Current Bioactive Compounds - Volume 15, Issue 4, 2019

Background: Phytoconstituents of fruits, vegetables, spice and herbs are important for human health. Phytoconstituents play an important role in the growth, development, defensive mechanism, colors, odour and flavors of plants. Psoralea corylifolia Linn (P. corylifolia) commonly known as ‘Bakuchi’ belongs to Leguminosae family widely distributed in China and Southeastern Asian countries. Methods: Various electronic databases such as PubMed, Science Direct, Scopus and Google were searched to collect the data of the present review. Further, all the collected information was categorized into different section as per the aim of the paper. Moreover, analyzed data were also presented in the graphical abstract. Results: Seventy-two research and review papers have been collected and were included in the present review. Nineteen papers contained general information’s of P. corylifolia, Psoralens and psoralidin whereas thirty paper data were presented in the pharmacological activities sections and remaining in the Analytical tools and discussion section. From these databases, we can say that P. corylifolia possesses antibacterial, anti-inflammatory, antifungal, antioxidant, antiflarial, estrogenic, antitumour, and immunomodulatory activities. Psoralens are mainly used in the treatment of psoriasis, vitiligo and dermatitis. Topical or oral psoralens followed by UVA radiation exposure are one of the best treatments of leucoderma. Psoralidin exhibits antioxidant, anti-apoptotic, anti-inflammatory and antitumor activities. Conclusion: This review summarizes an overview of P. corylifolia, psoralen and its derivative psoralidin with respects to their pharmacological activities, medicinal uses, biological activities and bioanalytical aspects. These data will be helpful in the translation of information from traditional to the modern medicine of psoralidin.

The genus Moquiniastrum belongs to the Asteraceae family and is widely and exclusively dispersed throughout South America. Its species adapt easily to different cultivation conditions, and present a varied chemical composition with a great performance in pharmacological and pharmacognosy studies, mainly for sesquiterpene lactones. Moquiniastrum polymorphum is a species distinguished in the genus, presenting socioeconomic potential in several sectors, besides great application in folk medicine to treat respiratory diseases. The bioactive properties highlighted in the research are antioxidant, allelopathic, anti-inflammatory, insecticidal, antiviral and antimicrobial activity, and toxicity against different cancer lines, among others. To date, from 21 species belonging to the genus Moquiniastrum 11 species have been studied for their chemical composition, and only five species have been studied for their biological or toxicological activity. Different parts of the plants have been analysed, such as flowers, leaves and bark of the trunk and roots, and extracts obtained by different extraction methods and solvents. The genus has in its chemical composition classes of molecules such as sesquiterpene lactones, sesquiterpenes, diterpenes, triterpenes, flavonoids, coumarins, caffeic acid derivatives, acetylene and non-protein amino acids. Isolation studies of the chemical constituents of the species are promising considering that they are safe to use since they do not cause changes in DNA and can be used even during the gestational period.

Background: Itraconazole is a triazole derivative and possesses structural similarities to the azole group (imidazoles and triazoles). It is a broad spectrum fungistatic. It belongs to BCS class II category i.e. it has poor solubility and high permeability. Objective: Dissolution enhancement of poorly soluble itraconazole using purified neem gum as a natural carrier via binary dispersions and other methods was studied. Topical gel formulations of binary dispersions were developed and evaluated for in vitro and in vivo antifungal activity. Methods: Five batches of solid dispersions (SD1-SD5) in various ratios of drug: neem gum were prepared by the solvent evaporation technique. Other mixtures were also prepared by kneading, cogrinding, physical mixing methods and evaluated further. Topical gel formulations were further developed and evaluated for antifungal activity (both in vitro and in vivo). Results: Equilibrium solubility studies of various mixtures indicated SD3 (1:3) as the optimum batch out of all solid dispersion batches. Equilibrium solubility studies of mixtures (KM, CGM, PM, SM) indicated significant solubility enhancement of kneading mixture in comparison to other mixtures. FTIR studies indicated no interaction of the drug to the polymer. DSC, SEM and XRD studies indicated a transition from crystalline to the amorphous state of the drug. SD3 batch showed remarkably improved dissolution characteristics (100% drug release in 1.5 h) in comparison to the pure drug (38% in 2h). Further, the topical gel of SD3 was evaluated for in vitro diffusion, in vitro and in vivo antifungal activity. Sustained drug release (53% in 24 h) was observed in SD3 based gel formulation which is significantly higher than that in comparison to pure drug based gel (30% in 24 h). The increased area of zone of inhibition of SD3 based gel indicated better antifungal activity of the SD3 gel formulation. Further histopathology examination of skin specimens indicated enhanced efficacy of SD3 based gel in comparison to pure drug based gel. Conclusion: Solid dispersion based topical gel formulation exhibits better antifungal activity in comparison to pure drug based gel.

Background: An efficient one-pot biocatalysed ultrasound assisted synthesis of dihydropyrimidinones/ thiones has been developed under solvent free conditions. Materials and Methods: The use of biodegradable, non toxic, agar-powder as a catalyst provide advantages like high yield, simple operation, mild reaction condition with short reaction time. 1,2,3,4- tetrahydropyrimidine-2-ones/thiones formed were characterized by mass and 1H NMR spectroscopy. Results: The dihydropyrimidinones substituted with electron donating groups like fluorine, hydroxy along with thienyl groups exhibited good antibacterial activity. The compounds exhibited favorable binding interactions with mycobacterium target protein H37Rv. Conclusion: 4-methoxy substituted dihydropyrimidinones derivative showed significant antituberculosis activity.

Background: Squalene Synthase is one of the cholesterol biosynthetic pathway enzymes, inhibition of which produces potent lipid lowering action. A variety of chemical classes have been evaluated for its inhibition to provide alternate antihyperlipidemic agents to statins. Methods: A series of N-substituted-sulfomoyl-phenyl-amino carboxylic acid derivatives were designed through pharmacophore modelling as Squalene Synthase inhibitors. We report here the synthesis, characterization and in vitro pharmacological screening of the designed molecules as Squalene synthase inhibitors. The target molecules were synthesized by a simple procedure and each molecule was characterized by IR, Mass, 1HNMR and 13CNMR spectroscopic techniques. As a primary site of action for cholesterol biosynthesis is liver, each of the molecules were first screened for in vitro cytotoxicity over human hepatic cell line (HepG2) by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay method. The enzyme inhibition assay was performed on cell lysates prepared from HepG2 cells by Human Squalene Synthase ELISA kit, where test compounds were added in the nontoxic concentrations only. Results: Compound 5f was found to be most potent with the IC50 value of 11.91 μM. The CTC50 value for 5f on human hepatic cell line was > 1000 μM so it was considered that the compound was relatively safe and might be free of hepatotoxicity. Conclusion: From the results of our studies, it was observed that compounds with poly nuclear aromatic or hetero aromatic substituent on a side chain were more potent enzyme inhibitors and a distance of 4-5 atoms is optimum between amide nitrogen and hydroxyl group of carboxylic acid.

Background: Infectious diseases are major leading cause of death in all parts of the world, because of the appearance of new multi drug resistant microbes. Therefore, the discovery of potential drug for effective treatment will help the slaughter of the microbes. The aim of the present study is to evaluate the presence of photochemical and antimicrobial activities of various crude extracts of leaves, fruits and root bark of Atalantia monophylla and Atalantia racemosa against human pathogens by using well diffusion method. Methods: Antimicrobial properties of the various extracts of Atalantia monophylla and Atalantia racemosa were studied against some human pathogenic microbes such as Gram-positive Bacteria, (Bacillus subtilis, Bacillus cereus, Staphylococcus aureus) Gram-negative Bacteria (Klebsiella pneumoniae, Pseudomonas aeruginosa, Escherichia coli) and human opportunistic fungal pathogens (Candida albicans and Aspergillus niger). All the extracts were comparable with standard drugs (Ciprofloxacin, Gentamicin, Nystatin. and Amphotericin B). Minimum inhibitory concentration (MIC), minimum bactericidal /fungicidal concentration (MBC/MFC) values were determined through a microdilution method. The phytochemical analysis of these plant extracts were carried out using standard mthods. Results: Methanolic leaf extract of A. monophylla has showed excellent antimicrobial activity against S. aureus (40mm). As well, the A. racemosa methanolic leaf extract shows notable inhibitory activity against S. aureus (38mm). At the same time, the least inhibition was observed in aqueous extract of A. monophylla against E.coli (9mm). The MIC ranged from 0.78 μg/mL to 50 μg/mL and MBC/MFC 1.56 to 50 μg/mL were recorded. Phytochemical analysis of alkaloids, steroids, saponins, flavonoids, tannins, terpenoids, phenolics and cardiae glycoside were recorded in various extracts of A. monophylla and A. racemosa respectively. Flavonoids, phenolics and cardiac glycoside were present only in methonalic leaf extract of A. monophylla. Conclusion: The result of this study concluded that methanolic leaf extract has possessed novel compounds with significant antimicrobial properties. Hence, we recommend this plant for further studies on the isolation and characterization of that lead antimicrobial potential molecule.

Background: Oxidation reactions are known to shorten the shelf life and cause damage to foods rich in fat, such as dairy products. One way to limit oxidation and increase the shelf life of fermented dairy products is to use natural antioxidants. The aim of this study was to examine the effect of adding pomegranate extracts in the antioxidant properties, rheological characteristics and the storage stability of the fermented product of kefir. Methods: The Pomegranate Juice (PGJ) and Peel Extracts (PGPE) (5%, 10% w/v) were added to kefir and the antioxidant properties were evaluated by using the methods of radical scavenging activity (DPPH) and Ferric Reducing Antioxidant Power Activity (FRAP). Spectrophotometric and instrumental methods were used to determine the Total Phenols (TPs), pH values, viscosity and flow behavioral index values of enriched with pomegranate kefir samples. The same properties were tested when kefir samples stored at 4°C for 7, 14, 21 and 28 days. Results: The addition of PGJ and PGPE results in an increase in the antioxidant activity (DPPH, FRAP) and total phenol content (TPs) of kefir samples. Increasing the concentration of the added PGJ and PGPE, results in an increase in the TP content and the DPPH activity of kefir. As far as the storage time is concerned, the results showed an increase in the amount of TP at 7th day and a reduction in the DPPH activity in the 14th day of storage. In contrary to the DPPH method, the increase in storage time has resulted in a reduction in antioxidant activity by the FRAP method. The addition of PGJ and PGPE in kefir results in a decrease in pH values while the pH of kefir samples increased during storage at 4°C for 28 days. The addition of PGJ and PGPE to kefir samples results to a decrease in viscosity and an increase in the flow behavior index. Increasing storage time results in increased flow behavior index of kefir samples. Conclusion: The addition of PGJ and PGPE increased the antioxidant activity and total phenols of the kefir product and preserved its properties during the total storage time of 28 days at 4°C.

Background: Malaria is one of the life threatening diseases which is caused by Plasmodium sp. of protozoa and uses Anopheles mosquitos as vector. Plasmodium vivax and Plasmodium falciparum are common form of malaria parasite. Artemisinin is reported for its antimalarial activities and Artemether which is a methyl ether derivative of Artemisinin, has been found effective against P. falciparum. Methods: In the present study, bioconversion of Artemisinin into Artemether was carried out experimentally and the statistical tools like experimental factorial design and Response Surface Methodology were used to find optimal conditions (concentration of Artemisinin, age of inoculum, temperature & pH) using Cunninghamella echinulata var. elegans. Experimental conditions for maximum product recovery from culture broth were also optimized using various polar and non-polar solvents for extraction. Artemether purity was analyzed by reverse-phase HPLC. Experimental data was fitted in a quadratic model and effect of various parameters was analyzed. Results: It was found that bioconversion of Artemisinin into Artemether is growth associated process. It was observed that molasses used as carbon source supported production of Artemether to 3.4g/L. The biomass and oxygen are key element affecting of bioconversion of Artemisinin into Artemether such as higher dissolved oxygen reduced the Artemether bioconversion. The highest bioconversion of Artemisinin into Artemether was obtained at temperature 25.5°C, 5g/L concentration of Artemisinin, at age of inoculum of 44.5 h and at pH 6.0. Model suggested the highest bioconversion of Artemisinin into Artemether was 54% at shake flask level which was near about experimental finding. An optimal condition for bioconversion was also analyzed and 64% bioconversion was obtained in 5L bioreactor. Conclusion: The outcomes of the study provided optimum conditions for bioconversion of Artemisinin into Artemether.