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Investigation of Host-guest Complexation Between 4-Sulfonylcalix 6 Arene and 15 Alkaloids from Traditional Chinese Medicines and Inhibitory Effect of Binding System on Proliferation of HepG2 and H9c2 Cells / 中国实验方剂学杂志
Chinese Journal of Experimental Traditional Medical Formulae ; (24): 119-126, 2021.
Article in Chinese | WPRIM | ID: wpr-906308
ABSTRACT

Objective:

To investigate bonding ability between 4-sulfonylcalix [6] arene (SCA6) and 15 alkaloidsmatrine, allomatrine, dauricine, daurisoline, quinidinequinine, crotaline, vincristine, gelsemine, koumine, tetrandrine, aloperine, oxymatrine, sophocarpine and sinomenine), and to evaluate viability<italic> in vitro</italic> of HepG2 and H9c2 cells with 12 alkaloids/SCA6 bonding systems (except allomatrine, oxymatrine, sinomenine).

Method:

Fluorescence competitive titration was used to determine the binding constants of alkaloids and SCA6, the inhibitory effect of alkaloid/SCA6 complex on proliferation of HepG2 and H9c2 cells was investigated by cell counting kit-8 (CCK-8).

Result:

All the 15 alkaloids had good bonding with SCA6 at the ratio of 1∶1 (the binding constants >1×10<sup>5</sup> mol·L<sup>-1</sup>, <italic>R</italic><sup>2</sup>>0.98), the aloperine (quinolizidine alkaloids) and SCA6 had the biggest binding constant (20.55×10<sup>6</sup> mol·L<sup>-1</sup>). In addition to gelsemine, crotaline, matrine and sophocarpine, 8 alkaloids (including aloperine, tetrandrine, dauricine, daurisoline, quinidinequininevincristine and koumine) exhibited significant anti-tumor effects on HepG2 cells. Except for daurisoline, the anti-proliferation effect of the other 11 alkaloids before and after binding with SCA6 had no difference in HepG2 cells. In addition to gelsemine, crotaline, matrine and sophocarpine, the anti-proliferation effect of the other 8 alkaloids before and after binding with SCA6 had no difference in H9c2 cells.

Conclusion:

SCA6 shows intense binding ability with bisbenzylisoquinolinequinolizidine and indole alkaloids. It can improve the solubility of alkaloids without affecting their anti-tumor activity, which provides a reference for subsequent related applications of SCA6 as a drug delivery carrier.

Full text: Available Index: WPRIM (Western Pacific) Language: Chinese Journal: Chinese Journal of Experimental Traditional Medical Formulae Year: 2021 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Language: Chinese Journal: Chinese Journal of Experimental Traditional Medical Formulae Year: 2021 Type: Article