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Pitaya is a cactaceae originally from Tropical and Subtropical America which belongs to the exotic fruit group, little explored to date by the food and pharmaceutical industries. The objective of the present study was to evaluate the chemical and physical-chemical properties, antioxidant activity and the fatty acid profile of the red pitaya fruit (pulp and peel) [Hylocereus undatus (Haw.) Britton & Rose], grown in Brazil. These analyses have shown that pitaya pulp has high moisture content (86.03%) and low lipid (0.16%) and protein (2.27%) content, which ensures a low fruit calorie value (53.68%). Among the highlighted minerals are potassium (3.090 mg / 100 g), manganese (2.230 mg / 100 g), chromium (1.250 mg / 100 g), sodium (0.140 mg / 100 g), calcium (0.040 mg / 100 g) and, at lower concentrations, phosphorus (0.003 mg / 100 g). On the other hand, the antioxidant activity of pitaya pulp (1266.3 μg mL–1) was lower than in the pitaya peel (445.2 μg mL–1). In the fatty portion of the fruit, we verified that the predominant fatty acid is linoleic acid (50.869% of total fatty acids in the fruit), followed by oleic acid (21.551%) and palmitic acid (12.632%). The antioxidant potential and the chemical properties of pitaya fruit can contribute to maintaining a healthy diet.

Methemoglobinemia is an altered state of haemoglobin that leads to impaired oxygen delivery to the body tissues. Deliberate ingestion of certain herbicides may lead to this condition. Modern herbicides are often synthetic mimics of natural plant hormones that interfere with growth of the target plants. These modern herbicides act by various mechanisms some of them being Acetyl co-enzyme A carboxylase inhibition, aceto lactate synthase inhibition, photosystem II inhibition, 4-hydroxy phenyl pyruvate dioxygenase inhibition and so on. We report a case of Methemoglobinemia after deliberate ingestion of an herbicide marketed to be safe and containing only biological extracts and filters. The patient was treated with ascorbic acid successfully. Our paper emphasizes the use of ascorbic acid as an alternative method in the treatment of Methemoglobinemia. Ascorbic acid is the main stay of treatment in patients with G6PD deficiency.

Sitagliptin (STG), a drug for treating Type Ii Diabetes Mellitus (T2DM), has been associated with severe joint pain in some patients. In this paper the metabolic profile of the drug has been investigated in order to determine metabolism and formation of reactive compounds which may contribute to this adverse effect. Metabolism of STG was investigated in vitro by incubation with freshly isolated Sprague-Dawley rat hepatocytes, to characterize Phase I and II metabolites, and the reaction mixture analysed on a zwitter ionic hydrophilic interaction (ZIC®-HILIC) column using LC-MS and LC-MS2 utilising electrospray ionization (ESI) in the positive ion mode. STG was metabolised to yield eleven metabolites, but in total only 3.1% of the parent drug was metabolised over 2 hrs incubation. These metabolites were structurally characterized on the basis of accurate mass analyses and the major metabolic routes for STG determined to be via aromatic oxidation (0.86%) and desaturation of N-C and C-C of the piperazine (0.44%). Novel metabolites of STG detected using these methods included STG N-glucuronide (M6) and a di-ketone metabolite (M4), hydroxylation of both the amine group and aromatic ring followed by formation of glucuronide metabolites (M5, M5’), oxidative desaturation of NH2 and di-hydroxylation of metabolites followed by loss of HF. Also, observed was an N-sulfate metabolite (0.07%) and acetylation followed by glucuronide conjugation was also found in trace amounts (

The aim of the paper is to present microbial transformation reactions as a step in the preparation of drugs or their key intermediates from plant derived compounds. Described are some successful applications of microbial transformation processes for preparation of steroid drugs and/or their important intermediates as well as some microbial transformations of terpenes, alkaloids, flavonoids and poly(phenols) affording derivatives with improved biological activities.

With the changing attitudes towards the legality of marijuana in the United States (US), there has been an abundance of rhetoric surrounding the potential societal effects of decriminalized cannabis use. These statements vary in degree from visions of the downfall of our moral and productive civilization, to the elimination of drug crime and a windfall of economic growth. From either side of this divisive issue, there has been a strongly expressed concern of the unknown consequences of a more readily available cannabis supply to the adolescent population, followed by what measures should be taken to curtail this risk. Given this country's unique relationship with mindaltering substances, a great deal of comparisons have been made with alcohol, as it is also a substance of recreation as well as abuse that is currently legal but has also gone through a period of prohibition. This paper looks to examine the validity of this comparison, as well as reviews the current research on the effects of early cannabis use on the adolescent brain.

Purpose: 16-dehydropregnenolone/DHP/CDRI-80/574, a new orally effective hypolipidemic agent presently in advanced clinical trials. This paper aims to study the absorption, distribution, metabolism and excretion profiles in order to delineate the possible cause(s) behind low bioavailability of CDRI-80/574 and also strategy to enhance the same. " Methods: Metabolic, Excretion and Pharmacokinetics studies were conducted in the Sprague-Dawley rats. Results: CDRI-80/574 exhibited log D: 4.5, absorption-half-life of 18 min and -constant 0.04/min by closed loop intestinal model in rats, was stable in gastric juice and 30% of RBCs transport/uptake was noted. CDRI-80/574 undergoes rapid metabolism in rat hepatic microsomal fractions; however extra hepatic tissues (intestinal-wall and -microvilli), showed less metabolism. IC50 of CDRI-80/574 was 2.22 nM, Km =15.8 nM, Vmax= 0.46 nmoles/mg protein/min, t1/2 was 3 min in microsomes. CDRI-80/574 was comparatively more stable in human hepatocytes (t1/2= 8.7 min) than rats (t1/2= 4.6 min). Aminobenzotriazole, ketoconazole, diltiazem and grapefruit juice inhibited CDRI- 80/574 metabolism, whereas, its metabolism was induced by phenobarbitone. Epoxy metabolite of CDRI-80/574 was synthesized and characterized. About 15% of CDRI-80/574 and 4 metabolites (hydrolysis/hydroxylation; m/z 317/319/321/330) were detected in feces. CDRI–80/574 was 7% bioavailable and exposure increased (2 fold) by grapefruit juice. Human CLinvivo was predicted to be 2.7 L/h/kg (45.83 ml/min/kg) by allometric scaling. Conclusion: CDRI-80/574 is the first hypolipidemic, synthetic compound of pregnane series, hence it is important to elucidate the major reason for its low bioavailability. The compound was fast metabolized by CYP3A4. Further the inhibitors of CYP3A4 were able to increase the bioavailability of CDRI-80/574.