as nonspecific HIV-1 RT inhibitors were detected and removed from the extracts. The IC50 values of the most potent extracts after the removal of tannins for the HIV-1 RT inhibition are as follows: Sambucus racemosa 0.017 mg/ml and Geranium phaeum 0.067 mg/ml. Daunomycine was chosen as a standard substance in the non-radioactive immuno assay used for screening. As a result from the future isolation and characterization of these compounds, new leading structures are expectable.
The interaction of a series gag peptide analogues with human cyclophilin A (hCypA) have been studied employing molecular docking and 3D-QSAR approaches. The Lamarckian Genetic Algorithm (LGA) and divide-and-conquer methods were applied to locate the binding orientations and conformations of the inhibitors interacting with hCypA. Good correlations between the calculated interaction free energies and experimental inhibitory activities suggest that the binding conformations of these inhibitors are reasonable. A novel interaction model was identified for inhibitors 11, 15, and 17 whose N-termini were modified by addition of the deaminovaline (Dav) group and the C-termini of 15 and 17 were modified by addition of a benzyl group. Accordingly, two new binding sites (sites A and D in Figure 1) were revealed, which show a strong correlation with inhibitor potency and thus can be used as a starting point for new inhibitor design. In addition, two predictive 3D-QSAR models were obtained by CoMFA and CoMSIA analyses based on the binding conformations derived from the molecular docking calculations. The reasonable r(cross)(2) (cross-validated) values 0.738 and 0.762 were obtained for CoMFA and CoMSIA models, respectively. The predictive ability of these models was validated by four peptide analogues test set. The CoMFA and CoMSIA field distributions are in general agreement with the structural characteristics of the binding groove of hCypA. This indicates the reasonableness of the binding model of the inhibitors with hCypA. Considering all these results together with the valuable clues of binding from references published recently, reasonable pharmacophore elements have been suggested, demonstrating that the 3D-QSAR models about peptide analogue inhibitors are expected to be further employed in predicting activities of the novel compounds for inhibiting hCypA.