Natural Products Journal, The - Volume 5, Issue 3, 2015

Natural monophenols exhibit various properties including antioxidant, therapeutic action and toxicity. This review is unique in application of a unifying mechanistic theme comprising electron transfer, reactive oxygen species and oxidative stress. Representative phenols are as follows: salicylic acid, guaiacol, eugenol, (S)-tyrosine, vanillin, capsaicin, 6-gingerol, carvacrol, thymol, tocopherol, 5-hydroxytryptamine, psilocin, sesamol, estradiol, cannabinoids, etoposide, morphine and heroin, cresols, and other related phenols, such as platensimycin and polyphenols (vancomycin and tetarimycin A). This approach to mode of action may assist in improved drug design.

Phytochemical investigation on the methanol extract of Phyllanthus myrtifolius leaves led to the isolation of a new oleanan derivative, 3β-(3’,4’-di-O-acetyl-α-L-arabinopyranosyl)-12-oleanen- 28-oic acid (1). The structure of compound 1 was determined mainly by extensive NMR data analysis. Together with this compound, six arylnaphtalene lignans 2–7 were also isolated and identified. The isolated compounds 1–7 were tested for their antibacterial activities against eight pathogenic bacteria, showing that compound 1 exhibited highest activity.

Loranthus micranthus, a parasitic plant of different hosts has been used for treating various diseases traditionally as it has pharmaceutically important phytochemicals. The methanol extract of L. micranthus two fractions (17 and 21) were selected based on visibility and less compounds in TLC for identification of phytochemicals in GC-MS and yielded 13 and 12 different chemical compounds respectively. The yielded compounds from each fraction have pharmaceutical importance and possess different biological activities. Each compound’s mass spectrum was given and analysed. The two fractions were evaluated for biological activities to know the efficacy of the compounds. In both, antioxidant activities (DPPH and FRAP), the fraction 17 had shown strong activity (74, 819.48± 0.05) compared to fraction 21 and standard. The albumin denaturation, membrane stabilization and proteinase activities were tested using these two fractions and fraction 17 exhibited strong activity on these tests effectively (87.39± 0.26, 81.67± 0.23 and 86.19± 0.25). The antilipoxygenase activity (63) of fraction 17 is near to standard. Fraction 17 strongly inhibited COX-1 and COX-2 activity. Based on the results, fraction 17 had 13 different phytochemicals and exhibited strong antioxidant, anti-inflammatory and COX-1 and COX-2 activity, which may be due to a combination of all compounds or any one single compound. It can be concluded that the fractions of methanol extract of Loranthus micranthus have pharmaceutically important compound(s) and further research is needed to isolate each compound to know the exact pharmaceutical compound.

Ayurveda, An Indian system of medicine has described several drugs from indigenous plant sources for use in the treatment of bronchial asthma and allergic disorders. Traditionally Fagonia schweinfurthii Hadidi (Family- Zygophylaceae) is used for allergies and other skin diseases. The current study evaluates the anti-histaminic activity of aqueous extract of F. schweinfurthii Hadidi and then anti-histaminic formulation (syrup) was prepared and evaluated for various parameters. Plant Fagonia schweinfurthii Hadidi was collected from local area. Aqueous extract was obtained by extraction of moderately coarse powder of F. schweinfurthii Hadidi was carried out by decoction method with water and dried. Anti-histaminic activity of plant extract was evaluated by using Guinea pig ileum and for the comparison of anti-histaminic activity ceterizine (10 mg) was used as model drug. In the present study it was found that aqueous extract of F. schweinfurthii Hadidi showed significant anti-histaminic activity. The outcomes of study showed that 16% and 18.8% inhibition in maximum response produced by histamine was observed for plant extract (1000 μg/ml) and standard drug (50 μg/ml) respectively when 5 μg/ml dose of histamine was used. From this study 2 g dose was selected for the preparation of syrup. The results indicate that aqueous extract of F. schweinfurthii Hadidi has significant anti-histaminic activity and syrup which contains 2 g of extract has similar anti-histaminic activity to marketed preparation.

Preparative separation and characterization of an indane carboxylic acid diastereomer 3 from chemical transformation of lapachol 1 and the enantiomeric resolution of each one of the former compounds by chiral HPLC, plus the comparison between the experimental and calculated CD spectra, by spectroscopic and quantum chemical calculation of their circular dichroism (CD) spectra is described. The use of simple and correct cis-trans nomenclature, based on the relative direction (above or below the ring plane) of the two priority substituents, namely the hydroxy and prenyl groups explains clearly the formation of the diastereomers in different proportions. The cis-isomer 3b was presumed to be the major diastereomer on the basis of steric factors (interaction with methyl ester) and later on, this assumption was experimentally confirmed (CD experimental-calculated comparison) and attributed (RS/SR) absolute configuration. The diastereoisomer 3a was attributed (RR/SS) or trans-isomer. The formation of compound 3 from Lapachol involves benzilic acid rearrangement reaction.

Kinnow mandarin (Citrus reticulata blanco) is the popular fruit crop in the world. In this study 12.5 % sodium dodecyl sulphate polyacryl amide gel electrophoresis (SDS-PAGE) method was used to observe comparative protein production pattern in different tissue culture stages of Kinnow mandarin. In this study embryogenic calli, non embryogenic calli, nucellar embryo, in vitro grown plant and seeds were used. In SDS gel total 31 protein bands were observed among them 9 or (29%) bands were polymorphic and 22 or (79.96%) were monomorphic with molecular weight ranging from 26 to 170 KDa of size. Two protein bands were similar among all tissue culture stages one was of 180 KDa and the other one between 72-55 KDa. Based on their banding pattern, similarity matrix with Jaccard’s coefficients was calculated and found 0.31 to 0.80. Dendrogram was constructed with Unweighted Pair Group Method with Arithmetic averages (UPGMA) which separated all bands into two main clusters. This comprised of seed and non embryogenic callus in one cluster and embryogenic callus, nucellar embryo in one group and in cluster with in vitro plant, respectively. It concludes that embryogenic callus and nucellar embryos have 80% similarity in their protein production profile, suggesting their similar properties for regeneration as both stages possess regenerative potential.

Oleanolic acid (3β-hydroxyolean-12-en-28-oic acid) belongs to pentacyclic triterpenoid compounds which are widely found in natural plants. Oleanolic acid and its derivatives possess several promising pharmacological activities. The chemical modifications made in the oleanane backbone mainly at carbons C3, C12 and C28 carboxylic acid, have led to a series of new synthetic oleanane triterpenoids. The Oleanolic acid derivatives at C-3 position exhibited the most potent activity. Here, a review of the advances in research on pharmacological activities and synthesis of Oleanolic acid derivatives at C-3 position are presented.

Essential oils from Artemisia nilagirica (Clarke) Pamp., Artemisia capillaris Thunb., Cymbopogon flexuosus (Nees ex Steud.) Watson, Hedychium spicatum Sm., Citrus limon (L.) Osbeck and Ocimum tenuiflorum L. were isolated to evaluate their antibacterial activity and to assess the synergistic effect of their mixture of equivalent amounts. The components of essential oils were elucidated by gas chromatography retention indices relative to n-alkanes and mass spectrometry. Among total characterised constituents, the major ones found in A. nilagirica, A. capillaries, C. flexuosus, H. spicatum, C. limon and O. sanctum were linalool (16.29%), capillene (42.06%), α -citral (28.08%), 1,8-cineole (30.84%), limonene (49.38%) and β -ocimene (22.80%), respectively. These oils and their formulation of equivalent amounts exhibited noteworthy activities against Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa and Escherichia coli. At a concentration of 100 μg/mL, all the oils and their formulation showed IZDs of 9-30 and 29-38 mm, respectively, whereas, MICs were recorded to 6.25-50 and 3.125 μg/mL, respectively. The study concludes that essential oils and their formulation exhibited strong activity against all bacterial species. The promising activity of novel formulation as compared to ampicillin is perhaps due to synergistic effect of its constituents, and the same could become a promising source of an antibiotic agent in near future.

The aim of this review paper is to summarize some marine natural sources (bacteria and fungi) known for their anti-inflammatory effects. We have collected data from MDPI, current contents, scientific research articles and journal publications. This review will give brief idea about the chemistry of novel marine compounds, mechanism of action, metabolites, biological sources of the compounds, synthesis of these marine natural products, as well as use of them in drug discovery and development. Different marine bacteria and fungi live in symbiosis with corals or sponges. Many actives have been isolated from these organisms. The quantity of actives obtained varies in different geographical and environmental conditions. These actives elucidate different mechanisms of action due to presence of different pharmacophore features in novel chemical templates. Efforts have been made to synthesize some structural analogs of isolated active anti-inflammatory compounds and SAR studies conducted. This review gives options for synthesis of new anti-inflammatory compounds thus expanding the chemical space in this category.