Evaluation of the activity of CYP2C19 in Gujrati and Marwadi subjects living in Mumbai (Bombay)

BACKGROUND: Inherited differences in the metabolism and disposition of drugs, and genetic polymorphisms in the targets of drug therapy (e.g., receptors), can greatly influence efficacy and toxicity of medications. Marked interethnic differences in CYP2C19 (a member of the cytochrome P-450 enzyme superfamily catalyzing phase I drug metabolism) which affects the metabolism of a number of clinically important drugs have been documented. The present study evaluated the activity of CYP2C19 in normal, healthy Gujrati and Marwadi subjects by phenotyping (a western Indian population). METHODS: All subjects received 20 mg of omeprazole, which was followed by blood collection at 3 hrs to estimate the metabolic ratio of omeprazole to 5-hydroxyomeprazole. The analysis was done by HPLC. RESULTS: It was seen that 10.36% of this population were poor metabolizers(PM) whereas 89.63% were extensive metabolizers(EM). CONCLUSION: A genotyping evaluation would better help in identifying population specific genotypes and thus help individualize drug therapy

Acanthus montanus: An experimental evaluation of the antimicrobial, anti-inflammatory and immunological properties of a traditional remedy for furuncles

<p>Abstract</p> <p>Background</p> <p><it>Acanthus montanus </it>(Nees) T. Anderson (Acanthaceae) is a shrub widespread in Africa, the Balkans, Romania, Greece and Eastern Mediterranean. It is used in African traditional medicine for the treatment of urogenital infections, urethral pain, endometritis, urinary disease, cystitis, leucorrhoea, aches and pains. In southeastern Nigeria, the root is popular and acclaimed highly effective in the treatment of furuncles. This study was undertaken to experimentally evaluate the antimicrobial and anti-inflammatory properties of the root extract as well as its effect on phagocytosis and specific cell-mediated immune response which may underlie the usefulness of the roots in treatment of furuncles.</p> <p>Methods</p> <p>The aqueous root extract (obtained by hot water maceration of the root powder) was studied for effects on the growth of clinically isolated strains of <it>Pseudomonas aeruginosa </it>and <it>Staphylococcus aureus</it>. The anti-inflammatory activity was investigated using acute topical edema of the mouse ear induced by xylene, acute paw edema induced by agar in rats, formaldehyde arthritis in rats, vascular permeability induced by acetic acid in mice and heat- and hypotonicity-induced haemolysis of ox red blood cells (RBCs). Also evaluated were the effects on <it>in vivo </it>leukocyte migration induced by agar, phagocytic activity of macrophages on <it>Candida albicans </it>and specific cell-mediated immune responses (delayed type hypersensitivity reaction (DTHR) induced by sheep red blood cell (SRBC)). The acute toxicity and lethality (LD₅₀) in mice and phytochemical constituents of the extract were also determined.</p> <p>Results</p> <p>The extract moderately inhibited the growth of the test organisms and significantly (<it>P </it>< 0.05) inhibited (57%) topical acute edema in the mouse ear. It significantly (<it>P </it>< 0.05) suppressed the development of acute edema of the rat paw in a non-dose-related manner and was not effective in inhibiting the global edematous response to formaldehyde arthritis. It also inhibited vascular permeability induced by acetic acid in mice and the haemolysis of ox RBCs induced by heat- and hypotonicity. The extract increased total leukocyte and neutrophil counts and caused a significant (<it>P </it>< 0.05) dose-related increase in the total number of macrophages at the 800 mg/kg dose. On phagocytic activity, the extract evoked a significant (<it>P </it>< 0.05) increase in the number of macrophages with ingested <it>C. albicans </it>at 800 mg/kg dose, and significantly (<it>P </it>< 0.05) inhibited DTHR in a dose-related manner. Phytochemical tests on the extract revealed an abundant presence of alkaloids and carbohydrates while saponins, glycosides, and terpenoids occurred in trace amounts. Acute toxicity test established an oral and intraperitoneal LD₅₀greater than 5,000 mg/kg.</p> <p>Conclusion</p> <p>The effectiveness of the root of <it>A. montanus </it>in the treatment of furuncles may largely derive from mobilization of leukocytes to the site of the infection and activation of phagocytic activity as well as suppression of exacerbated immune responses by its constituents. Antimicrobial and anti-inflammatory activities are likely contributory mechanisms. Phytochemical constituents such as alkaloids and carbohydrates may be responsible for these pharmacological activities.</p

A review on herbal antiasthmatics

In traditional systems of medicine, many plants have been documented to be useful for the treatment of various respiratory disorders including asthma. In the last two decades the use of medicinal plants and natural products has been increased dramatically all over the world. Current synthetic drugs used in pharmacotherapy of asthma are unable to act at all the stages and targets of asthma. However some herbal alternatives employed in asthma are proven to provide symptomatic relief and assist in the inhibition of disease progression also. The herbs have shown interesting results in various target specific biological activities such as bronchodilation, mast cell stabilization, anti-anaphylactic, anti-inflammatory, anti-spasmodic, anti-allergic, immunomodulatory and inhibition of mediators such as leukotrienes, lipoxygenase, cyclooxygenase, platelet activating, phosphodiesterase and cytokine, in the treatment of asthma. This paper is an attempt to classify these pharmacological and clinical findings based on their possible mechanism of action reported. It also signifies the need for development of polyherbal formulations containing various herbs acting at particular sites of the pathophysiological cascade of asthma for prophylaxis as well as for the treatment of asthma

Membrane stabilization as a mechanism of the anti-inflammatory activity of methanol extract of garden egg (<it>Solanum aethiopicum)</it>

<p>Abstract</p> <p>Background</p> <p>Some observations and reports show that people with high consumption of <it>Solanum aethiopicum</it> (African garden egg) have relief in arthritic pains and swelling. We aimed at assessing the effect of methanol extract of <it>Solanum aethiopicum</it> in experimentally induced inflammation using leukocyte mobilization and vascular permeability tests in rats and human red blood cell (HRBC) membrane stabilization as studies.</p> <p>Methods</p> <p>Twenty five (25) adult Wistar rats of either sex (120 g – 200 g) divided into five groups of five rats each were used for each of the animal models. Groups 2, 3 and 4 were administered varied doses of the extract (100, 200 and 400 mg/kg), while groups 1 (vehicle control) and 5 (treatment control) received normal saline and indomethacin (50 mg/kg) respectively. Vascular permeability was induced by the intra-peritoneal injection of 1 ml of acetic acid and monitored using 0.5 ml intravenous injection of 1% Evans blue solution. Leukocyte mobilization was induced by the intra-peritoneal injection of 0.5 ml of 3% agar suspension in normal saline. Heat and hypotonicity induced heamolysis of HRBC membrane was used to assess membrane stabilization.</p> <p>Results</p> <p>The methanol extracts of garden egg significantly and dose dependently reduced (p≤0.05) the acetic acid induced vascular permeability and agar induced leukocyte mobilization in rats. The percentage inhibitions of induced vascular permeability were 21 ± 3.39, 25 ±1.92 and 60 ± 3.81 for the 100, 200 and 400 mg/kg of the extract while the inhibitions of the agar induced leucocyte migration were 23 ± 2.17, 26 ± 1.58 and 32 ± 1.58 for the 100, 200 and 400 mg/kg of the extract respectively. The extract also, at doses of 100, 200, 400, 600 and 800 μg/ml significantly inhibited heat induced lysis of the human red cell membrane with values of 66.46 ± 2.89, 65.14 ± 4.58, 46.53 ± 2.52, 61.88 ± 4.51and 86.67 ± 3.06 respectively.</p> <p>Conclusions</p> <p>These results show that methanol extract of <it>Solanum aethiopicum</it> has anti-inflammatory properties and can reduce inflammatory injury and tissue damage.</p