Development from natural products

Nature has been a potential source of therapeutic agents for thousands of years. An impressive number of modem dmgs have been derived from natural sources. Over the last century, a number of top selling dmgs have been developed from natural products. Anticancer dmg vincristine from Vinca rosea, narcotic analgesic morphine from Papaver somniferum, antimalarial dmg artemisinin from Artemisia annua, anticancer dmg Taxol from Taxus brevifolia and antibiotic peniciUins from Penicillium ssp. are just a few examples. 

Cragg GM, Newman DJ (2005) Drug discovery and development from natural products the way forward. In 11th NAPRECA symposium book of proceedings, Antananarivo, Madagascar, pp 56-69... 

Gilani AUH (1998) Novel developments from natural products in cardiovascular research. Phytother Res 12 S66-S69... 

Gordon, M. C., David, J. Newman drag discovery and development from natural products. In The Wcty Forward, IlthNAPRECA Symposium Book of Proceedings, Pcatsamtanvo. Madagascar, 2005, pp. 56-69. 

These chemorational techniques have generated great interest in, and high expectations for, the acceleration of development of innovative pesticides. However, many purportedly successful appHcations of QSAR procedures have reHed on the quaHtative insights traditionally associated with art-based pesticide development programs. Retrospective QSAR analyses have, however, been helpful in identifying the best compounds for specific uses (17). Chemorational techniques have also found some appHcations in the development of pesticides from natural product lead compounds, the best known examples being the synthetic pyrethroid insecticides (19) modeled on the plant natural product, pyrethmm. 

A great deal of interest has been shown in the mass spectral analysis of natural products. In most cases it is desirable to develop techniques incorporating g.l.c. to enable the separation of the components obtained in extracts from natural products. The volatility required for g.l.c. is... 

Agrochemicals from Natural Products, edited by C. R. A. Godfrey Seed Development and Germination, edited by Jaime Kigel and Gad Galili Nitrogen Fertilization in the Environment, edited by Peter Edward Bacon Phytohormones in Soils Microbial Production and Function, William T. 

Irrational Approach This approach is the historical method of discovering and developing drugs. It involves empirical observations of the pharmacological effects from the screening of many chemical compounds, mainly those from natural products. The active component that gives rise to the observed effects is isolated. The chemical formula is determined, and modifications are made to improve its properties. This approach has yielded many drugs available today. 

In some cases, drug materials are isolated from natural products. In other cases, natural product extraction constitutes the raw material or intermediate for production of the drug via a semisynthetic route. Methods for chemical reactions, product purification, control parameters, and analytical procedures are developed and they form the basis for the chemistry, manufacturing, and control (CMC) information for regulatory application. 

Jones P, Steinkuhler C. (2008) From natural products to small molecule ketone histone deacetylase inhibitors Development of new class specific agents. Curr Pharm Des 14 545-561. 

Antihypertensive FOSHU products are accepted as a food that possesses ACE inhibitory action. So far, 120 antihypertensive or ACE inhibitory items have been developed from natural food materials such as sardine muscle, milk, dried bonito, sesame, seaweed and royal jelly (Table 1). 

Formidable chemical obstacles stood in the way of clinical development of these agents derived from natural products, notably in formulation of very poorly soluble compounds for intravenous infusion and in manufacture of bulk drug. For a time, production of Taxol from the bark of the Pacific Yew tree aroused public controversy, which became a story of nature and politics in pursuit of an anti-cancer drug [22]. 

Alkaloids are used as fertilizers for some crops. Mittex AG in Germany has developed a natural product, Lupinex, which contains quinolizidine alkaloids, minerals and carbohydrates. Lupinex has more than 9% N, 1% P and 2% K. The raw material for this natural product is a waste received from the lupin alkaloid remowing process, when the edible and non-edible components of food... 

The number of synthetically produced fragrance and flavor chemicals has since expanded continually as a result of the systematic investigation of essential oils and fragrance complexes for odoriferous compounds. Initially, only major components were isolated from natural products their structure was then elucidated and processes were developed for their isolation or synthesis. With the development of modern analytical techniques, however, it became possible to isolate and identify... 

Apart from natural-product-derived modem medicine, natural products are also used directly in the natural pharmaceutical industry that is growing rapidly in Europe and North America, as well as in the traditional medicine programmes being incorporated into the primary health care systems of Mexico, The People s Repuhhc of China, Nigeria and other developing countries. 

---