Anti-fertility effects of fractions from Carica papaya (Pawpaw) Linn. methanol root extract in male Wistar rats

The methanol root extracts of Carica papaya (Pawpaw) are used in eastern Nigeria for the treatment of malaria, hepatitis and jaundice. The aim of this study was to investigate the effects of the fractions isolated from C. papaya methanol root extract on fertility in male Wistar rats using sperm counts, percentage defective sperm cells (morphology), biochemical and hormonal assays as biomarkers. The roots of C. papaya were extracted using 80% methanol for 72 h. Oral acute toxicity study was done with the crude extract for 24 h. The extract was fractionated by column chromatography using petroleum ether, chloroform, ethyl acetate and methanol. The petroleum ether fraction was further fractionated on preparative TLC using ethyl acetate–methanol solvent systems to isolate CPFE 1, CPFE 2 and CPFM 1. The 3 fractions (75 mg/kg) were used to treat male Wistar rats orally for 60 days. Animals were euthanized and testes collected, homogenized and used for sperm count and motility. Plasma and serum were used to assay biochemical parameters including aspartate aminotransferase (AST), blood urea nitrogen (BUN), total bilirubin (TB), alkaline phosphatase (ALP), alanine aminotransferase (ALT), gamma glutamyl transferase (GGT), triglycerides, hormones (LH and FSH). Histopathological study of the testes, kidney, heart and liver were conducted. Acute toxicity result showed that C. papaya root extract produced no mortalities at the dose of 2000 mg/kg but induced CNS-related symptoms as well as diuresis. The fractions significantly (P < 0.01) produced decreases in sperm counts and increased the percentage of defective sperm cells. There were significant (P < 0.05) increases in aspartate aminotransferase (AST) and blood urea nitrogen (BUN). Histopathological studies showed mild kidney and cardiac hyperaemia, slight hepatic degeneration and severe necrosis of the germinal epithelium of the testes. This study calls for some level of caution in the use of these roots and its extracts/fractions in traditional medicine for treating diseases. On the other hand, it could be a good source of drug for birth control.     

Antimicrobial,antifertility, and antiradiation studies of Ga(III) and Tl(I) complexes with N∩S and N ∩ O donor systems

New complexes of gallium(III) and thallium(I) derived from 5,6-dimethyl-1H-indol-2,3-dione hydrazinecarbothioamide (L¹H) and 5,6-dimethyl-1H-indol-2,3-dione hydrazinecarboxamide (L²H) have been prepared and investigated using a combination of microanalytical analysis, melting point, molar conductance measurement, electronic, IR, ¹H NMR, and ¹³C NMR spectral studies. Gallium isopropoxide interacts with the ligands in 1 : 1, 1 : 2, and 1 : 3 molar ratios resulting in the formation of colored products, whereas TlCl forms only unimolar products. The mono- and bis-alkoxy derivatives are dimeric, while the tris ligand metal complexes are monomeric. On the basis of conductance and spectral evidences, a pentacoordinate structure for gallium(III) 1 : 1 complexes, hexacoordinate structure for 1 : 2 and 1 : 3 complexes, and a bicoordinate geometry for thallium(I) complexes have been assigned. The ligands are coordinated to gallium(III) and thallium(I) via the azomethine nitrogen and the thiolic sulfur/enolic oxygen. The antimicrobial activities of the ligands and complexes have been screened in vitro against bacteria Pseudomonas cepacicola and Bacillus subtilis and fungi Collectatrichum capsici and Fusarium oxysporum. The complexes have higher activities than the free bases. In vivo studies of the ligands and their corresponding complexes have also been carried out to assess their antifertility and antiradiation activities. The results of these activities indicate the antiandrogenic and radiation protective nature of these complexes.     

SALT,SOLVENT AND SUBSTITUENT EFFECTS IN THE HYDROXIDE AND ALKOXIDE PROMOTED DECOMPOSITION OF PHOSPHONIUM COMPOUNDS

Abstract

The 1,2,3-trithiolan of endo-dicyclopentadiene, C₁₀H₁₂S₃ (1) can be polymerized to give low molecular weight polymers (C₁₀H₁₂S₃)_n, n = 3–6, by heating or by exposure to UV irradiation. The polymers differ according to the method of polymerization as revealed by their n.m.r. spectra. Depolymerization of both types of polymer can be achieved by heating with amines, and especially with R₃N. Desulphurization of (1) by Na₂SO₃ or triphenylphosphine produces a polymer of composition (C₁₀H₁₂S₂)_n, n= ca 18–19. The depolymerization of this material by Et₃N regenerated some (1).     

Antifertility and biocidal activities of organometallics of silicon,germanium, titanium and zirconium derived from 2-acetylthiophene thiosemicarbazone

A comparative biochemical study of four Group IV element compounds with specific sulphur-containing organic substrates has been carried out and discussed. The structural characterizations of these organometallics, viz. Me₂SiLCl, Me₂SiL₂, Me₃SiL, Ph₂SiLCl, Ph₂SiL₂, Ph₃SiL, Ph₃GeL, Cp₂TiLCl, Cp₂TiL₂, Cp₂ZrLCl and Cp₂ZrL₂ (where LH?2-acetylthiophene thiosemicarbazone) had been deduced on the basis of various physico-chemical and instrumental techniques, viz., IR, UV, ¹H NMR, ¹³C NMR AND ²⁹SI NMR spectral studies. All the organometallics and the parent thiomine have been screened against a number of microbes and their sterilizing power in male mice tested. The results of these biocidal studies show that the organosilicon(IV) and organogermanium(IV) compounds are more active than the organotitanium(IV) and organozirconium(IV) derivatives. An attempt has also been made to correlate the structural aspects of the molecule with its biological activity.