Researchers at the 246th National Meeting & Exhibition of the American Chemical Society (ACS), have described ingredients found in nature that show potential in eliminating AIDS, Alzheimer’s, Cancer and other diseases.
Dr. Paul Wender a speaker at the exhibition, described efficient new ways of making prostatin as well as other drug candidates found in sea creatures, that are more effective for AIDS, Alzheimer’s and dug resistant cancers.
Prostatin is extracted from the bark of Samoan mamala tree. Wender synthesized prostatin in large amounts. Another scientist, Paul Cox, heard a native healer praise mamala bark tea as a remedy for viral hepatitis. It led scientists at the National Cancer Institute to analyze the bark and identify prostratin as a key ingredient. Wender’s synthesis of prostratin opened the door to research on the substance and enabled his team to change prostratin’s architecture.
“We now have made synthetic variants of prostratin, called analogs, that are 100 times more potent than the natural product,” Wender said. “That’s part of the basis for our approach to advancing potentially transformative treatments for AIDS, Alzheimer’s disease and resistant cancer. The mamala tree did not start making prostratin millions of years ago to treat a disease that appeared in the 20th century. The same is true for other substances that occur naturally in plants and animals. But we now have the tools to read nature’s library and use the lessons learned there to design, make and study new molecules that address unmet medical needs. This “function-oriented” approach seeks to identify useful parts of molecules and then, based on this knowledge, to design new and more readily synthesized molecules that work better or work in totally new ways. This is a well-validated strategy, perhaps best exemplified by the emergence of modern aviation from knowledge of how birds fly.”
The synthetic version of prostratin shows promise in laboratory tests for both preventing HIV from infecting human cells and flushing dormant HIV viruses that are hiding inside human latently infected cells.
Wender’s group has synthesized a substance called bryostatin, a chemical that occurs naturally in sea creatures called bryzoans.
“Bryostatin has shown great promise in laboratory experiments as the basis for development of potentially transformative medicines for cancer, Alzheimer’s disease and the eradication of HIV/AIDS,” Wender said. “However, its limited supply from natural sources has slowed research, and as with prostratin, it was not evolved in nature for modern therapeutic use. We have overcome both the supply and performance barriers by designing simpler and thus more readily synthesized analogs of bryostatin — over 100 of them so far. When tested in various assays related to HIV/AIDS eradication, these analogs are up to 1,000-fold more potent in flushing HIV out of its hiding places than prostratin. Much needs to be done, but we are on a promising trajectory.”
Wender noted that bryostatin and its analogs may also have benefits for people who have had strokes or other conditions in which learning and memory are impaired.The compound is known to improve learning and memory in laboratory rats. It appears to cause formation of new connections in the brain that are associated with learning and memory.
Other scientists are on the same pathway of extracting substances from nature to treat AIDS. The neem tree of India is known as the “village pharmacy.”
Dr. Sonia Arora and her students found 20 compounds present in various types of neem extracts. Extracts from neem leaves, bark and flowers are used throughout the Indian subcontinent to fight against pathogenic bacteria and fungi. “The farther you go into the villages of India, the more uses of neem you see,” says Arora. Tree branches are used instead of toothpaste and toothbrushes to keep teeth and gums healthy, and neem extracts are used to control the spread of malaria.
When they modeled these compounds against the proteins critical for the HIV life-cycle, Arora and her team discovered that most of the neem compounds attacked the HIV protease, a protein essential for making new copies of the virus.
American Chemical Society (ACS) (2013, September 9). Translating nature’s library yields drug leads for aids, cancer, Alzheimer’s disease.
Federation of American Societies for Experimental Biology (FASEB) (2012, April 22