ARTICLE Issue 011
Amol A. Kulkarni, Ph.D. Associate Professor, College of Pharmacy, is Researching Treatment of Viral infections and Neurodegenerative Disorders
Amol A. Kulkarni, Ph.D.
Dr. Amol Kulkarni recently described his research as focused on the development of small, non-peptidic, natural product-inspired molecular scaffolds for the treatment of viral (including retroviral) infections and neurodegenerative disorders, such as Alzheimer’s Disease (AD), Parkinson’s Disease (PD), etc.
He further provides a description of his two major ongoing projects below.
Project 1: Development of novel curcumin analogs as antiretroviral and neuroprotective agents
Figure 1: Chemical structure of curcumin
Curcumin (figure 1), is a bis-phenolic natural product isolated from rhizomes of Curcuma longa (turmeric). It has displayed impressive pleiotropic activity as antiretroviral, anticancer, anti-inflammatory, neuroprotective, and anti-diabetic agent. However, low plasma half-life and facile conversion into pharmacologically-inactive glucuronide derivatives have severely restricted its clinical use. Our group has developed a library of approx. 20 covalently-modified analogs of curcumin. Some of our covalently-modified analogs of curcumin have displayed potent activity against HIV-1 and other retroviruses. Our analogs have also shown promising neuroprotective and neurogenesis-promoting activities in in-vitro assays. We are currently developing potent, dual-acting hybrid molecules that feature a chemical combination of our covalently-modified curcumin analogs with other pharmacophores.
Project 2: Development of quinoline-based small molecules with anti-Filovirus activity
Filovirus infections (such as Ebola infections) are characterized by hemorrhagic fever and are associated with high rates of mortality. Our group is developing quinoline-based small molecules that can be used for the clinical management of filovirus infections.
"We welcome enthusiastic, highly-motivated individuals interested in medicinal chemistry, drug development, organic synthesis, and spectroscopy to join our research group. Interested individuals should contact Amol Kulkarni, Ph.D. (email@example.com), "he states.
His recent publications include
1. Kumari, N.; Kulkarni, A. A. Lin, X.; McLean, C.; Ammosova, T.; Hipolito, M.; Nekhai, S.; Nwulia, E. (2015) "Inhibition of HIV-1 by Curcumin A, a novel curcumin analog" (manuscript accepted).
2. Fortunak, J. M., de Souza, R. O., Kulkarni, A. A., King, C. L., Ellison, T., Miranda, L. S. M. (2014) "Active Pharmaceutical Ingredients for Antiretroviral Treatment in Low- and Middle-income Countries: A Survey" Antiviral therapy, 19, 15-29.
3. Ammosova, T., Platonov, M., Ivanov, A., Kont, Y. S., Kumari, N., Kehn-Hall, K., Jerebtsova, M., Kulkarni, A. A., Üren, A., Kovalskyy, D., Nekhai, S. (2014) 1E7-03, a Small Molecule Targeting Host Protein Phosphatase-1, inhibits HIV-1 transcription" British Journal of Pharmacology, 171, 5059-75.
4. Hurley, L. L., Akinfiresoye, L., Nwulia, E., Kamiya, A., Kulkarni, A. A., Tizabi, Y. (2013) "Antidepressant-like effects of curcumin in WKY rat model of depression is associated with an increase in hippocampal BDNF" Behavioral Brain Research, 239, 27-30.
Patent applications are as follows:
1. "Lipophilic Curcumin Analogs and Methods of Inhibiting HIV-1, Treating latent HIV in Brain, and Preventing HIV-Mediated Cognitive Decline"
Inventors: Evaristus A. Nwulia and Amol A. Kulkarni
Application Number: 13/793,755 (Filed: March 11, 2013)
Pub. No.: US 2014/0051742 A1 (Publication Date: February 20, 2014)
2. "Green Chemistry Synthesis of the Antimalarial Drug Amodiaquine"
Inventors: Fortunak, Joseph, M., Kulkarni, Amol A., and King Christopher
Application Number: 61610267 (Filed: March 9, 2013)
Dr. Kulkarni is currently funded for the following cycles and grant amounts:
Behavioural Science Foundation Award, Behavioural Science Foundation
Total Award Amount: $85,385
PCSP Research Award, Pilot and Collaborative Studies Program
Georgetown Howard Universities Center for Clinical and Translational
Total Award Amount: $50,000
U19 Research Award, National Institute of Allergy and Infectious Diseases, NIH
Total Award Amount: $ 3,211,769
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