Regulation of schizonticide activity

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Quinidine and quinine have schizonticide activity due to the inhibition of nucleic acid synthesis through DNA intercalation. This activity is also based on carbohydrate metabolism. The action of both of these alkaloids is a result of their binding to sarcoplasmic reticular vesicles and the resulting reduced uptake of Ca2+. These alkaloids are also active on Na+ and K+-ATPase, both in an encouraging or inhibiting sense. Both alkaloids therefore have been developed as strong anti-malarial products. The basic product used has been quinine, and quinidine has been an alternative. These applications are currently decreasing in popularity because some malaria-causing agents (e.g. Plasmodium spp.) exhibit resistance. Modifications of these alkaloids or the finding of new molecules with anti-malarial properties is necessary for the process to develop. These alkaloids may have other applications as well. Quinidine is an antiarrhythmic agent, and quinine is used in the treatment of myotonic disorders.

2. Alkaloids as drugs

Medical applications of alkaloids have led to the production of drugs and drug components. They can be based on pure natural alkaloids, as in the case of extracts. Purified alkaloids, partially and even totally synthesized compounds based on the natural alkaloid structure, are also used. Chemically modified alkaloids are yet another example. Chemically modifying the structure affects biological activity. The general trend in modern medicine is to develop compounds that are biologically more active than those found in nature. This is achieved in many cases by alkaloid modifications and synthesis. However, natural compounds themselves are very important because they are the basis for artificial drugs. Moreover, alkaloids used as natural products are important in phytomedicine, alternative medicine and homeopathy. Still today, folk- and ethnomedicine rely heavily on their use.

Aconitine-, ajmaline- and sanguinarine-based drugs have medicinal importance and are dosed clinically. The drugs are medical products developed by the pharmaceutical industry. Physicians have the right to determine the prescription, that is the use of these products and determination of dosage. Pharmecuticals based on these alkaloids are relatively strong. Several researched and patented drugs such as Aconitysat (aconitine) and Rauwopur (ajmaline) can be found on the pharmaceutical market today. Sanguinarine is generally used in toothpastes. Toothpaste generally has no side effects along with its anti-cavity properties.

Atropine-, hyoscine- and hyoscyamine-based drugs are developed on a large scale and they also have a variety of clinical purposes. Atropinol, for example, is based on atropine. This drug contains atropine sulphate. Another example is Buscopan, based on hyoscine. Hyoscyamine is used in transdermal plasters. Bella sanol also contains hyoscyamine. The therapeutic use is similar to that of atropine. At least 50 different products from these alkaloids have been developed and introduced on the pharmaceutical market.

Drugs based on eserine, galanthamine, nicotine, lobeline and tubocurarine are also prominent. Two examples of drugs containing eserine are Anticholium and Pilo-Eserin. There are at least 20 different products based on this alkaloid.

Nivalina is one drug that contains galanthamine. There are others as well, but less so than with the eserine drugs. Galanthamine-containing medicines have potential uses in the treatment of Alzheimer's disease. Because of this, a greater number of products containing galanthamine is expected to reach the market.

Nicotine is used in many products on the pharmaceutical market, for example Nicorette or Nicoderm. At least 20 different products are known to contain nicotine. These drugs are delivered in different forms. One of these is a transdermal plaster. Nicotine chewing gum and tablets are also available. These drugs are used especially to reduce nicotine cravings.

The drugs that contain lobeline are, for example, Stopsmoke or Lobatox. These products are used for similar purposes as drugs that contain nicotine.

Tubocurarine-containing drugs such as Tubarine or Jexin are used in surgical procedures as muscle relaxants.

Alkaloids such as boldine, codeine, narceine and morphine are also important in clinical practice. Boldosal and Oxyboldine are good examples of boldine-based drugs with morphine-like properties.

Codeine is a component of at least 250 pharmeaceutical products on the market. Codicaps or Codipront can be mentioned as examples. All of these products are opium derivatives.

Narceine-containing drugs are similar to those of codeine. They are used to treat coughs. Paneraj is an example of a typical trademark.

There is a long list of morphine-containing drugs. These drugs are used in serious instances, for example in cases of surgical operations and post-operation treatments. Morphalgin and Spasmofen are examples.

The alkaloids ephedrine, ergotamine, ergometrine and yohimbine are used in many forms. Products like Dorex or Endrine contain ephedrine as their major component. They are used for many purposes, including treating nasal cold symptoms or in bronchial asthma. More than 25 different drugs containing ephedrine have been developed today.

Ergotamine is an active alkaloid produced by fungi with many applications on the market. Pharmauceticals such as Ergostat or Migral are typical examples of ergotamine-based products. Drugs containing this alkaloid are used widely in the treatment of migraines.

Ergometrine is also an ergot alkaloid. It can be found in several products on the market, including Ergometron and Syntometrine.

Yohimbine can be found in drugs such as Aphrodyne or Yohimex. About 20 different products containing this alkaloid have been developed. These drugs are aphrodisiacs used to treat impotency and impotency-related problems in men.

Many other alkaloids are used with various applications. One of them is strychnine, an alkaloid known to be strongly toxic to animals. Drugs such as Dysurgal or Pasuma contain strychnine in clinical doses. Strychnine-containing drugs are used in many disorders, including those of the eye.

Vinblastine and vincristine are two further examples of important drug constituents. Vinblastine is found in such drugs as Periblastine or Velban, and vincristine in such drugs as Norcristine or Pericristine. These drugs are used in oncology as cancer treatments. Drugs with vinblastine are also used in the treatment of Hodgkin's disease, and those containing vincrastine in the treatment of Burkitt's disease as well as brain and lung tumours.

Many other alkaloid-based medicines exist. Drugs based on berberine are used in the treatment of infections as well as in the treatment of AIDS.

Stimulant drugs are often based on caffeine, cathine, theobromine and theophylline. Caffeine is a component of more than 300 different drugs. It is also a minor component in many other pharmaceuticals. Analgen or Panax are examples of caffeine-based drugs. Cathine is found in drugs such as Amorphan or Recatol. They have an anorectic influence of the liver. More than 25 different drugs have been developed from theobromine, for example Atrofed and Seominal. These drugs serve many clinical purposes including treating asthma and Angina pectoris. Moreover, 200 different drugs have been developed from theophylline. Theochron and Euphyllin are examples. Theophylline-containing drugs are used to treat bronchitis and asthma.

The applications containing quinidine and quinine are very well known and relatively old. Drugs such as Quinidex or Quinalan are good examples of quini-dine applications. Quinine can be found in drugs such as Adaquin or Biquinate. These drugs are important in the prevention and treatment of malaria.

3. Agricultural applications

The alkaloids are known in food and agricultural production. Many crops contain these compounds. In food crops these molecules are a problem and topic of discussion due to possible health hazards and the fact that they have to be removed from plants by breeding and especially hybridization. Alkaloid-rich (bitter) and alkaloid-poor (sweet) cultivars are developed as a result. Both kinds of cultivars are needed for different purposes (Table 24). The total removal of alkaloids through breeding is not currently possible. However, it is possible to reduce alkaloid content to such levels that plant material is suitable for use in foraging and feed. The other way of the removing of alkaloids from plant material is via industrial processing. It is possible to completely remove alkaloids from raw plant material via technological means. Such kinds of industrial processing can be found in the food industry. Alkaloids are no longer problematic in the case of processed feed or fodder. However, problems still exist when fresh or unprocessed raw material is used.

The possibility of developing physiologically functional foods using botanicals is presently a major discussion point in many countries. Alkaloids as such botanicals are difficult compounds solely for the reason of their strong bio-activity. On the other hand, this bioactivity can be used in the development of feed and food. However, physiologically functional foods should not be too chemically strong, and doses have to be much more slight that clinic doses. Moreover, one of the possibilities for the potential use of the alkaloids in the food is developing of the so-called "natural, plant-based vaccines". The development of these kinds of applications is notable. Genetically modified plants

Table 24 Potential usage of alkaloid-rich and alkaloid-poor Washington lupine (Lupinus polyphyllus Lindl.) in agriculture

Potential Product

Alkaloid-Rich Genotype

Alkaloid-Poor Genotype

Biological pesticides

Lupanine as major

alkaloid

Biological fertilizers

Alkaloid extract

Organic matter

Biogas heat composts

Biomass with alkaloids

Biomass

Plant management

Seeds, saplings, vaccines

Seeds, saplings, vaccines

of Bradyrhizobium

of Bradyrizobium

Plant industry

Seeds, sapling

Seeds, saplings

Amino acids

Protein tablets3

Protein tabletsa

Fibre

Fibre diet tabletsa

Fibre diet tabletsa

Aroma substances

Flavouringsa

Flavouringsa

Feed components

High-content protein

High-content protein feed

feeda

Note: a Using technological processing. More details in the source (Ref. [348]).

Note: a Using technological processing. More details in the source (Ref. [348]).

(GMP) can contain additional genes and produce new proteins594. Alkaloids as botanicals can be therefore produced in the plants in which they usually do not exist. In the treatment of diseases such as cancer or AIDS, plant (food) vaccines are reasonable to develop.

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