Previously, we showed that the crude methanol extracts of Leucas indica flowers exhibited antioxidant properties and in the current study, crude methanol flower extracts of L. indica showed anticancerous properties as evidenced cytotoxicity (MTT assay test) against the selected cancerous cell lines HeLa, HCT116, HL-60, and MCF-7. Therefore, further analysis was performed to isolate and purify the bioactive compound using activity-guided repeated fractionation of the methanol extract by silica gel column chromatography. After collection of different fractions, all the fractions were subjected to TLC analysis and the fractions which yielded the same compounds on TLC were further analyzed for physicochemical and spectroscopic analyses, e.g., UV, IR, 1H NMR, 13C NMR, COSY, HSQC, and mass spectroscopy. The bioactive compound isolated was elucidated as 6-hydroxy-3-(4-hydroxyphenyl)-7-(3,4,5-trihydroxy-6-)(hydroxymethyl)tetrahydro-2H-pyran-2yl)-4H-chromen-4-one. Based on the antioxidant and anticancerous properties, L. indica might be a promising source of useful natural products and the newly bioactive compound might offer opportunities to develop new anticancerous drugs.
Linuron is well known for its antiandrogenic property. However, the effects of linuron on testicular and epididymal pro-and antioxidant status are not well defined. On the other hand, α-lipoic acid is well known as universal antioxidant. Therefore, the purpose of this study was twofold: firstly to investigate whether linuron exposure alters antioxidant status in the testis and epididymis of rats and if so, whether the supplementation of α-lipoic acid mitigates linuron-induced oxidative toxicity in rats. To address this question, α-lipoic acid at a dose of 70 mg/Kg body weight (three times a week) was administered to linuron exposed rats (10 or 50 mg/Kg body weight, every alternate day over a period of 60 days), and the selected reproductive endpoints were analyzed after 60 days. Respective controls were maintained in parallel. Linuron at selected doses reduced testicular daily sperm count, and epididymal sperm count, sperm motility, sperm viability, and number of tail coiled sperm, reduced activity levels of 3β-and 17β-hydroxysteroid dehydrogenases, decreased expression levels of StAR mRNA, inhibition of testosterone levels, and elevated levels of testicular cholesterol in rats over controls. Linuron intoxication deteriorated the structural integrity of testis and epididymis associated with reduced the reproductive performance over controls. Conversely, α-lipoic acid supplementation enhanced sperm quality and improved the testosterone synthesis pathway in linuron exposed rats over its respective control. Administration of α-lipoic acid restored inhibition of testicular and epididymal enzymatic (superoxide dismutase, catalase, glutathione reductase, glutathione peroxidise) and non-enzymatic (glutathione content), increased lipid peroxidation and protein carbonyl content produced by linuron in rats. α-lipoic acid supplementation inhibited the expression levels of testicular caspase-3 mRNA levels and also its activity in linuron treated rats. To summate, α-lipoic acid-induced protection of reproductive health in linuron treated rats could be attributed to its antioxidant, and steroidogenic properties.
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