Identification, isolation and characterization of active compounds from the Indian green mussels to develop drugs

Abstract

Recent studies showed that green mussel is not only an inexpensive source of protein for human consumption but also possess some complex bioactive compounds that have tremendous potential in medicine. Two compounds identified, (NIO-1 and NIO-2) display biological activity against the malaria parasite (mouse and human tested). A compound (NIO-3) may find use for developing effective drugs for the prevention and treatment of osteoporosis, osteoarthritis, rheumatoid arthritis, prevention of bone loss in bone metastasis, Paget's disease and other bone disorders of clinical importance. The compound (NIO-3) also possesses the ability to induce differentiation of dendritic cells from its bone marrow precursors. A compound (NIO-4) has also been isolated and characterized which is responsible for inhibition of the activity of the Rep protein of the Gemini virus. Subsequently, however, we have prepared several analogs of this compound and we now have a derivative, which exhibits a 20-fold increase in potency. This compound has been termed as (NIO-5). A compound (NIO-6) has been characterized for tuberculosis. To improve upon this, we have prepared and tested several analogues of this compound. Now we have an analogue that displays between 10 to 20 fold greater potency than NIO-6 and with no detectable growth of the bacteria up to 40 days after initiation of the culture. This improved analog has been termed as (NIO-7). Although the crude extract showed promise, our results discussed above reveal that we faced difficulties as we proceeded in the activity-guided fractionation for searching an anti-HIV compound. Interestingly, a chemical analysis suggested to us that the active principle was probably a small peptide sequence incorporated into silicon-based nanoparticles. To verify this we chemically synthesized the peptide and, in parallel, also standardized protocols for the generation of a range of silicon-based nanoparticles. Following this the peptide was incorporated into each of these nanoparticle compositions and then tested for bioactivity. One of these formulations was able to reproduce the activity of the native material. This synthetic formulation has been termed as (NIO-8).