Natural Products Journal, The - Volume 7, Issue 4, 2017

Background: Coniothyrium had great potential in controlling Sclerotinia diseases in green houses and field with a high specificity. An important and steadily increasing number of natural products have been isolated from Coniothyrium spp, and the biological activities have not yet been fully elaborated. Objective: To promote the development of Coniothyrium source. Method: To analysis and sum up the literatures concerned. Results: The secondary metabolites of Coniothyrium mainly consisted of polyketides, polyaromatic compounds, and simple aromatic compounds, which have strong biological activity. Conclusion: Coniothyrium spp. as a source of biologically active metabolites is especially signifcant and ensures interest on this subject for years to come.

Cassia siamea Lamk is a tropical plant of family Caesalpiniaceae and is native of Southeast Asia. It is well-known for its nutritional, medicinal and economic importance and has been traditionally used for the treatment of ailments such as fever, malaria, diabetes, hypertension, asthma, constipation, diuresis, CNS disorders, jaundice, abdominal pain and menstrual pain either in crude form or as decoction of leaves and flowers. In some part of Asia, leaves and flowers of C. siamea are used as vegetables. Exhaustive literature is surveyed and summarized in this review to bring singlepot information for C. siamea available since 1925. C. siamea plant is found to be medicinally important for the treatment of several pathological complications. At the same time, it has also nutritional and economic importance. The major phytochemical constituents present include anthraquinones along with coumarins, alkaloids, flavonoids, glycosides, triterpenoids, sterols and other polyphenols. Further research on this plant has explored its specific pharmacological properties such as analgesic, antioxidant, anti-inflammatory, antimalarial, vasorelaxant, antitumor, antiarrhythmic, antiandrogen, anti-HIV and anxiolytic activity in various in vitro and in vivo studies. There is couple of reports that show toxicity concerns of this plant. It is an attempt to summarize morphological, microscopic, phytochemical, pharmacological and toxicological studies for improving research exploration and biomedical application potential of C. siamea.

Background: Plants offer various novel and structurally diverse potential chemical moieties which can be used as drugs or as leads for drug discovery. A comprehensive overview of the genus Diospyros L. (Family: Ebenaceae) is presented. Methods: A through literature search has been carried out using various search engines and all the reported data is incorporated followed by discussion of various selected experimental procedures for extraction, isolation and pharmacological evaluation. Results: The available data supports importance of Diospyros melanoxylon from its traditional medicinal value to advance pharmacognostic and pharmacological studies. Extracts and pure compounds from this genus have been reported for their antimicrobial, anti-inflammatory, cytotoxic, antidiabetic, antioxidant, antidiarrheal, and antiprotozoal activities. The medicinal uses section is concluded with details for various isolated chemical constituents. Conclusion: Presence of proteins and amino acids, tannin and phenolic compound, glycoside, sterol and steroids is found to be correlated with different pharmacological activities. The narrative review provide guidelines for the current area of research as well as for future investigations to benefit the field of medicinal and pharmaceutical sciences.

Background: Overproduction of biologically relevant free radicals in vascular tissues contributes to the development of endothelial dysfunction and progression of atherosclerotic lesions. Hypochlorite is a potent oxidizing and chlorinating ion, and its overproduction by neutrophils is linked to the development of vascular damage. Resveratrol has shown vasoprotective effects in several experimental models of vascular dysfunction. Objective: This study was performed to assess the effects of resveratrol on hypochlorite-induced endothelial dysfunction. Methods: Endothelial dysfunction was induced in isolated rat aortic rings by incubation with 75 μM sodium hypochlorite. The vasoprotective effect of resveratrol at concentrations of 0.1, 1 and 10 μM was assessed by adding it to a buffer solution for 30 min before or after incubation with sodium hypochlorite. Results: Incubating aortic rings with sodium hypochlorite induced endothelial dysfunction, whereas aortic rings incubated with 10 μM resveratrol before and after adding sodium hypochlorite showed less pronounced endothelial dysfunction, as evidenced by higher maximal relaxation and lower EC50 values. Treating aortic rings with 75 μM hypochlorite, 10 μM resveratrol or a combination of the two did not affect endothelium-independent relaxation. Conclusion: The results reveal that resveratrol attenuates the development of hypochlorite-induced endothelial dysfunction.

Background: Various techniques have been applied for detecting anacardic acid, cardanol, cardol, and 2-methylcardol and their degrees of unsaturation in a complex mixture of a highly corrosive cashew nut shell liquid found in the cashew (anacardium occidentale) nut shells. However, very little has been reported on the applicability of matrix-assisted laser desorption/ionisation time-of-flight mass spectrometry for the same. The aim of this paper is to report the application of this technique for identifying those components in technical cashew nut shell liquid obtained by a hot-roasting process. Methods: The cashew nut shell liquid analyte was diluted in acetone before adding a matrix of 2,5- dihydroxybenzoic acid, which contained acetone in a volumetric ratio of 1:2. This was followed by doping the analyte with either sodium or silver trifluoroacetate. Results: The mass spectra obtained by both sodium trifluoroacetate and silver trifluoroacetate dopants revealed existence of well-resolved peaks ascribed to cardanol and cardol in the analyte. It was further observed that the peaks corresponding to 2-methyl cardol and anacardic acid in the analyte could only be detected by using sodium trifluoroacetate dopant. The results have further revealed the possibility of the material to contain traces of other components between 0.3 and 23%. Peaks associated with those components may have been overlapped with peaks ascribed to the phenolic components. Conclusion: The results therefore suggest that this technique may be applicable for characterising the composition of technical cashew nut shell liquids when proper sample preparation is done and appropriate solvents, dopants and matrices are used.

Background: Compounds containing CN3 groups are named as guanidine derivatives, which have a rich history in biological and bio-inspired activity. Many guanidine moieties are reported for the antimicrobial activity. Present study aims to the enhancement of bio-activity of the guanidine subunits by conjugating with benzothiazole. Methods: A new series of benzothiazole guanidines have been synthesized from the reaction of thiourea derivatives of 6-substituted benzothiazoles with different substituted anilines in presence of HgCl2. The synthesized compounds were characterized through FT-IR, mass and 1H NMR spectral techniques. The synthesized compounds were screened for the Antimicrobial activity by disc diffusion method and antioxidant activity was assigned by DPPH and ABTS assay. Results: The products were screened for antimicrobial activity. They were found to exhibit moderate to potent activity against the tested microorganisms and have shown minimum inhibition concentration of 1.56 μg/mL for Candida albicans, 0.78 μg/mL for Aspergillus niger, 25 μg/mL for S. aureus and 12.5 μg/mL for E. coli. The derivatives were also tested for antioxidant DPPH and ABTS assays and they were found to have significant activities compared to the standards. Conclusion: In the present work, a new series of benzothiazole guanidinyl derivatives were synthesized in good yields by employing HgCl2 reagent. Synthesized compounds were screened for antimicrobial and antioxidant activities and compounds containing p-methoxy, o-hydroxy showed better antioxidant activities and antimicrobial activities.

Background: Papaya (Carica papaya) is well known for its medicinal properties as well as its use in traditional system of medicine. The recent rise in the knowledge of medicinal properties of papaya has significantly contributed to the modern pharmaceutical industries. Objectives: In this study, methanolic extracts of papaya leaves, un-ripened peels and seeds were studied for their phytochemical composition, antioxidant, anti-inflammatory, antidiabetic and anticancer properties. Methods: Bioactive compounds were identified using GC-MS analysis. The antioxidant effects of extracts were estimated by radical scavenging assay. In vitro anti-inflammatory activity was estimated by human red blood cell membrane stabilisation method. Antidiabetic activity of extracts was determined by α-amylase inhibition method. The viability of cells was assessed by MTT assay using MCF-7 and vero cell lines. Results: The free radical scavenging activity of methanolic extracts of leaf was found to be 67.78%, un-ripened peel 77.47%, and 90.12% at 1.0 mg/mL concentration. The percentage protection was calculated to be 75.87%, 91.25% and 88.25% and percentage hemolysis was calculated to be 24.12%, 8.75% and 11.75% of leaf, un-ripened peel and seed extract respectively. α-amylase inhibition (antidiabetic activity) of 86.93%, 62.16% and 59.90% was estimated in methanolic leaf, unripened peel, and seed extract respectively. In methanolic seed extract, the cell viability at 500 μg/mL concentration was 25.29%, the extract lysed 74.70% MCF-7 cells with IC50 lysis value of 183.48 μg/mL. Conclusion: From the results obtained in the present study, it can be concluded that the leaf extracts showed potential antidiabetic and anti-inflammatory activities. Peel extracts have high anti-oxidant & anti-inflammatory activity and seed extracts showed higher level of MCF-7 cell line inhibition.

Background: Essential oils, obtained by hydro distillation of plant parts, are important products in the world and have been traditionally used for treatment of infections and diseases. Due to their significant impact from an environmental point of view, there has been extensive research to explore and determine the antimicrobial activity of the plant essential oils. Methods: The chemical composition of the hydro distilled essential oils obtained from leaves of Cupressus sempervirens L. and Juniperus phoenicea L., collected from three different altitudes (125, 391, and 851 m high of sea level) at Al-Jabel Al-Akhdar area, Libya were analyzed by GC/MS, and higher than 30 compounds were determined in total. The impact of the altitude on the quantity and chemical constituents of the essential oils was studied. Results: The yield of the essential oils significantly depends on the species of the trees and the highest yield (0.29%) was obtained with C. sempervirens of altitude I (125 m) while the lowest (0.05%) was found with that obtained from altitude III (851 m). The chemical composition confirmed that the oils were rich in essential phytochemicals including monoterpenes, monoterpenes hydrocarbons, sesquiterpenes and diterpenes. These constituents revealed some variability among the oils displaying interesting chemotypes, 1R-α-pinene (15.06-27.33%), α-myrcene (3.89-7.94%), 3-carene (3.31- 19.63%), limonene (3.93-19.39%), terpinolene (1.91-6.62%), α -terpinyl acetate (5.45-12.98%), β - caryophyllene (1.17-23.92%), and (E)-germacrene D (2.08-4.43%) which were the main constituents of the oils isolated from three altitudes. The oils were tested in vitro for antifungal activity against Botrytis cinerea (Pers.) as plant pathogen. In general, the oils exhibited an inhibition of the mycelia growth and the most significant result was obtained with J. phoenicea oils with EC50 111.73, 195.21 and 210.19 μg/ml at altitudes I, II and III, respectively. Conclusion: The results of this work points out the importance of the environmental conditions which are in direct relation with the altitude could affect significantly the oil composition both in qualitative and quantitative. Consequently, their biological activities are considerably influenced. Moreover, the obtained data offer the opportunity to choose essential oils with preferential compounds for pharmaceutical, antimicrobial, and food industries in such important region in Libya.

Background: One of the trends in the pharmaceutical, cosmetic and food market is the development of products with natural components, especially plant products. Besides being used as a beverage, yerba mate (Ilex paraguariensis St. Hil.) has traditionally been used in folk medicine due to its many therapeutic effects. Objective: The present study aims to evaluate the yerba mate utilization profile in the pharmaceutical and food industry by analyzing patent documents. Methods: Patent documents were retrieved using Derwent Innovations Index database. Results: Although the number of patent applications had remained almost constant throughout the years, it has been increasing since 2008. The applicants are preponderantly companies and applications are technologically concentrated in the food, pharmaceutical and cosmetic industries, where yerba mate has been used as a component for diverse products, including energy drinks, weight loss, and anti-wrinkle preparations. Conclusion: These data can serve to promote innovation and strategic planning, optimizing yerba mate uses in pharmaceuticals, cosmetics, and food supplements; therefore enhancing the aggregate value of the plant culture.

Background: The use of plants for the treatment, cure and prevention of diseases is one of the oldest medicinal practices of humanity. These plants are able to produce much diversified natural compounds (e.g. alkaloids, polyphenols, etc.) which have many pharmaceutical applications. Objective: The aim of the present study was to evaluate the antioxidant capacity and antibacterial activity of Zizyphus lotus extracts, which has been used traditionally in folk medicine of Algeria. Methods: The leaves of plants were submitted to extraction by water and methanol to give methanolic (Met.E) and aqueous (Aq.E). The extracts were analyzed by HPLC-TOF/MS and their antioxidant activity was determined using DPPH and ABTS free radical-scavenging test, when the antibacterial activity was determined using disc diffusion method. Results: The quantitative analysis of polyphenols and flavonoids content showed that the Met.E had the highest amount (562.04 μg EAG/mg E and 66.34 μg EQ/mg E, respectively). The HPLC-TOF/MS analysis of Met.E reveals the presence of two major compounds, rutin and gentisic acid, when Aq.E contain rutin and quercetin-3-β-D-glucoside as a major compound. Results showed that the Met.E exhibited the highest antiradical activity against DPPH and ABTS free radical with EC50=28.19±0.51 μg/mL, and EC50=3.82±0.03 μg/mL, respectively. Moreover, the Met. E of Z. lotus presents a moderate antibacterial activity against Staphylococcus aureus, Micrococcus luteus and Bacillus subtilis, with inhibition zone ranging from 09 to 13 mm. In addition, The Met.E showed a better MIC against M. luteus and B. subtilis (MIC= 25 μg/mL). Conclusion: Our results showed that the methanolic extract of Z. lotus reported a considerable antioxidant and antibacterial activities which may be due to their richness on polyphenols and flavonoids.