



From penicillin to Taxol, most new drugs have had their roots in natural products, but scientists worry that the approach is in decline
By Brendan Borrell | July 9, 2009 | 7
In the 19th century, Friedrich Sertümer, a pharmacist's apprentice, isolated morphine from the latex resin of the opium poppy ( Papaver somniferum )....[More]
In the 19th century, Friedrich Sertümer, a pharmacist's apprentice, isolated morphine from the latex resin of the opium poppy (Papaver somniferum). This achievement marked the first time a pure pharmaceutical compound had been isolated from a plant and set off the era of modern medicine. Today, morphine remains one of the most widely used painkillers, and researchers in Australia have even designed genetically modified poppies to increase yields and reduce costs associated with harvesting the drug. [Less] [Link to this slide]
Penicillin , the world's first antibiotic, was described in 1928 when Alexander Fleming at Saint Mary's Hospital in London noticed a strange fungus was killing off his bacterial colonies....[More]
Penicillin, the world's first antibiotic, was described in 1928 when Alexander Fleming at Saint Mary's Hospital in London noticed a strange fungus was killing off his bacterial colonies. Ten years later, Howard Florey and Ernst Chain at the University of Oxford began working on a way to isolate the compound from the penicillium fungus and produce enough of it to be used on wounded soldiers during World War II. [Less] [Link to this slide]
Cone snails have one of the most potent venoms known, which they use to paralyze small fish by blocking the movement of calcium ions in their prey's nerve cells, thereby preventing the neurons from functioning normally....[More]
Cone snails have one of the most potent venoms known, which they use to paralyze small fish by blocking the movement of calcium ions in their prey's nerve cells, thereby preventing the neurons from functioning normally. In 2004 the U.S. Food and Drug Administration approved a synthetic drug called Prialt, which is based on the venom of from Conus magus and is used to treat chronic pain. Jon-Paul Bingham, a neuroscientist at Clarkson University in Potsdam, N.Y., told the BBC that "these snails are nature's pharmaceutical drug designers.... We estimate there are 75,000 compounds out there that could have some potential use in all kinds of applications." [Less] [Link to this slide]
In 1977 researchers proved that an extract from the Pacific yew tree, paclitaxel ( Taxol ), had the potential to fight tumors , and conservationists worried it would require the harvesting of 360,000 trees every year....[More]
In 1977 researchers proved that an extract from the Pacific yew tree, paclitaxel (Taxol), had the potential to fight tumors, and conservationists worried it would require the harvesting of 360,000 trees every year. The compound was eventually synthesized from European yew needles, and Taxol became the most successful anticancer drug of its day, earning Bristol-Myers Squibb Co. some $9 billion. But controversy erupted again after a congressional investigation revealed in 2003 that the government had spent over $183 million to fund Taxol research, and only had recouped $35 million in royalties. "Medicare has paid more than a half billion taxpayer dollars to buy a taxpayer-funded drug for the taxpayers who funded it," Sen. Ron Wyden (D–Ore.) once complained. [Less] [Link to this slide]
The antimalaria drug Artemisinin comes from the Chinese wormwood tree, but until recently it was far too expensive for use in fighting malaria in Africa and other developing countries....[More]
The antimalaria drug Artemisinin comes from the Chinese wormwood tree, but until recently it was far too expensive for use in fighting malaria in Africa and other developing countries. Then, synthetic biologist Jay Keasling of the University of California, Berkeley, coaxed a yeast to synthesize it. In 2004 the company he co-founded, Amyris Biotechnologies, brought the price down from $2.40 per dose to less than a quarter, revealing how powerful a role synthetic biology can play in bringing natural medicines to market. [Less] [Link to this slide]
Discovered in soil fungus on Easter Island in the Pacific, rapamycin is an immunosuppressant long used to prevent organ rejection in transplant patients, but it is now finding applications in a wide variety of other maladies....[More]
Discovered in soil fungus on Easter Island in the Pacific, rapamycin is an immunosuppressant long used to prevent organ rejection in transplant patients, but it is now finding applications in a wide variety of other maladies. This week in Nature, scientists demonstrated that it could increase lifespan in mice by 30 percent. Other researchers have shown it may be able to fight cancers, such as Kaposi's sarcoma, and prevent epileptic seizures in children. And last month, Emory University scientists reported that rapamycin can make vaccines more effective and longer lasting by boosting the immune system's memory. [Less] [Link to this slide]
The human whipworm ( Trichuris trichiura ) afflicts some 500 million people worldwide with diarrhea, anemia and even rectal prolapse, but David Pritchard of the University of Nottingham in England says we should be taking a closer look at it for its ability to moderate inflammatory bowel disease....[More]
The human whipworm (Trichuris trichiura) afflicts some 500 million people worldwide with diarrhea, anemia and even rectal prolapse, but David Pritchard of the University of Nottingham in England says we should be taking a closer look at it for its ability to moderate inflammatory bowel disease. In fact, Pritchard, a parasitologist, argues that drugmakers should be investigating other pathogenic organisms, including anthrax and the yeast that cause vaginal infections, in order to understand how they suppress the human immune system. Understanding that trick can help assist transplant patients and asthma sufferers threatened by the immunological response of their own bodies. [Less] [Link to this slide]
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7 Comments
Add Comment"...it may soon be possible to automatically separate all of the chemicals in an organism..." Is that really what is needed to find treatments that work? Natural products are often effective because they contain multiple compounds working together. It works a bit like tritherapy drugs for AIDS.
Reply | Report Abuse | Link to thisMoreover, we don't need Big Pharma to patent natural products. We need public funding for unpatented medical research.
The natural world does contain untold millions of bioactive compounds. However, the usual approach to drug discovery goes something like this: 1) somebody isolates a few mg of a compound from a plant and disocovers it has some biological activity - there is rarely enough available to test it properly; 2) chemists attempt to synthesise the natural product, this often takes years of work; 3) the resulting array of molecules is tested, if they are too toxic or otherwise not suitable, all this work has effectively been wasted. Also it is often not known how natural products work in the body - much of the complex structure of a natural product can be unecessary or even contribute to side effects or solubility problems.
Reply | Report Abuse | Link to thisRecently a new approach based on detailed biological study has been used - the anti-flu drug relenza was developed specifically to inhibit an enzyme active site on the surface of the flu virus once the structure of both the site and the substate that normally binds there were known by crystallography. With increased biological understanding it makes sense to design drugs by this rational procedure rather than the hit and miss natural product synthesis and testing approach.
I'm not saying that natural products are valueless, and I'm the first to admit that natural biosynthesis processes have a lot to teach us but I think it is inevitable that a drift away from the use of natural products (either isolated or synthetic) as drugs is inevitable and beneficial.
More than half of all drugs are derived from a living organism, yet mankind is destroying the natural world at a stunning rate. I have no doubt the cure to many dreaded diseases exist in Mother nature's pharmacy, but we may lose them before they can be discovered. Also, if the pharma. companies would provide local communities with roaylties this would incentivize nations to preserve their biodiversity. However, I realize this is probably asking too much of capitalism.
Reply | Report Abuse | Link to thisNatural compounds are not necessarily complex. There are quite a number of small molecules. An isolated active compound can be structurally modified so that the new compound may be patented and have higher potency.
Reply | Report Abuse | Link to thisNice post!
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Reply | Report Abuse | Link to thisWht is the importance of investigating MAPK and NF-kappakb pathways actvation of raw cell line by antigens....?
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