ABSTRACT
Arbutus andrachne L. is widely distributed in Jordan. Tyrosinase is the key enzyme in the biosynthesis of melanin. This preliminary study was carried out to assess the possible anti-tyrosinase activity of A. andrachne extracts. Arbutin, hydroquinone and kojic acid were selected as inhibitor standards. Five different extracts (chloroform, butanol, ethanol, methanol and water) were prepared from A. andrachne stems and their activities were compared with the selected tyrosinase inhibitors. IC(50) was measured for both, standard and plant extracts. Among the different extracts, the methanolic extract exhibited the highest anttyrosinase activity with an IC(50) value (1 mg mL(-1)). Furthermore, 9 mg A. andrachne methanolic extract showed 97.49% inhibition of tyrosinase activity. Arbutin, hydroquinone, beta-sitosterol and ursolic acid were identified in the different extracts of A. andrachne by thin layer chromatography (TLC) and isolated by preparative TLC from the methanolic and chloroform stem extracts, respectively.
Subject(s)
Ericaceae/chemistry , Peptides/pharmacology , Plant Extracts/pharmacology , Arbutin/pharmacology , Hydroquinones/pharmacology , Inhibitory Concentration 50 , Plant Stems/chemistry , Pyrones/pharmacology , Tyrosine/metabolismABSTRACT
Meloxicam, a selective cyclooxygenase-2 inhibitor, was administered orally or intravaginally, to sperm-positive female rabbits to assess its effect on ovulation. A single oral dose (20 mg/kg), administered 5 h postcoitus resulted in 100% contraceptive rate. On the other hand, for females receiving meloxicam suppositories (14.9 mg/kg), 5 h postcoitus, the contraceptive rate was 62.5% compared to placebo. The decrease in the contraceptive effect of meloxicam suppository may be due to the rejection of the dose by some females. Corpora lutea, maternal plasma progesterone, ovary fresh weight and maternal body weight gain were not affected by meloxicam treatment compared to placebo. Histopathologically, the surface of the ovary of meloxicam-treated females appears irregular and dilated due to the presence of different-sized cysts. Some of the cystic follicles were retained ova. Further, immunohistochemical stains for estrogen and progesterone receptors showed positive staining in granulosa cells and the wall of the unruptured follicle. It is concluded that contraceptive effect of meloxicam in female rabbits resulted in a failure of follicular rupturing.
Subject(s)
Contraceptive Agents, Female/administration & dosage , Cyclooxygenase Inhibitors/administration & dosage , Ovarian Follicle/drug effects , Thiazines/administration & dosage , Thiazoles/administration & dosage , Administration, Intravaginal , Administration, Oral , Animals , Cyclooxygenase 2 , Cyclooxygenase 2 Inhibitors , Female , Granulosa Cells/chemistry , Immunohistochemistry , Isoenzymes/antagonists & inhibitors , Meloxicam , Ovary/anatomy & histology , Ovary/drug effects , Ovulation/drug effects , Placebos , Progesterone/blood , Prostaglandin-Endoperoxide Synthases , Rabbits , Receptors, Estrogen/analysis , Receptors, Progesterone/analysisABSTRACT
The nonsteroidal antiinflammatory, selective cyclo-oxygenase-2 (COX-2) inhibitor, meloxicam, was tested to assess its effect on rabbit ovulation. Meloxicam in different doses was administered intraperitoneally (ip) to adult female Californian rabbits at 2, 5, 8, and 24 h postcoitus with sperm-positive rabbits. Rabbits were killed on Day 10 of gestation. Meloxicam produced significant inhibition of ovulation in rabbits. This inhibition of ovulation by meloxicam was dose- and time-dependent. Ovulation in rabbits was completely inhibited by a single ip administration of meloxicam (20 mg/kg) when the drug was administered at 2 and 5 h postcoitus, whereas neither ovulation nor implantation were inhibited (pregnancy rate 75%) by the same dose administered 24 h postcoitus (approximately 14 h post ovulation). Further, ovulation was completely inhibited by 10 mg/kg of meloxicam when the drug was administered at 5 or 8 h postcoitus, but there was less inhibition of ovulation when 10 mg/kg of the drug was administered at 2 or 24 h postcoitus (pregnancy rate 25 and 80%, respectively). Corpora lutea, maternal plasma progesterone, ovary fresh weight, and maternal body weight gain were affected by meloxicam treatment. Histopathological findings observed in the ovaries of treated rabbits included microscopic dilatation of graffian follicles, particularly mature follicles. Some of the follicles were cystically dilated in addition to severe hemorrhage within the follicles which lost ova. These results show that ovulation can be inhibited in rabbits by meloxicam. Further studies are needed to assess the value of selective COX-2 inhibitors as potential nonhormonal contraceptive agents.
Subject(s)
Cyclooxygenase Inhibitors/pharmacology , Indomethacin/pharmacology , Ovulation , Thiazines/pharmacology , Thiazoles/pharmacology , Animals , Female , Meloxicam , Ovary/pathology , Pregnancy , RabbitsABSTRACT
Two accurate, precise and sensitive thin layer chromatographic (TLC) and second derivative UV-spectrophotometric procedures are described for the simultaneous determination of ascorbic acid and dipyrone in pure form and in pharmaceutical dosage forms. The TLC method involved direct application of methanolic solutions of tested samples on silica gel TLC plates using water:methanol (95:5 v/v) as developing system. The developed plates were then directly scanned at 260 nm using a TLC scanner. The second method depends on second derivative UV-spectrophotometry with zero crossing technique of measurement. Second derivative amplitudes at 280 and 272 nm were selected for the determination of ascorbic acid and dipyrone, respectively. Both methods show good linearity, precision and reproducibility. They are simple and do not require manipulation prior to analysis. The proposed methods have been successfully applied to the determination of the drugs in various pharmaceutical dosage forms such as tablets and ampoules.
