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Tag: Belen Cassera

Antiplasmodial flavanones and a stilbene from Carpha glomerata

graphical abstract

Abstract

Bioassay-guided fractionation of an extract of Carpha glomerata (Cyperaceae) led to the isolation of seven compounds. Compounds 1 (carphorin A), 3 (carphorin C), 4(carphorin D), and 5 (carphabene) are new compounds, and compound 2 (8-(3″-hydroxyisoamyl)-naringenin) was isolated for the first time as a natural product. All structures were elucidated based on analyses of their HR-ESIMS and 1D and 2D NMR data. Compounds 12, and 6, which have prenyl or hydroxyprenyl side chains, exhibited antiplasmodial activities with IC50 values of 5.2 ± 0.6, 3.4 ± 0.4, and 6.7 ± 0.8 µM against the drug-resistant Dd2 strain of Plasmodium falciparum. In addition the prenylated stilbene 5 also showed good activity, with IC50 5.8 ± 0.7 µM.

Namki Cho, Ana Lisa Valenciano, Yongle Du, Jason Clement, Maria B. Cassera, Michael Goetz, David G. I. Kingston. 2018. Bioorganic & Medicinal Chemistry Letters; 28(20):3368-3371. https://doi.org/10.1016/j.bmcl.2018.09.003

Visiting Scholar: Elvis Ofori Ameyaw

 

scholar Elvis Ameyaw

Elvis Ofori Ameyaw is a Fulbright Scholar visiting M. Belen Cassera‘s laboratory in the department of molecular biology and biochemistry. He is a senior lecturer, Head of the Department of Biomedical Sciences and the Vice-Dean of the School of Allied Health Sciences in the College of Health and Allied Sciences at the University of Cape Coast in Ghana.

Dr. Ameyaw holds a B. Pharm and Ph.D. in Pharmacology. His research focuses on natural product drug discovery for infectious, in particular, malaria and Leishmania, and inflammatory diseases. At the University of Georgia, he is using in vitro techniques to screen some natural products isolates from plants that are traditionally used to treat malaria in Ghana.

“UGA is globally known for excellent research and education and my host scientist, Prof. M. Belen Cassera has created an envious and reputable niche in natural product research,” said Dr. Ameyaw.

The availability of seminars and other opportunities to interact with leading scientists also factored into Dr. Ameyaw’s decision to come to UGA.

“The research staff at UGA are very supportive and willing to share ideas.” said Dr. Ameyaw.

Athens reminds him of the college town of Cape Coast where he resides and works in Ghana.

“The city makes me feel at home away from home.”

Read more about Dr. Cassera’s natural products research.

New UGA Drug Discovery Core lab works to develop treatment of leading diseases

Drug Discovery Center team
Members of the Drug Discovery Core steering committee in the new DDC laboratory (from left to right): Shelley Hooks, interim director of the Center for Drug Discovery and associate professor of pharmaceutical and biomedical sciences; Scott Pegan, chair of the steering committee and associate professor of pharmaceutical and biomedical sciences; Belen Cassera, associate professor of biochemistry and molecular biology; Kojo Mensa-Wilmot, professor and head of UGA’s cellular biology department and director of the Chemical Biology Group; and Brian Cummings, director of the Interdisciplinary Toxicology Program and professor of pharmaceutical and biomedical sciences.

Athens, Ga. – The University of Georgia has created the Drug Discovery Core laboratory, a campus-wide collaborative facility designed to hasten the development of therapeutic drugs for a number of major diseases.

A survey distributed to UGA researchers in 2016 identified chemical screening and toxicity profiling as the most critical needs for enhancing drug discovery research at UGA, and the DDC will address many of those needs for faculty working in infectious disease, regenerative medicine, cancer biology and other human health-focused disciplines.

Phase one of the new lab will allow for the curation, management and distribution of chemical libraries containing more than 50,000 compounds. The lab also will enable researchers to rapidly screen these chemical libraries in miniaturized models of various diseases using robotics and high-throughput signal detection. Finally, the lab will provide opportunities to identify potential toxicity of the compounds and determine if their chemical properties will allow them to be successfully delivered to patients. Additional capabilities, including pharmacokinetic characterization, genotoxicity and assay design, are under development.

“The most immediate outcome of the DDC lab will be to generate preliminary data from pilot chemical screens, which is necessary to secure large drug discovery grants from the National Institutes of Health to fund more advanced drug discovery research,” said Shelley Hooks, interim director of the Center for Drug Discovery and associate professor of pharmaceutical and biomedical science. “The longer-term goals of the lab are to discover and develop new drug candidates and chemical probes, as well as enhance training of graduate students in biotechnology.”

Creation of the DDC was initiated by Hooks in collaboration with Brian Cummings, director of the Interdisciplinary Toxicology Program and professor in the pharmaceutical and biomedical sciences department, and Scott Pegan, chair of the DDC steering committee and associate professor of pharmaceutical and biomedical sciences.

Sponsoring campus organizations include the College of Pharmacy, the College of Veterinary Medicine, the Office of Research, the Center for Tropical and Emerging Diseases and the Department of Cellular Biology.

The laboratory is located in Room 224 of the Wilson Building in the College of Pharmacy. For more information on capability, resources and access to the libraries and screening instruments, contact Pegan (spegan@uga.edu) or see cdd.rx.uga.edu.

Writer: Mickey Y. Montevideo
Contact: Shelley B. Hooks