Preparation and physicochemical evaluation of topical formulations of purified curcuminoids from Curcuma longa rhizome

Background and objectives: The purpose of this study was optimization of semisolid topical formulation from ethanol extract of turmeric and evaluation of rheological characterization and investigation of physicochemical control tests. Methods: The ethanolic extract was prepared with Soxhlet method and the compounds were isolated with silica gel column chromatography. Isolation of curcuminoids was accomplished by preparative HPLC.  The accelerated and real time stability tests for the formulations were investigated at 40±2 °C/70% RH for 90 days and 30±2° C/35%±5 RH for 12 month, respectively. Results: The yield of pure curcuminoids was 0.8%.The results of rheograms at 25° C showed pseudoplastic, plastic and pseudoplastic behavior for the ointment, cream and gel formulations respectively. The pH was measured by using  a  digital  type  of  pH  meter  by  dipping  the  glass electrical probe  for all of formulation, and the consequences exhibited PH values of 6.6, 6.8 and 6.9for the ointment, cream and gel, respectively. The results of cumulative release (µg/cm2) for ointment, cream and gel formulation achieved with dissolution media which contained buffer phosphate with pH 7.2 and 1% tween 20 after 24 h were 693.6, 648.5 and 650.5, respectively. Discussion:  The advantage of this method extraction compared to previously described methods, was utilizing safer solvent for extraction. The cumulative release of formulation and drug content during the physicochemical control tests was compared with commercial product and showed no significant different (p˃ 0.05).The formulations of this study showed functional and physical stability in the period of the study

Seasonal variations of Laurus nobilis L. leaves volatile oil components in Isfahan, Iran

Laurus nobilis L. (sweet laurel) is one of the volatile oil bearing plants of Lauraceae family. It is cultivated in different parts of Iran and its leaves and fruits have been used in food, cosmetics and pharmaceutical industries. There are a few reports about the effects of some environmental conditions on the quality and quantity of laurel volatiles. The goal of our work was to search the seasonal variations on the L. nobilis leaves volatile composition. The volatiles of four samples of the dried leaves of L. nobilis collected in March, June, September and December 2009 in Isfahan, Iran were prepared by using a Clevenger type apparatus for 3 hours and were analyzed by gas chromatography-mass spectroscopy. Twenty-nine, thirty-one, thirty-three and thirty-four components consisting 96.91%, 97.66%, 97.46% and 95.44% of the total compounds were identified of the volatiles obtained with yields of 1.1%, 1.5%, 1.4% and 0.8% (w/w), subsequently. The main compound was found to be 1,8-cineole (30.80-40.25%). Although twenty-seven out of thirty-six volatile components were similar in different seasons, there were some differences between other compounds of our four samples. While the essential oil composition of the March and June plant samples were characterized by presence of 1,8-cineole, δ-3-carene and camphor, the volatiles of September and December plant samples contained 1,8-cineole, camphene and sabinene. Some compounds like eugenol, methyl eugenol and α-terpenyl acetate were not affected apparently by seasonal changes

Echinophorin D a new polyacetylene from an edible plant, Echinophora platyloba aerial parts

Background and objectives: The aerial parts of Echinophora platyloba are added to cheese and yoghurt for flavoring. Besides, it is used for the treatment of flatulence and as air freshener. Despite several pharmacological studies on the plant, no attempt has been made to isolate non-volatile secondary metabolites from this plant. So, phytochemical investigation seems to be useful for better use of this plant in and to discover new compounds. Methods: Powdered aerial parts of the plant were extracted by Soxhlet apparatus with hexane, dichloromethane (DCM) and acetone. The concentrated acetone extract was fractionated using silica open column and mixture of heptane and ethyl acetate while DCM extract was fractionated by reverse phase column chromatography on RP-18 sorbent using mixture of methanol and water as solvent system with decreasing polarity. All subfractions were analysed by 1H- NMR, COSY, HSQC, HMBC and 13C-NMR. Results: After column chromatography and HPLC purification of DCM extract one new polyacetylene compound called echinophorin D was obtained and one fatty acid (coriolic acid) and one esteric polyacetylene (echinophorin B) were isolated and identified from the acetone extract. Conclusion: Due to the isolation of coriolic acid for the first time from this genus and the role of this fatty acid in inflammatory processes and anticancer activity as well as isolating polyacetylene compounds which have antioxidant and anti-tomur activity, this plant can be used as a source for compounds with antioxidant and anticancer effects

Acute and subchronic toxicological evaluation of Echinophora platyloba DC (Apiaceae) total extract in Wistar rats

OBJECTIVE: Echinophora platyloba DC is a widely used herbal medicine and food seasoning in Iran. It is claimed to exert antimicrobial, antifungal, and antispasmodic effects. Despite the prevalent use of this plant as a food and medicine, there are no reports on its possible toxic effects. To evaluate the safety of E. platyloba, we tested its acute and sub-chronic toxicity in male and female Wistar rats. METHODS: Rats were orally treated with four different single doses of E. platyloba total extract and screened for signs of toxicity two weeks after administration. In the sub-chronic toxicity study, E. platyloba was administered for 45 days. Mortality, clinical signs, body weight changes, hematological and biochemical parameters, gross findings, organ weights, and histological markers were monitored during the study. RESULTS: We found no mortality and no abnormality in clinical signs, body weight, or necropsy findings in any of the animals in the acute study. The results of the subchronic study showed no significant difference in hematological parameters in either sex. There was a significant increase in lactate dehydrogenase in the female groups. A significant increase in the relative lung weight of female rats was noted at 500 mg/kg. Histopathological examinations revealed intra-alveolar hemorrhage in the male rats (500 mg/kg). In the females, congestion of the alveolar capillaries (at 500 mg/kg) and liver bridging necrosis (at 200 mg/kg) were significantly increased. CONCLUSION: The no observed adverse effect level of E. platyloba was determined to be 200 and 50 mg/kg for male and female rats, respectively

Grandivittin as a natural minor groove binder extracted from Ferulago macrocarpa to ct-DNA, experimental and in silico analysis

Ferulago macrocarpa (Fenzl) Boiss., is an endemic medicinal herb of Iran. In this study a dihydrofuranocoumarin called grandivittin (GRA) was separate and purified from Ferulago macrocarpa (Fenzl) Boiss, and characterized by 1H NMR and Mass spectroscopic methods. The electrochemical behavior of GRA was evaluated by cyclic voltammetry (CV). The interaction of GRA with calf thymus double strand deoxyribonucleic acid (ct-DNA), was evaluated by CV, differential pulse voltammetry (DPV), fluorescence, UV�Vis, FT-IR and molecular modeling methods. The thermodynamic parameters of GRA-DNA complex were measured and reported as: �H = 15.04 kJ mol�1, �S = 105.54 J mol�1 and �G = �15.62 kJ mol�1. Docking simulation was performed to investigate the probable binding mode of GRA to various DNA, too. The polymerase extension study was performed using real-time PCR to confirm the inhibitory effect of GRA on polymerase extension activity as a mirror of binding to ct-DNA. However, all data showed that the grooves binding especially minor groove between GRA and ct-DNA is more predominant rather than other binding modes. © 2016 Elsevier Ireland Lt

Mechanistic in vitro evaluation of Prosopis farcta roots as an antidiabetic folk medicinal plant

Background and objectives: Prosopis farcta has been used as a traditional herbal medicine for treating diabetes mellitus.The aim of this study was investigating the antidiabetic mechanisms of infusion extract of P. farcta and discovering the active extract for the first time. Methods: Six different extracts of P. farcta were prepared using five different solvents [ethanol, n-hexane, acetone, ethanol: water (1:1 v/v), and water]. Cytotoxicity and cell proliferation assays were performed on mouse pancreatic β-cells (β-TC3) using the MTT method. The effects of P. farcta on glucose metabolism (in HepG-2 hepatocellular carcinoma cell line) were evaluated. The protective effects of various P. farcta extracts on cytotoxicity, mitochondrial membrane potential (MMP), and streptozotocin-induced apoptosis in β-TC3 cells were investigated. Results: P. farcta did not affect the viability of β-TC3 and HepG-2 cells up to 0.5 mg/ml. Infusion (INF) was the only extract which could protect cells against STZ. The proliferation results showed P. farcta extract did not increase proliferation in β-TC3 cell line compare to control. Conclusion: Only INF attenuated the death and apoptosis induced by STZ in β-TC3 cells. It could exert a significant glucose-lowering effect

Isolation and purification of sesquiterpene coumarins from Ferula assa-foetida and their in vitro interaction study with DNA

Background and objectives: Interaction of compounds with ct-DNA can affect the replication, protein synthesis and cell division. Different species of the genus Ferula (Apiaceae) have shown various biomedical applications for many centuries. Biological features of this genus such as cytotoxicity, antibacterial, antiviral, P-glycoprotein (P-gp) inhibitory and antiinflammatory activity have been attributed to sesquiterpene coumarins. Consequently, binding studies of sesquiterpen coumarin with ct-DNA are useful for the understanding of the reaction mechanism and providing guidance for the application and design of new and more efficient drugs targeted to DNA. Interaction of galbanic acid (GA) with ct-DNA, was evaluated by cyclic voltammetry (CV), diggerential pulse voltammetry (DPV), enhancement fluorescence, UV-VIS and FT-IR spectroscopy. Methods: The oleo gum-resin of Ferula assa-foetida was collected and dried in spring. Hexane extract of gum was prepared and defatted. Several coumarins were purified using normal open and preparative column and high performance liquid chromatographic methods and the structures were elucidated. GA is one of constituents isolated and binding interaction with ct-DNA was studied by CV, DPV, fluorescence, UV-Vis, FT-IR and spectroscopy.  Results: GA bears two cathodic peaks. The cathodic peaks I and II may correspond to the reduction of the alkene groups (-C3=C4- and –C6=C11-) at the electrode surface, respectively with average binding site size of 1.7. Conclusion: Binding of GA with ct-DNA caused significance chances in electrochemical and spectral characteristics of GA confirming the interaction mode of GA with ct-DNA in partial intercalation via DNA groove mode

Macrocyclic diterpenoids from the Iranian plant Euphorbia bungei Boiss.

An acetone extract from the aerial parts of Euphorbia bungei afforded three new (2, 3 and 5) and one known (4) macrocyclic diterpenoids. Several cycloartane triterpenoids were also obtained, two of which (6a and 6b) were assayed for antiviral effects. The structures of all new compounds were elucidated using modern spectroscopic methods including 2D NMR and HRMS