Forskolin: upcoming antiglaucoma molecule.

Forskolin is the first pharmaceutical drug and product derived from a plant to be approved in India by the DCGI in 2006. Forskolin (7beta-acetoxy-8, 13-epoxy-1a, 6ß, 9a-trihydroxy-labd-14-en-11-one) is a diterpenoid isolated from plant Coleus forskohlii (Lamiaceae). It is a lipid-soluble compound that can penetrate cell membranes and stimulates the enzyme adenylate cyclase which, in turn, stimulates ciliary epithelium to activate cyclic adenosine monophosphate, which decreases intraocular pressure (IOP) by reducing aqueous humor inflow. The topical application of forskolin is capable of reducing IOP in rabbits, monkeys, and humans. In its drug interactions, forskolin may act synergistically with epinephrine, ephedrine and pseudoephedrine. Whereas the effects of anti-clotting medications like warfarin, clopidogre, aspirin, anoxaparin, etc., may be enhanced by forskolin. Forskolin is contraindicated in the medications for people with ulcers as forskolin may increase acid level. Forskolin has a very good shelf-life of five years. Recently, its Ophthalmic inserts and in situ gels for sustained and delayed-release drug delivery systems were tested in New Zealand Albino Rabbits for its antiglaucoma efficacy. This drug review explains Forskolin as a drug, its antiglaucoma potential and recent findings of forskolin as an antiglaucoma agent. The literature search method used for this review was different databases and search engines like PubMed, International Pharmaceutical Abstracts, Google, Medicinal and Aromatic Plants (MAPA).

Reversal of CRF- and stress-induced anorexia by an ayurvedic formulation

Trikatu churna is one of the commonly used Ayurvedic formulations in the traditional system of medicine in India for the treatment of agnimandya, i.e. anorexia. Trikatu contains equal amounts of finely powdered rhizomes of Zingiber officinale Roscoe (Zingiberaceae) and fruits of Piper longum L. and Piper nigrum L. (Piperaceae). The chief objective of the study was to determine the antianorectic effects of three drugs individually and to compare these effects with the effect of Trikatu. The activity of the drugs was studied after anorexia was induced in rats by (1) physical stress arising from immobilization for 60 min; (2) intraperitoneal injection of Escherichia coli lipopolysaccharide (LPS, 100 μg/kg body weight); and (3) intraperitoneal administration of fluoxetine (8 mg/kg body weight). Similar doses of the extracts were tested on freely feeding rats and on rats that had been deprived of food for 20 h. Corticotrophin-releasing factor (CRF, 0.3 μg/rat) can induce anxiogenic-like behavior and reduced food intake. This model was also studied, and the results were compared. The components of Trikatu churna failed to individually reverse the inhibition of feeding. In contrast, Trikatu churna pretreatment reversed stress-, fluoxetine- and CRF-induced anorexia. The study provides strong evidence of the synergistic action of Ayurvedic formulas and also proves the ability of Trikatu churna to reduce stress and CRF-induced anorexia.

Optimizing conditions for gallic acid extraction from Caesalpinia decapetala wood.

Caesalpinia decapetala is a wild plant found in the Sub-Himalayan tract and planted in hedges throughout in India. The bark of Caesalpinia decapetala is a rich source of tannins. It has been used in treatment of jaundice, stomach disorders and biliousness. The leaves and root are used as purgative and emmenagogue. The process described in this paper outline the extraction of gallic acid from Caesalpinia decapetala which is used as antioxidant and anti-inflammatory. Optimization of various solvent extraction parameters was performed to assess maximum yield of gallic acid from Caesalpinia decapetala wood. The extraction parameters optimized are solvent, temperature and time for extraction. Optimization was carried out by performing different sets of experiments. The most suitable conditions for extraction of gallic acid were found to be extraction at temperature (65-70(o)C), extraction time 48 hours and solvent composition Ethanol: Water (70:30). At these optimum extraction parameters the maximum yield of gallic acid obtained is 17.85%.

Diuretic activity of squamate mistletoe, Viscum angulatum.

Viscum angulatum Heyne ex DC (Viscaceae) is a leafless hemiparasitic shrub traditionally used in Asian countries for the treatment of hypertension. In the present study, the methanol extract of the whole plant was examined for diuretic activity in rats. The activity was evaluated using parameters such as urine volume after 5, 19, and 24 h and urine sodium, potassium, and chloride concentrations. The extract was further scrutinized for polyphenolic compounds and triterpenoids. The extract demonstrated a significant increase in and dose-dependent effect on urine excretion volume in comparison to the normal group in the tested range of 100-400 mg/kg. The extract demonstrated comparable saluretic and higher natriuretic activity (Na(+)/K(+)) compared to the furosemide treated group. However, the Cl(-)/Na(+) + K(+) ratio, which indicates carbonic anhydrase mediated activity, remained unaffected. HPLC and quantitative analysis of the extract revealed that polyphenolic compounds and the triterpenoid, oleanolic acid, are the major phytochemicals, and are proposed to be responsible for the observed diuretic effect. Oleanolic acid has been reported to possess diuretic activity with significant potassium loss in rats. In contrast to pure oleanolic acid, the extract demonstrated a valuable potassium-sparing effect. This suggests modulation of the diuretic effect of oleanolic acid by polyphenolics present in the extract. The observed dose-dependent potassium-sparing diuretic effect is a hereto unreported property of this plant.

Immunomodulatory activity of Toxicodendron pubescens in experimental models.

BACKGROUND: Toxicodendron pubescens is a botanical name of Rhus toxicodendron (Rhus tox). This plant is widely used in its homeopathically diluted form in the treatment of inflammatory and edematous conditions. In this study, various dilutions of Rhus tox including its crude form have been evaluated for their effects on immune response in the in vivo and in vitro experimental models. METHODS: Rhus tox in the form of mother tincture, 6cH, 30cH, 200cH and 1000cH dilutions was tested through in vivo models including sheep red blood cells (SRBCs) induced cellular and humoral immune response in C57/BL6 mice. The effects of Rhus tox dilutions were also evaluated in vitro on the functions of human polymorphonuclear (PMN) cells such as phagocytosis and intracellular killing of Candida albicans, chemotaxis, and reduction of nitroblue tetrazolium (NBT) dye. RESULTS: Rhus tox was found to intensify SRBCs induced antibody titer and delayed type hypersensitivity response in mice. Even higher dilutions such as 200cH and 1000cH were found to affect the immune response; however, the crude form, mother tincture, 6cH and 30cH dilutions revealed more potent effects than the 200cH and 1000cH dilutions. In in vitro assays, all the dilutions exerted stimulation of phagocytosis, candidacidal activity and chemotaxis of human PMN cells. The NBT dye reduction assay revealed that oxidative processes in the PMN cells are accelerated in the presence of Rhus tox. This study shows that Rhus tox possesses immunostimulatory activity in its crude form as well as in homeopathically diluted forms. These effects appeared to be concentration dependent as higher dilutions had less potent effects.

Antioxidant and cytotoxic activities of Caesalpinia pulcherrima wood.

Antioxidant and cytotoxic activities of the methanolic and aqueous extracts of Caesalpinia pulcherrima wood were studied in in vitro models. Both extracts exhibited strong antioxidant activity, as evidenced by the low IC50 values in both 1,1-diphenyl-2-picryl hydrazyl (DPPH), nitric oxide and superoxide scavenging methods; the values were found to be less or comparable to those of gallic acid, the standard used. To determine the cytotoxic activity, extracts were tested for toxic effects to brine shrimp larvae. In this assay, the methanolic extract had little effect, but aqueous extract was relatively toxic. The antioxidant and cytotoxic activities may be attributed to the total phenolic content in the wood.