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Natural products in therapy. Prospects, goals and means in modern research.

A review is presented which shows the vegetable kingdom as an almost inexhaustible reservoir of potential drugs. Some historical aspects about the use of plants and their constituents in medicine are dealth with. A number of problems connected with the search for new prototype drugs of biological origin is reported as well as modern methods used in this promising research. Some examples are given concerning recent results of investigations of plants used in traditional and modern medicine in China. Special attention is paid to the present role of natural products in therapy: as biologically active compounds as such, as starting materials for (semi)synthetic drugs and, last but not least, as source of inspiration or as models for the synthesis of new drugs with better therapeutic, chemical or physical properties than the original compounds.

Animals↗

Diversifying microbial natural products for drug discovery.

Historically, nature has provided the source for the majority of the drugs in use today. More than 20,000 microbial secondary metabolites have been described, but only a small percentage of these have been carried forward as natural product drugs. Natural products are in tough competition with large chemical libraries and with combinatorial chemistries. Hence, each step of a natural product program has to be more efficient than ever, starting from the collection of environmental samples and the selection of strains, to metabolic expression, genetic exploitation, sample preparation and chemical dereplication. This review will focus on approaches for diversifying microbial natural product strains and extract libraries, while decreasing genetic and chemical redundancy.

Bacteria↗

Marine pharmacology in 2000: marine compounds with antibacterial, anticoagulant, antifungal, anti-inflammatory, antimalarial, antiplatelet, antituberculosis, and antiviral activities; affecting the cardiovascular, immune, and nervous systems and other miscellaneous mechanisms of action.

During 2000 research on the pharmacology of marine chemicals involved investigators from Australia, Brazil, Canada, Egypt, France, Germany, India, Indonesia, Israel, Italy, Japan, the Netherlands, New Zealand, Phillipines, Singapore, Slovenia, South Korea, Spain, Sweden, Switzerland, United Kingdom, and the United States. This current review, a sequel to the authors' 1998 and 1999 reviews, classifies 68 peer-reviewed articles on the basis of the reported preclinical pharmacologic properties of marine chemicals derived from a diverse group of marine animals, algae, fungi, and bacteria. Antibacterial, anticoagulant, antifungal, antimalarial, antiplatelet, antituberculosis, or antiviral activity was reported for 35 marine chemicals. An additional 20 marine compounds were shown to have significant effects on the cardiovascular and nervous system, and to possess anti-inflammatory or immunosuppressant properties. Finally, 23 marine compounds were reported to act on a variety of molecular targets and thus could potentially contribute to several pharmacologic classes. Thus, as in 1998 and 1999, during 2000 pharmacologic research with marine chemicals continued to contribute potentially novel chemical leads to the ongoing global search for therapeutic agents in the treatment of multiple disease categories.

Anti-Bacterial Agents↗

Therapeutic potential of plant photosensitizers.

Many bioactive phytochemicals have been shown in recent years to be photosensitizers, i.e. their toxic activities against viruses, micro-organisms, insects or cells are dependent on or are augmented by light of certain wavelengths. These activities are often selective, and this has led to the concept of therapeutic prospects in the control of infectious diseases, pests and cancer. Reaction mechanisms commonly involve singlet oxygen and radicals, which are thought to cause photodamage to membranes or macromolecules. The main classes of plant photosensitizers reviewed here are polyyines (acetylenes, thiophenes and related compounds); furanyl compounds; beta-carbolines and other alkaloids; and complex quinones. We propose that within each group of phytochemicals there are several representatives that merit further study for therapeutic abilities in appropriate animal models.

Animals↗

Jaborandi: an interdisciplinary appraisal.

In spite of many references to Pilocarpus Jaborandi Holmes in ethnological and botanical sources and suggestions of its employment for a variety of diseases, it has not been possible to pin down the use of its leaves to any particular purpose amongst South American Indians. While the medically important jaborandis are species of Pilocarpus, it is true that this vernacular name is commonly applied to other rutaceous and numerous piperaceous plants as well. The introduction of jaborandi leaves to western medicine goes back to 1873, when Symphronio Coutinho went to Europe, taking with him samples of the leaves. The copious sweating and salivation brought about by the leaves attracted the attention of French physicians. Soon jaborandi leaves were being employed in the treatment of many diseases. In 1875, Hardy and Gerrard independently discovered the alkaloid pilocarpine. Most therapeutic applications of jaborandi leaves and pilocarpine fell into disuse and were discontinued. What remained was the use of the latter in ophthalmology, where it had been introduced as a miotic by Weber in 1876. The mixture of pilocarpine and another natural product, physostigmine, remains to this day one of the mainstays in ophthalmology.

Alkaloids↗

Medicinal and toxic plants from Equatorial Africa: a pharmacologic approach.

The pharmacological approach to the study of plants used in traditional medicine is discussed. On the basis of personal experience in the Republics of Congo and Central Africa the author finds only a very small percentage of non-active plants among those used in traditional medicine. Some previously unknown plants are reported.

Africa, Central↗

Traditional medicine in Latin America, with particular reference to Mexico.

The present research on Mexican traditional medicine points to the resources made available by the Mexican Institutions for the study of the plants used in popular medicine which, in rural areas, follows the Aztec and Maya traditions. The most interesting feature of traditional medicine is its partial integration with many elements of modern medicine. The study of medicinal plants has been undertaken mostly by a research institute, IMEPLAM, which, under the auspices of CEESTEM, has information on computer on over 500 plants. The screening of these plants in progress with the aim of evaluating their therapeutic properties, both at the pharmacological and chemical level.

Latin America↗

Medicinal plants in Colombia.

The botanical aspects of the plants of Colombia have been studied thoroughly since the 18th century. Nevertheless, although plants are used to a large extent in traditional medicine in Colombia, there has been little investigation into their properties. Some research has not been initiated. This work is supported by the existence of the National Herbarium in Bogotá, in which there are 180 000 specimens belonging to 10 000 different species.

Colombia↗