In all kinds of organisms, there are many active substances throughout the whole life process. Compounds with five-membered heterocyclic units of styrene and propylene are one of them. Among these natural products, indole ring compounds play an important role. They mainly exist in nature in the form of alkaloids.
Indole is related to "India". In 1866, indole was first obtained from 2-hydroxy indole by zinc powder treatment. Indole is formed by the condensation of two carbon atoms in the benzene and pyrrole rings, so it is also called benzopyrrole. The chemical shifts of protons on the indole ring are not completely equal. Indole is a colourless flake crystal with strong fecal odor. Indole is aromatic and its electrophilic substitution activity is higher than benzene. In the indole molecule, because the pyrrole ring is not as stable as the benzene ring, the addition and substitution reactions mostly occur on the pyrrole ring, especially the substitution reactions occur on the three positions of the indole. Indole is an intermediate for the production of tryptophan, and is also a raw material for the production of a series of pharmaceuticals, bioactive substances, dyes, spices and chemical products, and has a wide range of uses.
Indole derivatives have shown tremendous applications in medicine. Indomethacin, also known as indomethacin, is an African anti-inflammatory drug. It was marketed in 1963 and has been used in clinic for more than 30 years. Indomethacin has antipyretic, analgesic and anti-inflammatory effects by inhibiting the synthesis of prostaglandins in vivo. It is one of the commonly used drugs and is used as a standard drug for evaluating non-margin anti-inflammatory drugs. Clinically, it is used to treat various types of rheumatism, rheumatoid arthritis, glomerulonephritis, Bater syndrome, orthostatic hypotension, dysmenorrhea, migraine, biliary colic, various kinds of tumor fever, non-specific low fever, ophthalmic diseases, urinary system and pediatric diseases.
Tryptophan prepared from indole is mainly used to treat depression, as a nutritional agent, essential amino acid tablets for artificial diet, as well as additives for infusion and protein hydrolysis, such as Figure 1.3. At the same time, tryptophan can be converted into many important physiological substances in the body, such as nicotinic acid, one of the B vitamins. If both of them are insufficient, it will cause epilepsy tryptophan in the body to produce 5-antelope tryptophan, the precursor of neurohormone by the action of vitamin B6, thus promoting sleep and mental stability. It has been used in healthy food and psychotropic drugs.
Tryptophan can be used as an antidepressant, useful for brain metabolism, and even as a hypnotic.
In addition, the indole unit exists in more than 1,000 known alkaloids in nature. It is the most widely discovered alkaloids, accounting for about one fourth of known alkaloids. Its structure is generally more complex, and it has many significant or important biological pharmacological activities. Commonly used hypotensive drug reserpine is a complex indocyanine derivative; Changchun alkaloid (vinblastine) is a kind of double indole alkaloid, soluble in chloroform, acetone and ethanol, insoluble in water and petroleum ether: vincristine (vincristine), also known as aldehyde Changchun base and new Changchun base, can be anticancer, its curative effect is about 10 times higher than that of Changchun alkali, vincristine is also a kind of bis indole alkaloid.
The simple alkaloid indole-3-monoacetic acid widely exists in various organisms. It is a plant growth stimulin, commonly known as auxin, widely exists in various plants. It is an essential factor for promoting plant growth and development, especially for rooting of plant cuttings. Studies have shown that its mechanism of action is related to the synthesis of RNA and protein. Because of the various physiological activities of a large number of indole alkaloids, people not only use plants containing them to treat diseases, but also directly use the extracted alkaloids to treat diseases, and carry out structural modification to find more drugs.
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