Natural Products Journal, The - Volume 7, Issue 1, 2017

The horn of the saiga antelope is often used in Traditional Chinese medicine (TCM). Its “popular” name in Chinese is ‘Lin Yan Jiao’ and the pharmaceutical name is Cornu Antelopis. It is as famous and valuable as musk, pilose antler (Lurong) and rhino horn, the most-renowned medicinal materials of animal origin used in TCM. However, the saiga has also joined the rhinoceros on the list of endangered species. The presented review briefly overviews an existing knowledge regarding the biologically active compounds at saiga horn. The main beneficial effects of the horn, which could be described in scientific terms, are mostly antipyretic and antiulcerative. Despite some indication of its efficacy, no specific compound from the saiga horn has yet been isolated or scientifically described. It can be assumed that the amino acid composition of the horns of various animals: the buffalo, the saiga, the ox and the goat is almost same in terms of nature and composition when they differ only in their ratios. The similarity of amino acid and peptide compounds has confirmed the similarity of anti-inflammatory and antiulcerative physiological actions. Thus, we can talk about the interchanging ability of horns. If someone believes in the positive influence of animal horns on human health, we can thoroughly recommend the use of horns from animals that are more abundant (such as water buffalo, rams) as compared to the critically endangered species such as saiga (or rhinoceros) with possible similar effect on the organism. There are also some evidences that the antipyretic effect is not strictly dependent on the origin of the horn and might be connected to the herbal substances prescribed and used in the preparation of Chinese medicine. However, only some thorough scientific research on TCM could provide new results that can identify the most active components of the extract and confirm our assumptions about the beneficial effects of extracts or powders of the horns.

Background: Two-Dimensional Electrophoresis (2-DE) is currently the most common technology used for proteome analysis. The greatest challenge to achieve a well resolved 2-DE map is the protein extract preparation. Evergreen and thick leaves are recalcitrant tissues containing extremely high levels of interfering molecules such as oxidative enzymes, phenolic compounds (simple phenols, flavonoids, condensed tannins, lignin), carbohydrates, nucleic acids and lipids which make the 2-DE analysis problematic. Objective: In the present study, we developed an easy-to-use protocol for optimal olive leaf proteins extraction in high phenolic content condition. Methods: To establish an effective protein extraction protocol, suitable for successive 2-DE processing, the three following protein extraction methods were tested: Phenol, TCA/Acetone-Phenol/SDS and TCA/Acetone-Methanol-Phenol/SDS. Results: Protein spots were undetectable in the 2-DE gel image using phenol extraction method. TCA/Acetone-Methanol-Phenol/SDS protocol showed a higher protein yield, a greater spot number, better spot resolution, higher spot intensities in the high and low molecular weight and minimal streaking on 2-DE gel than the classical TCA/Acetone-Phenol/SDS method. Conclusion: TCA/Acetone-Methanol-Phenol/SDS protocol proved to be the most suitable method to extract proteins from a green recalcitrant phenolic rich tissue as olive leaf (Olea europea L.). Our implemented protocol is expected to be applicable to other recalcitrant plant tissues.

Background: Colorectal carcinoma is the fourth most common internal malignancy; it is second only to carcinoma of the lung as a cause of carcinoma death. 6-Mercaptopurine (6-MP) is a drug of choice in the treatment of Crohn's disease, ulcerative colitis and colorectal cancer. The drug shows irritation on gastric exposure. It has poor bioavailability with half life less than 2 h. Targeted delivery of 6-MP will provide an effective and safe therapy for colon diseases. Objective: Objective of the present work was to design, develop and optimize colon targeted delivery with help of polymers guar gum and HPMC K100 for 6-Mercaptopurine, which will act as site targeted delivery for treatment of colon diseases. Method: Targeted delivery was prepared by press/compression coating technique. Preliminary study had shown 4:1 ratio of microcrystalline cellulose and croscarmellose sodium was optimum for core tablet. 32 full factorial design was applied. Amount of guar gum and hydroxypropyl methylcellulose (HPMC K100) were employed as independent variables while responses evaluated were hardness and swelling index at 5 h. Results: Optimized GD batch contain 26.32% and 73.68% w/w of total polymer weight of guar gum and HPMC K100, respectively. This prevented the release of drug in the gastric region and allowed drug release ≥90% in colonic region after ≥8 h. In-vivo x-ray imaging placebo study revealed that, tablet was observed in colonic part at 5h and disintegrated at ~ 8 h. Optimized formulation was found to be physically and chemically stable. Conclusion: Optimize GD batch had shown retardation of the drug release in upper GI tract which will enhance therapeutic activity of the drug at the site. This system hence will act as a potential site and time controlled colon targeted delivery.

Background: Orthosiphon stamineus is a medicinal herb rich in caffeic acid derivatives. Rosmarinic acid is one of the caffeic acid-based phytochemicals which is also well-known for its antioxidant and anti-inflammatory properties. Objective: This study was focused on the preparation of rosmarinic acid-rich fraction to enhance the antioxidant capacity of O. stamineus. Method: The rosmarinic acid-rich fraction was prepared by using an integrated technique of reflux extraction and column chromatography. The concentration of ethanol was varied from 0-100 %v/v to optimize the yield of rosmarinic acid in the fraction. Results: This technique increased the rosmarinic acid content from 0.14 %w/w in the dried whole plant to 1.9 %w/w in the crude extract till 4.1 %w/w in the 80 %v/v ethanol fraction. The consecutive elution of packed column also produced eupatorin-rich fraction from 0.0008 %w/w in the dried whole plant to 0.17 %w/w in the crude extract and 0.5 %w/w in the 40 %v/v ethanol fraction. The increment of rosmarinic acid content enhanced the radical scavenging activity in the fractions. The IC50 was significantly decreased from 2424 to 37.7 ppm for the crude extract and its 80 %v/v ethanol fraction, respectively. Therefore, the increase of rosmarinic acid content also increased the antioxidant capacity of the plant extract. Conclusion: This rosmarinic acid-rich fraction could be further developed into various useful herbal products for the benefits of mankind.

Background: Gasoline is a mixture of several hydrocarbons and additives and is associated with numerous adverse health effects including renal function impairment. The aim of this study was to evaluate the ameliorative effect of Cymbopogon citratus on gasoline vapour-induced renal function impairment. Methods: Seventy-two mature female Wistar albino rats were divided in-to six groups (n = 12 per group). Group (G1) was the control group; G2 was exposed to gasoline vapour alone; G3, G4, and G5 were exposed to gasoline vapour and co-administered 500 mg/kg, 1000 mg/kg, and 1500 mg/kg C. citratus, respectively; and G6 was exposed to gasoline vapour and co-administered 200 mg/kg vitamin C. After 35 days of treatment, the animals were sacrificed, and blood was obtained for biochemical analysis. Nephrotoxicity was evaluated by measuring serum levels of the renal biochemical parameters creatinine (Cr), urea (Ur), glucose (Glu), uric acid (UA), sodium (Na+), potassium (K+), bicarbonate (HCO3 -), and chloride (Cl-). Gasoline vapour-induced nephrotoxicity was confirmed by histopathological examination of the kidney sections. Results: Results showed significant (p<0.05) increases in the levels of serum renal biochemical and hismorphological profile in animals exposed to gasoline alone (G2) compared to the levels in control animals (G1). However, when Cymbopogon citratus decoction was co-administered, these increases in renal parameters were dose-dependently reversed. Similar changes were observed in vitamin Ctreated animals. Conclusion: The results suggest the ameliorative effect of Cymbopogon citratus on gasoline vapourinduced nephrotoxicity. The ameliorative effect was evident through improvement of the biochemical and histopathological markers of nephrotoxicity. The changes observed in malonaldehyde suggest that the ameliorative effect of Cymbopogon citratus might be attributable to the antioxidant activity of its bioactive constituents.

Aim: The aim of the study was to investigate hypoglycemic and hypolipidemic activities of aqueous extracts of Centaurium erythraea (CnE) and Ajuga iva (AjI) after daily oral dosing for 60 days in a rodent model of metabolic syndrome (MetS). Materials and Methods: Meriones shawi rats were fed a high caloric diet and forced to limited physical activity for 180 days to develop obesity, hyperglycemia and hyperlipidemia (OHH) as a model of MetS. After administration of single oral doses of test substances [extracts of CnE (250 mg/kg) and AjI (150 mg/kg), and reference drug [glibenclamide (GLB; 3 mg/kg)] to OHH rats, plasma levels of glucose, insulin, Total Cholesterol (TC), and Triglycerides (TG) were measured. In the sub-chronic study, the effect of daily oral dosing of test substances for 60 days to OHH rats, on Body Weight (BW), plasma glucose, insulin, TC, Low Density Lipoprotein (LDL)-cholesterol, High Density Lipoprotein (HDL)-cholesterol, TG, and free fatty acids were determined; insulin resistance (IR as HOMA-IR and QUICKI) and atherosclerotic index were calculated. Results and Conclusion: Meriones shawi rats developed OHH, hyperinsulinemia, IR and dyslipidemia- typical components of MetS. Single doses of test substances decreased only hyperglycemia. In the sub-chronic study, the test substances reduced plasma glucose, insulin, TC and LDL-cholesterol, as well as HOMA-IR and atherosclerotic index (AjI-extract > CnE-extract > GLB); plasma level of TG decreased with AjI only. These two plants may have the potential to be used therapeutically in the treatment of diabetes and possibly MetS, since, previous toxicological studies have shown a wide margin of safety for AjI and CnE.

Background: The umê (Prunus mume Siebold et Zucc.) or Chinese plum is used to prepare many food products and is used in traditional medicine. Methods: In this study, 26 clones grown in the Jundiaí do Centro de Frutas do Instituto Agronômico (IAC), in São Paulo, Brazil were analyzed. The fruits from each clone were placed in polystyrene trays, wrapped in polyvinyl chloride film and stored at 8 oC for 21 days. Portions of each sample were collected every three days and analyzed for weight loss and yield of pulp, as well as ascorbic acid, total soluble solids, titratable acidity, pH and colors of the pulp and peel. Results: The results were submitted to principal component analysis by dividing the clones into four groups. Clones 6 and 18 produced the most pulp, while clone 3 had the lowest respiratory activity. Clones 13 and 15 had intermediate respiratory activity when compared to the others. However, they did not lose as much weight during storage. Clones 15 and 1 had the largest concentration of ascorbic acid. Conclusion: These results can be used to select the best clones for each commercial application.

Background: Coriander, curry leaf and wild mint are among the most popular spices, and well known for their nutraceutical and Essential Oils (EOs) bearing properties. Objective: The present study aims to estimate total phenolic content, proline content, free radical scavenging activity, and volatile composition of the fresh leaves of coriander, curry leaf and wild mint. Method: A modified Folin-Ciocalteu method was used to estimate the total phenolic content and proline content, whereas 2,2-diphenyl-1-picrylhydrazyl (DPPH), and ferric ion reducing antioxidant power assay (FRAP) methods were used to determine the free radical scavenging activity. EOs were extracted through hydro-distillation method and subjected to GC-MS to identify their components. Results: Curry leaf was found to have highest total phenolic content (70.12 mg GAE/g), followed by wild mint (29.04 mg GAE/g) and coriander (24.02 mg GAE/g), whereas the uppermost proline content was obtained in curry leaf (453 mg/g), followed by mint (402 mg/g) and coriander (397 mg/g). All the extracts showed remarkable free-radical scavenging activity with EC 50 values of 56.38 mg/100 g for curry leaf, 50.55 mg/100 g for wild mint and 49.89 mg/100 g for coriander. trans 2- Dodecenal (17%), 2-methylenecyclopentanol (9%), dodecanal (8%), cyclooctane (8%), 9-tetradecenal (8%) and decanal (8%) were found to be the major components in coriander oil. The wild mint EO contained menthol (52%), limonene (11%) and trans-dihydrocarvone (5%) as main components, whereas caryophyllene (19%), β -panasinsene (16%) and caryophyllene oxide (9%) were the principal constituents of curry leaf EO. Conclusion: The study concluded that coriander, curry leaf and wild mint are the rich source of antioxidants, and phenolics contents, and thus, could be used as potent nutraceutical agents in daily foods. Moreover, the EOs obtained from these spices contained various oxygenated compounds which might be useful for food and pharmaceutical industries.

Background: Persimmons of the Rama Forte variety are well-accepted in the market, but the harvest season is short. The use of post-harvest treatment, such as UV-C radiation can extend the shelf life of the fruits. So, the ability of UV-C radiation and refrigeration to preserve these persimmons was studied. Methods: The fruits were harvested manually while their peels were yellow and then exposed to UV-C for 0, 5, 10, 15 and 20 min, placed in polystyrene bags and stored at 7±1ºC and 85±5% relative humidity. Results: The loss of mass did not exceed 0.5% for any treatment. The peak respiratory activity occurred on the 5th day, but the production of CO2 was lower (50.2 mL of CO2 Kg-1 h-1) for the fruits that were exposed to UV-C for 10 min. The pH, soluble solids, titratable acidity and color did not show significant differences between different methods of post-harvest treatment. On the other hand, the concentrations of total phenolics, anthocyanins and carotenoids decreased after the fruits were irradiated with UV-C light. Conclusion: The loss of mass did not exceed 0.5% for any treatment. The peak respiratory activity occurred on the 5th day, but the production of CO2 was lower (50.2 mL of CO2 Kg-1 h-1) for the fruits that were exposed to UV-C for 10 min. The pH, soluble solids, titratable acidity and color did not show significant differences between different methods of post-harvest treatment. On the other hand, the concentrations of total phenolics, anthocyanins and carotenoids decreased after the fruits were irradiated with UV-C light.