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1.
Bioorg Chem ; 138: 106657, 2023 09.
Artigo em Inglês | MEDLINE | ID: mdl-37302316

RESUMO

Ginsenoside 3ß,12ß,21α,22ß-Hydroxy-24-norolean-12-ene (G-M6), a phase I metabolite of anti-tumor medication 20(R)-25-methoxyl-dammarane-3ß,12ß,20-triol (AD-1), beats the parent drug in anti-ovarian cancer efficacy. The mechanism of action for ovarian cancer, however, is uncertain. Using network pharmacology, human ovarian cancer cells and nude mouse ovarian cancer xenotransplantation model, the anti-ovarian cancer mechanism of G-M6 was preliminarily explored in this study. The PPAR signal pathway is the key signal pathway of the G-M6 anti-ovarian cancer mechanism, according to data mining and network analysis. Docking tests demonstrated that the bioactive chemical G-M6 was capable of forming a stable bond with the PPARγ target protein capsule. Using human ovarian cancer cells and xenograft model of ovarian cancer to evaluate the anticancer activity of G-M6. The IC50 value of G-M6 was 5.83±0.36, lower than AD-1 and Gemcitabine. The tumor weight of the RSG 80 mg/kg group (C), G-M6 80 mg/kg group (I), and RSG 80 mg/kg + G-M6 80 mg/kg group (J) after the intervention was as follows: C < I < J. The tumor inhibition rates of groups C, I, and J were 28.6%, 88.7%, and 92.6%, respectively. When RSG and G-M6 are combined to treat ovarian cancer, q = 1.00 is calculated according to King's formula, which indicates that RSG and G-M6 have additive effects. Its molecular mechanism may involve the up-regulation of PPARγ and Bcl-2 protein expressions, and the down-regulation of Bax, Cytochrome C (Cyt. C), Caspase-3, and Caspase-9 protein expressions. These findings serve as a reference for further research into the processes behind ginsenoside G-M6's ovarian cancer therapy.


Assuntos
Ginsenosídeos , Neoplasias Ovarianas , Camundongos , Animais , Humanos , Feminino , Ginsenosídeos/farmacologia , PPAR gama , Farmacologia em Rede , Linhagem Celular Tumoral , Neoplasias Ovarianas/tratamento farmacológico , Neoplasias Ovarianas/patologia , Biologia Molecular
2.
Carbohydr Polym ; 257: 117534, 2021 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-33541623

RESUMO

A chitosan-based chiral hydrogel was fabricated by grafting achiral salicylaldehyde (SA) on chitosan chains, followed by supramolecular assembly (CS-SA hydrogel hereafter). The structures and properties of the CS-SA hydrogel were characterized and investigated. The results indicated that the swelling ability of the CS-SA hydrogel depended on the medium pH and crosslinking degree. Circular dichroism measurements revealed that the chiral information of the chitosan was successfully transcribed to the achiral salicylic chromophores through imine bonds. Chiroptical switches based on acid-base responses of the imine bond and the OH fragment of SA and the swelling properties of the CS-SA hydrogel were fabricated, which is first reported for a chitosan-based hydrogel. In addition, a gel film showed good fatigue resistance under external stimuli. IMPLICATION, INHIBIT, and PASS logic gates and a logic circuit based on the chiroptical switches were successfully designed. This study suggests a new method of constructing biobased chiral functional materials.

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