| Description: |
Convolvine and its derivatives exhibit pronounced antihypoxic, immunomodulating, and anti-inflammatory activity, they exhibit cytotoxic activity, the alkaloids N-benzylconvolvine and N-chloroacetylconvolvine at concentrations of 10 ug/mL exhibit the greatest activity against HeLa and Hep cancer cell cultures. Convolvine blocks the M-receptors of the heart and intestine but raises the sensitivity of the M-receptors of the salivary gland and of the CNS,convolvine has revealed characteristics of a sedative and nootropic agent. |
| Targets: |
Immunology & Inflammation related |
| In vitro: |
| Chemistry of Natural Compounds,2011,47(4): 608-11. | | Derivatives of the alkaloid convolvine and their pharmacological activity[Reference: WebLink] |
METHODS AND RESULTS:
The alkaloid contents of Convolvulus subhirsutus and C. pseudocanthabrica growing in various regions of Uzbekistan, Kazakhstan, and Tadzhikistan were previously investigated and were found to include ~10 tropane alkaloids [ 1 , 2 ]. The alkaloid composition and content depended on the habitat. Thus, total alkaloids in C. subhirsutus growing in Uzbekistan was 0.6–0.75% (aerial part) and 0.6–1.6% (roots) [ 2 , 3 ]; in Tadzhikistan, 0.12%(aerial part) [ 4 ]. The main alkaloids in all plants were nortropine derivatives convolvine ( 1 , 3,4-dimethoxybenzoyloxynortropane) and Convolamine (3,4-dimethoxybenzoyloxytropane), which amounted to 40–50% of the total. The alkylation and acylation of the NH group in 1 were studied [ 3 ].
CONCLUSIONS:
Preliminary tests showed that the synthesized compounds included some with pronounced antihypoxic, immunomodulating, and anti-inflammatory activity. | | Chemistry of Natural Compounds, 2013,48(6):1039-41. | | Synthesis of convolinine and cytotoxic activity of alkaloids of the genus Convolvulus and their derivatives[Reference: WebLink] | The minor base convolinine was synthesized.
METHODS AND RESULTS:
The activity of alkaloids from plants of the genus Convolvulus and their derivatives against HeLa and Hep cancer cell cultures and primary fibroblast culture was studied. It was found that the alkaloid Convolvine and its derivatives exhibited cytotoxic activity.
CONCLUSIONS:
The alkaloids N-benzylConvolvine (4) and N-chloroacetylConvolvine (5) at concentrations of 10 μg/mL exhibited the greatest activity against HeLa and Hep cancer cell cultures. The percent suppression of HeLa cervical carcinoma cells by alkaloid 4 was 35%; of Hep laryngeal cancer cells, 81.6%. |
|
| In vivo: |
| Chemistry of Natural Compounds,1998,34(1):56-8. | | Neuro- and psychopharmacological investigation of the alkaloids convolvine and atropine[Reference: WebLink] | It has been established that Convolvine blocks the M-receptors of the heart and intestine but raises the sensitivity of the M-receptors of the salivary gland and of the CNS, while atropine blocks all the abovementioned M-receptors.
METHODS AND RESULTS:
Convolvine has revealed characteristics of a sedative and nootropic agent. Atropine, however, which is known as a psychomotor stimulator, prevents the realization of a conditioned gastromotor reflex. An analysis has been made of the relationship between features of the pharmacological activities and chemical structures of Convolvine and atropine. |
|
Cell. 2018 Jan 11;172(1-2):249-261.e12. doi: 10.1016/j.cell.2017.12.019.IF=36.216(2019)
Cell Metab. 2020 Mar 3;31(3):534-548.e5. doi: 10.1016/j.cmet.2020.01.002.IF=22.415(2019)
Mol Cell. 2017 Nov 16;68(4):673-685.e6. doi: 10.1016/j.molcel.2017.10.022.IF=14.548(2019)
ACS Nano. 2018 Apr 24;12(4): 3385-3396. doi: 10.1021/acsnano.7b08969.IF=13.903(2019)
Nature Plants. 2016 Dec 22;3: 16206. doi: 10.1038/nplants.2016.205.IF=13.297(2019)
Sci Adv. 2018 Oct 24;4(10): eaat6994. doi: 10.1126/sciadv.aat6994.IF=12.804(2019)
