DESIGNING OF COUMARIN DERIVATIVES AS SQUALENE SYNTHASE INHIBITORS

Objective: The importance of this research work is to design a library of novel coumarin derivatives by docking evaluation of the designed coumarin derivatives as squalene synthase inhibitor.Methods: The three-dimensional structure of designed molecules of squalene synthase inhibitors was collected from Protein Data Bank. The designed molecules were docked onto the enzymes that are squalene synthase inhibitor - 3WCM, 3WCJ, and 3Q2Z protein using SYBYL-X 2.1. Using a standard protocol, the protein was subjected to minimization and protomol generation.Results: By this method, we visualized the possible binding and also estimated the protein interactions with our intended coumarin library, using SYBYL-X 2.1 software. Into the active site of the selected enzymes, all the 20 coumarins were docked and then the docking scores revealed that the compounds possess high affinity toward the selected enzymes.Conclusion: With the help of virtual evaluation, we have elaborated a fast synthetically accessible coumarin-based compounds, and it is an advanced and original scaffold in the area of probable human squalene synthase inhibitors. Some of the developed compounds show better binding property than ligand, and in 3q2Z, the compound 5d shows better binding property than the protein. Furthermore, 6g and 6c have good binding property. In 3 WCM, the compound 6f has better property. In 3 WCJ, the compounds 6g and 6f show better binding property than the protein

The CURRENT TRENDS AND TREATMENTS IN DIABETIC RETINOPATHY

The drastically increasing issues of the disease scenario currently are with different types of diabetes all over the world. It has been reported, approximately 592 million are suffering from the disease throughout the world. It affects differently in different patients with the disease. There have been reports that it is affected differently and also has different side effects. It is also been reported that diabetes mellitus leads to the cause of diabetic retinopathy (DR) and also diabetic macular edema. It is considered as one of the most common causes which is linked to DR. DR has been considered as one of the most important causes for the loss of vision or impaired vision. The drugs show different types of incompatibility such as toxicity, solubility issues, aggregation, and chemical degradation these can be improved by applying several methods. DR is classified according to “Airlie House” into different categories and based on different strategies and consideration. It was found that DR is the main cause for vision loss and also there no much strategies for development of new treatment. The treatment involved is laser photocoagulation and vitrectomy, among these the effective treatment, was found to be laser photocoagulation. This is mainly characterized as proliferative and non-proliferative DR. Different therapeutic agents have been taken for the study these includes vascular endothelial growth factor, renin-angiotensin system inhibitors and nonsteroidal anti-inflammatory drugs, they are certainly different interventions for the treatment, they are nanotechnology and liposome. Nanotechnology applied is the most effective and also acceptable way of treatment

The distribution and ecology of the fresh- and brackish-water medusae of the world.

Limnocnida and Craspedacusta are the two main genera of Cnidaria from continental waters which have a free-swimming medusa in their life cycle. Both originated in tropical-subtropical Asia, but Limnocnida is also found in Africa, with one species (L. tanganjicae) perhaps endemic to lake Tanganyika. Halmomises from Trinidad, and two genera (Mansariella, Keralica) from India have limited ranges. No freshwater medusae evolved in Europe and the Americas (aside from Trinidad), but Craspedacusta sowerbii, by virtue of its drought resistant stages, has managed to colonise all continents, except Antarctica, in the course of the twentieth century. In all, there are about 10–14 freshwater species of medusae. An additional 4–5 species of Moerisia, Australomedusa, and Craspedacusta are sequestered in continental salt-lakes, while a few genera occur in brackish-water seas and estuaries (e.g. Moerisia, Odessia, Ostroumovia). This reduced diversity is probably due to (1) a rarity of drought resistant stages, adjusted to upstream dispersal, in the life cycle, and (2) difficulties to adapt the osmoregulatory system to a hypotonic environment.The feeding ecology of the freshwater medusae is also examined. Like all Cnidaria, they are opportunistic predators. However, fish egg predation might be their major means of subsistence, other types of food being taken only occasionally, or when fish eggs and larvae are scarce. Their impact on the true zooplankton might therefore be limited to short pulses of planktivory. Whether they are themselves limited by predation remains to be studied; many fish in the invasive part of their range avoid them, but some macrocrustaceans readily consume them. It is hypothesized that this might explain their success in Lake Tanganyika, and their absence from lake Baical. Finally, the absence of endemic species from South America could relate to the great diversity bf small-sized predatory aquatic reptiles on this subcontinent