INDOLE ALKALOIDS AND THEIR ANALOGUES: BIOLOGICAL ACTIVITY STUDY

DOI: https://doi.org/10.29296/25877313-2018-09-01
Issue: 
9
Year: 
2018

O.N. Tolkachev Dr.Sc. (Chem.), Professor, All-Russian Research Institute of Medicinal and Aromatic Plants (Moscow) E-mail: vilarnii@mail.ru V.N.Tolkachev Ph.D. (Chem.), Leading Research Scientist, N.N.Blokhin National Scientific Medical Oncological Center (Moscow) O.P. Sheichenko Ph.D. (Chem.), Head of Phytochemistry Department, All-Russian Research Institute of Medicinal and Aromatic Plants (Moscow) E-mail: vilarnii.sheichenko@mail.ru T.V. Fateeva Head of Microbioligical Laboratory, All-Russian Research Institute of Medicinal and Aromatic Plants (Moscow) E-mail: fateeva2551@mail.ru A.V. Semenov Ph.D.(Med.), Moscow Scientific Institute of Pediatry and Child’s Surgery, Public Health Ministry (Moscow) E.A. Abizov Dr.Sc. (Pharm.), Associate Professor, Leading Research Scientist, Research Center of Medical Application, Ministry of Public Health (Moscow)

Review on biological activity study of indole alkaloids possessed antitumor action studied in VILAR, FGBU «NMIC N.N.Blokhin oncology, Public Health Ministry, Russia, NII Pediatry, Scientific Center. Expertise of Medicinal Use and the prospects of their use in medicine is discussed. Natural indol al-kaloids were studied on antitumor activity. Derivatives of substituted indole-2-carboxylic acid: 1-(3,4,5-triacetoxybenzoyl)-2-methoxycarbonyl-indole (IIа), 1-(3,4,5-trimetoxybenzoyl)-indole-2-carboxylic acid (IIb), 1-(3,4,5-trimetoxybenzoyl)-2-ethoxycarbonyl-indole (IIc), 2-ethoxycarbonyl-5-methoxy-indole (IId) were synthesized. Their inhibitory action on cytoskelet dependent cell functions is studied. There were found that inhibitory action on capping of in-dole derivatives were comparative with that of the most active compounds IIa, IIb and IId. In vivo study of the compounds Ia and IId were shown to be equal in activity with cytochalasin B at the concentrations 10-5-10-6, while Zaditen and DMSO were not active at these concentrations. Simple synthetic indole analogues of cytochalasins without macrocyclic lactone fragment were produced. The compounds were studied on sup-pression of systemic anaphylactic reaction in sensitized with horse serum on guinea pigs. The compounds 5 and 19 were shown in vivo to increase surviv-ing in all subgroups of experimental animals (45.5%). The compound 5 possessed the minimal toxic index among indole derivatives tested.

Keywords: 
indole alkaloids of Catharanthus roseus
of Vinca minor
of Claviceps purpurea
of Elaeagnus angustifolia
ß-carboline alkaloids
galloyl-indoles
their derivatives
analogues of cytochalazines B and D
biological activity

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