Natural Products Journal, The - Volume 6, Issue 2, 2016

The genus Rheum is a member of the family Polygonaceae. Rheum species, generally known as Rhubarb growing in high altitude, are important medicinal herbs containing secondary metabolites and grow in India, China, Korea, and Japan. Several chemical constituents from Rheum species are pharmacologically important. Besides being used as herbal medicine and also used in the vegetables and for making natural dyes. More than 250 constituents including anthraquinones (emodin, chrysophanol, physcion, aloe-emodin, and emodin glycosides), anthrones, flavonoids, acylglucosides, pyrones stilbene etc. are the major bioactives of rhubarb that exhibit several biological activities are used folk medicine for the treatment of fever, dysentery, blood coagulation, laxative, anticancer and also used in various skin diseases. This article is an attempt to highlight several of chemical constituents isolated from these species and their medicinal properties.

Background: A resurgent interest in the use of natural product based inhibitors against the influenza virus has resulted from the widespread resistance to current antiviral therapeutics among circulating strains. Natural products derived from food sources in particular, offer the benefit of a safer pharmacological profile and may offer broader health benefits. Objective: To identify new anthocyanins from black elderberry (Sambucus nigra) that will inhibit the function of influenza neuraminidase while avoiding complications associated with mutations in the active site of strains resistant to current inhibitors. Method: The mild solvent extraction process minimizes the exposure of the anthocyanins to non-acidic pH solutions, high temperature and pressure, and ambient light, in order to prevent their chemical transformation or degradation. Total anthocyanin yields are equivalent or better to those reported based on the recovery of cyanidin-3-O-glucoside. The characterization of additional anthocyanin components has been achieved by liquid chromatography coupled to electrospray ionization mass spectrometry (LC-ESI-MS) in conjunction with tandem mass spectrometry (MS/MS). Results: The results demonstrate an improved mild recovery method that has enabled the isolation and detection of previously unidentified minor anthocyanin components in elderberry of inhibitory potential against the influenza virus including prenylated cyanidin-3-O-sambubioside, prenylated and other derivatives of cyanidin-3-acetylrutinoside, and a type A proanthocyanin dimer of cyanidin-3-O-sambubioside. Conclusion: The improved recovery of anthocyanins from elderberries, under mild extraction conditions in a manner that preserves their structural integrity, and which yields a wider variety of previously unidentified compounds, should aid in their use and development in the treatment of influenza infections.

Eupatorium serotinum Michx. (late thoroughwort, Asteraceae) is a perennial herbaceous plant that is common to the eastern United States. The plant has diaphoretic effects, and has a folk remedy usage as a fever reducer. Relatively little is known about the chemistry of this plant. To better understand the chemistry of this plant and for the identification of taxonomic markers for the plant, we have isolated three sesquiterpenoids from Eupatorium serotinum. The compounds were identified by NMR and MS spectroscopic methods.

The present research focuses on the molecular docking analysis of the isolated compound from the seaweed “Sargassum wightii” on cancer specific HER2 or HER2/neu also known as CD340. The ethanol derived compounds capable of binding to HER2 receptor is implicated for the breast cancer. The crystal structure of the HER2 protein with the resolution of 1.63Ao (Pdb entry 4RJ3) collected from the pdb website (www.pdb). Missing alignments and the side chains are prepared to fit for the insilico analysis. Seven bioactive compounds isolated from the hydro-alcoholic mixture using GC-MS are docked against HER2 using Schrodinger 2013.1 (Glide version 5.9). The binding sites, glide score and the energy of the 7 compounds with the HER2 protein are compared. The isolated compounds with most negative glide score such as benzoic acid, 2-hydroxy-ethyl ester, methyl salicylate, diethyl phthalate and phytol exhibited efficient in inhibiting the HER2 receptor of breast cancer. The Pharmacokinetics and Pharmacodynamics (ADME) properties of the selected highest glide scored compounds are performed using QikProp 3.6 module from Schrodinger-Maestro software. The compounds were showed significant ADME properties in basic criteria of Molecular weight (MW), H-Bond donor, H-Bond acceptor and log P (O/W). The results of the study showed that the compounds of “Sargassum wightii” may be a good target for breast Cancer.

Lyophilized Acmella oleracea capitula, leaves and stems were extracted with methanol at 100 °C and 10 MPa (100 atm) pressure in a sealed container and analyzed by LC-HRMS and NMR. This solubilized 28.3% of the leaves, 24.7% of the stems and 31.1% of the capitula. The NMR spectra were dominated by signals due to the CHO and CH2O of carbohydrates. Spilanthol and other Nalkamides were present in the methanolic extracts at concentrations that were too low to enable their detection by NMR. In contrast, LC-HRMS was able to quantify spilanthol (deca-2E,6Z,8E-trienoic acid isobutylamide, syn. affinin, C14H23NO) and detect at least ten other N-alkamides as [M+H]+ ions with the following molecular formulas and m/z values: C13H17NO (1), C17H17NO (2), C15H19NO (3), C15H21NO (4), C16H23NO (5), C17H23NO (6), C14H25NO (7), C15H25NO (8), C14H21NO (9) and C16H25NO (10). The concentrations of spilanthol in the capitula, leaves and stems were 16.5, 0.344 and 0.241 mg/g dry weight. To confirm its presence by NMR, partial purification was required. So, a portion of the residues remaining after evaporating off the methanol were partitioned between chloroform and deionized water. The percentage of amphiphilic compounds in the capitula, leaves and stems were 7.69, 8.42 and 3.09% dry weight, respectively. NMR signals due to spilanthol were seen in their spectra.

Stevia Rebaudiana leaves have functional and sensory properties superior to those of many other high-potency sweeteners. Dental caries is an infectious microbiological disease that affects almost every human. There is a linear correlation of sugar consumption with dental caries in populations worldwide. Present invention was directed to design and develop Stevia based polyherbal formulation with enhanced performance in oral care as Stevia inhibits the growth of dental caries causing microorganisms. In the present study, twelve pure isolates grown on Snyder agar medium and five MTCC strains i.e. Streptococcus mutans, Staphylococcus aureus, Curvularia lunata, Escherichia coli and Bacillus subtilis were screened for antimicrobial activity through agar well diffusion method. Metabolites from plant leaves were extracted using six different solvents and investigated for phytochemical properties. Few cultures were found to be belonging to Staphylococcus species, Bacillus sp., Clostridium sp., Neisseria sp., and Escherichia. coli. On the basis of maximum zone of inhibition produced against cultures, diethyl ether extracts of plant were effective against bacteria and fungi, followed by petroleum ether and chloroform and finally minimum inhibitory concentration and minimum bactericidal concentration of extracts were performed. The phytochemical screening of different extracts of Stevia showed the presence of various secondary metabolites. Herbal formulation prepared in diethyl ether extract displayed significant bioactivity against all twelve isolated cultures and standard cultures. The study holds importance as one needs to be familiarized with alternatives to sugar and type of food products that are available with substitute sweetening agents, as we have the responsibility to reduce the incidence of dental caries by emphasizing the role of sugars in caries formation.

Imperatorin, Heraclenin and Auraptene were isolated from the fruit pulp of Aegle marmelos correa. The structure of these compounds was confirmed by spectroscopic and single X-ray analysis. Among them Heraclenin crystallized out in large from the fruit pulp oil without further purification by conventional chromatographic techniques. The anti-microbial activity was performed on Xanthomonas oryzae pv. Oryzae and Colletotrichum lindemuthianum.

A jelly prepared from Eugenia brasiliensis fruit pulp was developed and evaluated for its rheological and sensorial properties, as well as its color. The fruit pulps were acidic (0.29±0.03 g citric acid equiv•100g-1 pulp) and contained 95.29±0.03% water, soluble solids (5°Brix), proteins (0.27±0.17%), lipids (0.13±0.02%) and a relatively low energy content (35.16 kcal). Several minerals were quantified. Here are the amounts of some of the most important minerals that were found in 100g of pulp: calcium (19.8 mg), potassium (160 mg), magnesium (6.61 mg) copper (91.9 μg), chromiun (4.23 μg) and manganese (0.07 mg). Analysis of the rheological properties of the pulp showed that it did not follow any of the standard mathematical models: the Power Law, Ostwald-Waele and Herschell-Bulkley, but the jelly followed the Power Law model, with the behavior of a non-Newtonian fluid. The colors of the jellies were also evaluated using the standard parameters L*, a*, b*, C* e h°. The sensory analysis of the gel containing 0.3% pectin showed an acceptability index ranging from 83.66 to 91.11%. The index for the intention to buy the jelly was 83%. So, the jelly is a good option for using this under-appreciated fruit.

Usage of excipients from natural sources is now the most attractive research areas. Most of the synthetic polymers used in the formulation are detrimental to some extent for the human physiological system. Herbal substitute will be the best choice to minimize long term adverse effect. The purposes of repeated dose toxicity testing are to obtain information about biologic activity of chemicals. In the present study, repeated oral toxicity study of formulation containing metformin 1000mg and sitagliptin 50mg in Swiss albino rats was studied. Microwave assisted acrylamide grafted C. tora is used as a polymer in the formulation. Rats of both sexes from control and different dose groups (100, 200 and 400 mg/Kg body wt.) exhibited normal body weight gain throughout dosing period. Study protocol was prior approved by animal ethics committee. Combination treatment for 28 days, formulation did not show any significant features of haematological, behavioural, hepatotoxicity and nephrotoxicity in rats. Therefore it can be concluded that the combination using the grafted polymer is safe in these repeated doses in rats.