Journal of Pharmaceutical Research

T. Ratna Kumari ¹, M. Vidyavathi ¹, S. Asha ¹, K. V. S. R. G. Prasad ¹

Affiliations
1 Institute of Pharmaceutical Technology, Sri Padmavati Mahila Visvavidyalayam (Women's University), Tirupati - 517 502, Andhra Pradesh, IN

Abstract

The aim of the study was to develop a microbial model for synthesis of paracetamol metabolite for further pharmacological and toxicological studies. The metabolite of paracetamol in microbial cultures was identified, isolated and confirmed using fermentation techniques, Thin Layer Chromatography (TLC) and High Pressure Liquid Chromatography (HPLC) followed by liquid chromatography/mass spectrometry (LC/MS). Among different organisms screened, Cunninghamella echinulata showed an extra peak at 5.1 min in HPLC compared to its controls indicating formation of a metabolite. The metabolite was further characterized by mass spectrometry and was found to be N-acetyl-p-benzoquinoneimine (NAPQI) which is a toxic metabolite. Cunninghamella echinulata was able to metabolize paracetamol to its toxic metabolite by N-hydroxylation and rearrangement similar to human beings. This study has developed a model to produce toxic metabolites of other similar drugs easily for further toxicological and pharmacological studies.

Keywords

Microbial Model, Metabolism, Paracetamol, N-Hydroxylation, NAPQI.

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B. Sailaja ¹, K. Bharathi ¹, K. V. S. R. G. Prasad ¹

Affiliations
1 Institute of Pharmaceutical Technology, Sri Padmavati Mahila Visvavidyalayam (Women’s University), TIRUPATI-517 502, IN

Abstract

The ischolar_mains of Ruellia tuberosa L. are recommended for kidney stone disorders in the Indian traditional system of medicine. Ethanolic extract of R. tuberosa ischolar_mains was evaluated for antiurolithiatic activity against 0.75% v/v ethylene glycol and 2% w/v ammonium chloride induced calcium oxalate urolithiasis and for antioxidant activity against hyperoxaluria induced oxidative stress in male albino rats. Ethylene glycol and ammonium chloride administration increased the deposition of calcium and oxalate in the kidneys, urinary excretion of calcium, oxalate and creatinine in the preventive and curative control rats. In these groups, increased levels of malondialdehyde and depleted levels of antioxidant enzymes, reduced glutathione and catalase were observed. On treatment with the extract, a significant reduction in the deposition of calcium, oxalate and also urinary excretion of calcium, oxalate and creatinine was observed, indicating its antiurolithiatic effect. The extract administration also decreased the extent of lipid peroxidation and enhanced the levels of antioxidant enzymes in the kidneys of urolithic rats, reflecting its antioxidant efficacy against hyperoxaluria induced renal oxidative stress. Results of the present study support the traditional claim of R. tuberosa ischolar_mains in treating renal calculi.

Keywords

Ruellia tuberosa, Calcium Oxalate Urolithiasis, Ethylene Glycol/Ammonium Chloride, Oxidative Stress, Antiurolithiatic and Antioxidant Activities.

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