- Introduction
- History
- Natural Drug Leads
- Combinatorial Approach
- Discoveries
- Conclusion
- References
- Contact Us
Natural Drugs
Many organisms produce unique compounds to protect themselves from their predators, parasites, and diseases. These compounds, once isolated, provide an effective starting point for drug design because they already have relevant biological activity. The best sources of natural leads are especially diverse environments where increased competition leads to a higher diversity of compounds.
Tropical forests are a well known source of drug leads with
exceptional biodiversity, even though they remain largely untapped
resources of lead compounds. Less than 5% of all plant species have
been screened for drug leads, and less than 0.1% of all animal species
have been examined. In spite of this low absolute coverage, 70% of
plants with known anti-cancer properties are found only in tropical
forests.
Studies from 1981 to 2002 for recent drug discoveries shows that new chemical entities derived from plant sources valued at 10% (Applied Chem.). This shows that there is a huge untapped potential with natural plant sources that remains untapped.
Studies from 1981 to 2002 for recent drug discoveries shows that new chemical entities derived from plant sources valued at 10% (Applied Chem.). This shows that there is a huge untapped potential with natural plant sources that remains untapped.
Deforestation of rainforests creates a real problem for drug discovery from natural leads. By destroying these biologically diverse regions, it is possible that new, undiscovered sources of drugs could be wiped out. With the increasing rates of deforestation and with so few of plants in this environment being screened for active ingredients, it is highly likely that new, natural drug leads will be lost if deforestation continues.
Microorganisms are another potent source of drug leads. In order to establish themselves in an environment, many produce anti-microbial agents to eliminate competitors. In addition, less than 1% of bacterial and 5% of fungal species are known. The classic example of such a drug discovery is the that of penicillin by Alexander Fleming from a mold that grew by accident from a contaminated experiment.
Very recently, the study of marine microorganisms, invertebrates, and vertebrates has led to new drug leads; the first marine-derived drug being approved in 2004. Compounds from these animals see applications in anti-pain, anti-inflammatory, and anti-cancer drug design. Less than 0.5 percent of the marine animals have received even a cursory effort to detect antineoplastic constituents. Thus, the most important marine animal and microorganism anticancer drug still await discovery. Furthermore, these natural products are a result of 3.8 billion years of evolutionary biosynthetic organic reactions aimed at even more specific molecular design and targeting. The net result of these trillions and trillions of biologically‐directed organic reactions (biosynthetic combinatorial processes) is an astronomical number of candidates for use as anticancer drugs and as drugs necessary across most medical indications. But they need to be discovered and developed to the clinic. Discoveries of active ingredients have been found in the Bryostatins, Dolastatins, Auristatins. As well as preclinical drugs have been developed from the spongistatins and cephlostatins. The discovery of new drugs based on marine organism constituents represents an exceedingly productive and exciting frontier for making great advances in medicine.
Very recently, the study of marine microorganisms, invertebrates, and vertebrates has led to new drug leads; the first marine-derived drug being approved in 2004. Compounds from these animals see applications in anti-pain, anti-inflammatory, and anti-cancer drug design. Less than 0.5 percent of the marine animals have received even a cursory effort to detect antineoplastic constituents. Thus, the most important marine animal and microorganism anticancer drug still await discovery. Furthermore, these natural products are a result of 3.8 billion years of evolutionary biosynthetic organic reactions aimed at even more specific molecular design and targeting. The net result of these trillions and trillions of biologically‐directed organic reactions (biosynthetic combinatorial processes) is an astronomical number of candidates for use as anticancer drugs and as drugs necessary across most medical indications. But they need to be discovered and developed to the clinic. Discoveries of active ingredients have been found in the Bryostatins, Dolastatins, Auristatins. As well as preclinical drugs have been developed from the spongistatins and cephlostatins. The discovery of new drugs based on marine organism constituents represents an exceedingly productive and exciting frontier for making great advances in medicine.