药物化学

Indanone derivatives share vital pharmacological properties, considered useful in alzheimer’s disease (AD).The aim of this study was synthesis and evaluate indolizine analogues if possess acetyl cholinesterase (AChE)inhibitory activity. The easily accessible three-step synthesis of these compounds resulted to be significantly less difficult and expensive than that of donepezil. Several compounds possess anti-cholinesterase activity in the order of micro and sub-micromolar. Particularly, compound 3k was the most potent inhibitors of the series. Compound 3k, showed potent inhibitory activity against acetyl cholinesterase enzyme with IC50 0.10 μmol/L. Indolizine analogues might be potential acetyl cholinesterase agents for AD.

Synthesis of some novel pyrimido[1,6-a]pyrimidine derivatives 4, 8 and 10 was described through the respective reactions of sodium salts of formyl ketones 1, 7 and 9 with 6-aminothiouracil. The characterization of the reaction products was confirmed by using the available elemental analysis and spectral data. One of these derivatives (4b), 1-thioxo-1,2,7,8,9,10-hexahydro-3H-pyrimido[1,6-a]quinazolin-3-one, was tested using sublethal dose level (10 mg/kg b. w./day for 3 weeks) and was found to have potent antihyperglycemic, antihyperlipidemic and antioxidant properties in neonatal streptozotocin-induced (n-STZ) diabetic male and female albino rats.

Carbon nanotubes (CNTs) possess exceptional mechanical and electrical properties, therefore researches and developments are performed in various fields. In recent years application to the medical field of CNTs attracted attention, and a large number of studies have begun to be performed. An applied study to cancer diagnosis and treatment, and a study to use for scaffold for regenerative medicine, besides, a study to compound in CNTs for the improvement of the function and durability of conventional biomaterials. In the applied study that properties of all CNTs were fully made use of in, development in the future is expected. In this review, we state it about the contents of a performed study for medical application of CNTs now, and introduce in particular the basic studies that are performed to apply CNTs to biomaterials in detail.

Objective: The prevalence of overweight and obesity is considered an important public issue in the United States and is increasing among both children and adults. There is evidence of aberrations in the vitamin D-endocrine system in obese subjects. Therefore, we will review the role of vitamin D in the adipose tissue.
Methods: Review Medline database literature and discuss the relationship between vitamin D status and obesity.
Results: It has been noted that vitamin D deficiency and obesity share many of the same risk factors, including both indirect – environmental factors (nutritional, racial, geographic, seasonal, and exposure to air pollution) -- -- and direct - genetic risk factors (vitamin D receptor, polycystic ovary syndrome, cytochrome P450, locus 20q13, vitamin D-binding protein gene polymorphisms, and aP2 gene). Vitamin D is fat-soluble and stored in adipose tissue. The serum concentration of 25-hydroxyvitamin D3(25OHD3) is inversely correlated with body weight. The vitamin D receptor (VDR) is present in adipose tissue and may contribute to the action of vitamin D and its analogs in adipocytes. 1,25-dihydroxy-vitamin D3 (1,25OHD3) exerts its actions mainly via its high affinity receptor VDR through a complex network of genomic (transcriptional and post-transcriptional) and non-genomic mechanisms.
Conclusion: Vitamin D plays a role in the regulation of adipose tissue. Obese individuals may need higher doses of vitamin D supplementation than do lean individuals to achieve optimal levels of 25OHD3.Calcitriol modulates adipokine expression and inhibits anti-inflammatory cytokine expression. Calcitriol definitely has a role in the human adipose tissue because of its active form of vitamin D3 metabolite, their receptors presented in adipocytes, and itse suppression of PTH levels.