Phenolic contents, elemental analysis, antioxidant and lipoxygenase inhibitory activities of Zanthoxylum armatum DC fruit, leaves and bark extracts.

Zanthoxylum armatum (DC) is a traditional spice and important herb used in Asia as a part of food and household medicine for the treatment of various conditions. The present study was designed to investigate in vitro for phenolic/flavonoid contents, antioxidant activities, lipoxygenase inhibitory activity, minerals and heavy-metal contents. The leaves, bark and fruit of Zanthoxylum armatum were extracted with organic solvent and evaluated for phenolic contents (Folin-Chiocalteu method), for flavonoids contents (colorimetric method), for in vitro antioxidant assays (DPPH and FRAP), lipoxygenase inhibitory activity (5-LOX assay), mineral contents (atomic absorption), and for heavy-metal contaminants (atomic absorption). The fruit contained the highest phenolic (25.6±1.2mg GAE/g) and flavonoid (26.3±1.4mg QE/g) contents and therefore, exhibited the most effective antioxidant properties in DPPH (88.5±0.9% inhibition) and FRAP (94.21±3.2% inhibition) assays. The extracts also inhibited the LOX enzyme, and the fruit showed more inhibition (63.8±1.2 %) as compared with the leaves and bark. Z. armatum contain valuable minerals and fortified with magnesium (4.948±0.2, 3.07±0.03 and 3.53±0.12) and potassium (0.19±0.011, 1.91±0.003, and 1.90±0.05) for leaves, fruit, and bark, respectively. The chemical profiling for heavy metals showed that their concentrations were within permissible limits. The data suggest that Z. armatum is a safe and valuable natural agent with functional properties for food and pharmaceutical industries.

Zanthoxylum armatum DC extracts from fruit, bark and leaf induce hypolipidemic and hypoglycemic effects in mice- in vivo and in vitro study.

BACKGROUND: Zanthoxylum armatum DC is an important medicinal plant of south East Asia, and has been used to treat various ailments in traditional medicine including diabetes. This study investigated the in vitro and in vivo antidiabetic and biochemical effects of extracts of Z. armatum in mice. METHOD: The extracts of fruit, bark and leaf from Z. armatum were tested for α-glucosidase inhibition activity. Albino mice of either sex weighing (26-30 g) assigned into groups. Diabetes was induced by IP injection of alloxan monohydrate (150 mg/kg). The extracts (500 mg/kg) and standard (Glibenclamide 10 mg/kg) were administered to mice for 15 days. Serum biochemical parameters were monitored for the period of study. RESULTS: The leaves and bark extracts showed maximum α-glucosidase inhibition (96.61 ± 2.13 and 93.58 ± 2.31% respectively). The extracts treated and the standard treated groups showed significant decrease in the fasting blood glucose levels compared to diabetic control. The effect was more pronounced in mice treated with leaves extract. In the in vivo studies body weights of diabetic mice treated with Z. armatum extracts and the standard did not reduced to extent as observed in diabetic control and this difference was significant (p < 0.05). There was a significance (p < 0.001) improvement in blood hemoglobin, urea, creatinine, cholesterol, and triglycerides of the extracts treated diabetic mice. The extracts showed hypolipidemic effect by reducing the LDL level. The extracts produced no prominent changes in proteins levels. CONCLUSION: It can be concluded that Z. armatum extracts showed excellent antidiabetic potential in vivo and in vitro and could be considered for further appraisal in clinical assessment and drug development.

Gaultheria trichophylla (Royle): a source of minerals and biologically active molecules, its antioxidant and anti-lipoxygenase activities.

BACKGROUND: Gaultheria trichophylla (Royle) is used as food and for treating many ailments in folk medicine especially against inflammation. The purpose of this in vitro study was to evaluate the ability of extracts of G. trichophylla as anti-oxidant and anti-inflammatory agent and for its mineral contents. METHODS: Powdered plant material (100 g) was extracted with 100 ml each of methanol, chloroform, and n-hexane using soxhlet extractor. Antioxidant activity of methanol extract was assessed by DPPH radical scavenging and FRAP assays. Determination of enzyme inhibition activity was determined using 5-LOX inhibitory activity. Total phenolic and flavonoids contents were measured by Folin-Chicalteu and colorimeteric methods respectively. Minerals and heavy metals contents were determined using Atomic absorption spectrophotometer. Qualitative HPLC analysis were performed using some standard phenolic compounds. RESULTS: The highest phenolic (17.5 ± 2.5 mg GA equivalent/g) and flavonoids (41.3 ± 0.1 mg QE equivalent/g) concentrations were found in methanol extract, which also showed more scavenging activity of 1, 1-diphenyl-2-picrylhydrazyl and ferrous reducing power with IC50 = 81.2 ± 0.2 and IC50 = 11.2 ± 0.1 µg/ml, respectively. The methanol and chloroform extracts showed best inhibition of 5-lipoxygenase enzyme with 90.5 ± 0.7% and 66.9 ± 0.1% at 0.5 mg/ml, respectively. G. trichophylla extract was also evaluated for mineral contents (K, Na, Ca, Mg, Fe, and Cu), and for chemical profiling of heavy metals (Cr, Pb, Cd, Co, Zn, Ni and Hg). CONCLUSION: Our current findings suggest that this plant is good source of minerals and concentration of all heavy metals were within permissible limits. The results revealed that this ignored plant has great pharmaceutical and nutraceutical potential.

Gut modulatory and butyrylcholinesterase inhibitory activities of Gaultheria trichophylla.

CONTEXT: Gaultheria trichophylla Royle (Ericaceae) and related species have been used in the traditional system of medicine for the treatment of diarrhoea, pain and inflammation. OBJECTIVE: The present investigation explores G. trichophylla for its potential activity in hyperactive gut disorders. MATERIALS AND METHODS: Antidiarrheal activity was evaluated on castor oil induced diarrhoea in mice with reference to standard drug verapamil. Gut modulatory activity was performed on isolated jejunum tissue preparations on spontaneous and high potassium induced contractions. Butyrylcholinesterase (BChE) inhibitory activity was performed with an in vitro study. Extract was tested for toxicity in mice. RESULTS: In the in vivo studies, the methanol extract of G. trichophylla and verapamil significantly (p < 0.05, 0.01, 0.001) inhibited the frequency of defecation as well as wetting of faeces when compared with the negative control. The methanol (Gt. MeOH) extract of G. trichophylla caused a dose-dependent inhibitory effect on spontaneous contractions in isolated rabbit jejunum preparations and exhibited a partial inhibitory effect against high K+ (80 mM) induced precontractions. Gt. MeOH shifted the Ca2+ concentration-response curves (CRCs) to the right, suggesting calcium channel blocking like constituents. In an in vitro assay Gt. MeOH inhibited BChE enzyme with an IC50 values of 35.52 ± 1.17 µg/mL. The extract showed no toxicity in mice at the dose of 3 g/kg. DISCUSSION AND CONCLUSION: This study provides evidence that G. trichophylla possesses combinations of inhibitory and stimulatory effects mediated through possible cholinergic and less potent calcium blocking constituents, respectively. The latter may be responsible for the antidiarrheal effect.

Antihaemorrhagic potentials of Fagonia cretica against Naja naja karachiensis (black Pakistan cobra) venom.

Plants have been extensively used as a remedy for the treatment of snake bites. The aim of this study was to determine the antivenom potentials of methanolic extract from the aerial parts (leaves and twigs) of Fagonia cretica L. on a haemorrhage induced by venom from Naja naja karachiensis. The haemorrhagic response of venom was dose dependent from 0.1 to 4.0 µg per 1.5 µL phosphate buffer saline (PBS) on vitelline veins of fertilised hens' eggs in their shells. The extract effectively eliminated and neutralised, in a dose-dependent manner, the haemorrhagic activity of snake venom. The minimum effective neutralising dose of F. cretica extract was found to be 15 µg per 1.5 µL PBS. The extract possesses potentials as haemorrhagic inhibitor against snake venom compared to the standard antiserum and various plants reported in the literature. This study also provides a scientific base for the use of F. cretica in traditional medicine for the treatment of snake bite.

Anti-tumor 12-deoxyphorbol esters from Euphorbia cornigera.

Nine (1-8 and 10) new and two (9 and 11) known compounds have been isolated from roots of Euphorbia cornigera Boiss. Their structure and relative stereochemistry were acquired through NMR ((1)H, (13)C, COSY-45, HOHAHA, HMQC, HMBC, NOE and HMBC) spectroscopic measurements. Compounds 1-10 were identified as diesters of 13,20-O-diacyl and 11 as 13-O-acetyl of 12-deoxyphorbol. Cytotoxic activity of the compounds was investigated on human KB cells by reduction of MTT. Compounds 8-10 displayed IC(50) of 0.8, 0.5, and 1.0 microg mL(-1), respectively, whereas the activity of rest of the compounds (1-7) was either very low or (11) zero even up to 1000 microg mL(-1). The inhibition of DNA synthesis through Trypan blue exclusion and Brd-U assay was investigation to figure out the role of compounds 8-10 and concluded that these were responsible for the death of KB cells. Significant correlation has been found between the cytotoxicity and DNA cross-link and DNA strand-break formation.