Schistosomiasis is a chronic parasitic disease affecting about 207 million individuals worldwide. It is still a major health problem in many tropical and subtropical countries, as well as for travelers from developed countries. The treatment strategies of schistosomiasis can be divided into two main routes: (a) chemotherapy treatment including trivalent antimony compounds, hycanthone mesylate, niridazole, metrifonate, oxamniquine, oltipraz, artemisinins, albendazole, amoscanate mirazid, and praziquantel; (b) vaccines that may play an important role in the control of schistosomiasis in the future.
Synthesis of new series of 5,6,7,8-tetrahydronaphthalene derivatives conjugated with chalcone, pyridine, pyrazole and isoxazole functionalities hoping to circumvent the unwanted ulcerogenic and other side effects of the already used nonsteroidal anti-inflammatory drugs.
Most currently used nonsteroidal anti-inflammatory drugs (NSAIDs) suffer from limitation in their therapeutic uses, since they cause gastrointestinal and renal side effects related to inhibition of cyclooxygenase1 (Cox1) in tissues where prostaglandins exert physiological effects.
Reaction of 2-acetyl tetralin (1) with some aromatic aldehydes in the presence of malononitrile yielded 2-amino-3-cyanopyridine derivatives 2a–c. Condensation of compound 1 with aromatic aldehydes afforded the chalcone derivatives 3a–c. Then, compound 3a reacted with hydrazine hydrate or phenyl hydrazine and yielded pyrazoline derivatives 4 or 5, respectively. Also, the reaction of compound 3c with hydroxylamine hydrochloride afforded the isoxazole derivative 6. Anti-inflammatory properties of the synthesized compounds were evaluated in vivo utilizing formalin induced paw edema method in rats, analgesic activities were tested via both hot plate and writhing methods.
Derivatives 2c and 3c revealed promising results when the anti-inflammatory, analgesic, and ulcerogenic activities of the synthesized compounds were evaluated. All of the compounds induced significant central and peripheral analgesia. The derivatives 2a, 2c, 3a, 3b, 3c, 5, and 6 showed higher activity than the standard ibuprofen.
The present study was designed to evaluate the safety of synthesized needle-like hydroxyapatite (HAp) nanoparticles ranging from 3 to 7 nm in diameter and from 27 to 46 nm in length when administered in female rats orally or subcutaneously at different concentrations.
Animals in different treatment groups were maintained on their respective diets as follows: group 1, untreated control; group 2, treated orally with HAp (300 mg/kg body weight) for 3 weeks; group 3, treated orally with a low dose of HAp (150 mg/kg body weight) for 3 weeks; and group 4, implanted subcutaneously with HAp (600 mg/kg body weight) once and left for 5 weeks. At the end of the experimentation period, blood samples were collected from all animals for biochemical analysis (alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, uric acid, urea, and creatinine). After sacrifice, histopathological examination of the liver and kidney was carried out.
The biochemical results showed an increase in alanine aminotransferase and aspartate aminotransferase in the groups treated orally and those treated subcutaneously. There was an increase in alkaline phosphatase only in the group receiving the high oral dose; however, animals treated with the low dose or those treated subcutaneously were comparable with the control group. All the rats showed normal kidney function because of normal levels of creatinine, urea, and uric acid. The histopathological results indicated that the liver and kidney of all rats treated with HAp (oral or subcutaneously) had a normal structure. The previous results confirmed the safety of the synthesized nanoneedle HAp when administered orally or subcutaneously at the suggested dose.