Design and synthesis of pyrazolo[3,4-d]pyrimidinone derivatives: Discovery of selective phosphodiesterase-5 inhibitors.

A novel series of 1,6-disubstituted pyrazolo[3,4-d]pyrimidin-7-one derivatives, 2a-h, 4a-d, 5 and 6, were successfully synthesized, which showed promising, and potent inhibition of phosphodiesterase 5 (PDE5). The inhibitory activities of 5, 4b, 2a, 2d, 2f, 4d and 4a against PDE5 were similar to that of sildenafil (100%). These compounds exhibited potent relaxant effects on isolated rat cavernosum tissue with pEC values ranging from 8.

Targeting of somatostatin receptors expressed in blood cells using quantum dots coated with vapreotide.

Cancer may be difficult to target, however, if cancer targeted this provides the chance for a better and more effective treatment. uantum dots (Qdots) coated vapreotide (VAP) as a somatostatin receptors (SSTRs) agonist can be efficient targeting issue since may reduce side effects and increase drug delivery to the target tissue. This study highlights the active targeting of cancer cells by cells imaging with improving the therapeutic outcomes.

Perindopril regulates the inflammatory mediators, NF-κB/TNF-α/IL-6, and apoptosis in cisplatin-induced renal dysfunction.

Cisplatin (CP) is an essential chemotherapeutic drug used over the world against many types of cancer. It has several side effects such as ototoxicity, myelosuppression, and nephrotoxicity. Nephrotoxicity is the most dangerous and is considered a dose-limiting one.

Neural and Endocrinal Pathobiochemistry of Vitiligo: Comparative Study for a Hypothesized Mechanism.

The etiology of vitiligo is still unclear. The aim is to investigate a neural and hormonal etio-pathology of vitiligo. Sixty acrofacial vitiligo patients were divided into two subgroups as active vitiligo patients group (AVPs;  = 35) and stable vitiligo patients group (SVP;  = 25).

Curcumin ameliorate DENA-induced HCC via modulating TGF-β, AKT, and caspase-3 expression in experimental rat model.

Hepatocellular carcinoma (HCC) is one of the most common malignancies worldwide. In laboratory animal models, diethylnitrosamine (DENA) is a well-known agent that has a potent hepatocarcinogenic effect that is used to induce HCC. As curcumin has a potent anti-inflammatory effect with strong therapeutic potential against a variety of cancers, our present study aims to investigate its curative effects and the possible mechanisms of action against DENA-induced HCC in male rats.

Behavior of intraocular pressure after intravitreal injection of triamcinolone acetonide among egyptians.

Purpose: To evaluate the changes in intraocular pressure (IOP) after intravitreal injection of triamcinolone acetonide for the management of diabetic macular edema (DME).

Methods: The study design is a prospective, interventional, two-arm, dose-response study. Nineteen patients with bilateral DME were included, one eye for every patient underwent intravitreal injection of 4 mg triamcinolone acetonide (group A, 19 eyes), and the other eye of the same patient underwent intravitreal injection of 8 mg triamcinolone acetonide (group B, 19 eyes); the selection as to which eye was to receive either dose was random.