Unveiling the potential of medicinal herbs as the source for in vitro screening toward the inhibition of Nrf2.

Autor: Nguyen MH; University of Health Sciences, Vietnam National University Ho Chi Minh City, YA1 Administrative Building, Hai Thuong Lan Ong Street, Dong Hoa Ward, Di An City, Binh Duong Province, 75308, Viet Nam.; Vietnam National University Ho Chi Minh City, Quarter 6, Linh Trung Ward, Thu Duc District, Ho Chi Minh City, 70000, Viet Nam., Nguyen NYT; University of Health Sciences, Vietnam National University Ho Chi Minh City, YA1 Administrative Building, Hai Thuong Lan Ong Street, Dong Hoa Ward, Di An City, Binh Duong Province, 75308, Viet Nam.; Vietnam National University Ho Chi Minh City, Quarter 6, Linh Trung Ward, Thu Duc District, Ho Chi Minh City, 70000, Viet Nam.; Faculty of Applied Science, University of Technology, Vietnam National University Ho Chi Minh City, 268 Ly Thuong Kiet Street Ward 14, District 10, Ho Chi Minh City, 70000, Viet Nam., Chen YS; Graduate Institute of Natural Products, College of Pharmacy, Kaohsiung Medical University, No.100, Shih-Chuan 1st Road, Sanmin District, Kaohsiung City, 80708, Taiwan.; National Natural Product Libraries and High-Throughput Screening Core Facility, Kaohsiung Medical University, No.100, Shih-Chuan 1st Road, Sanmin District, Kaohsiung City, 80708, Taiwan., Nguyen Le HT; University of Health Sciences, Vietnam National University Ho Chi Minh City, YA1 Administrative Building, Hai Thuong Lan Ong Street, Dong Hoa Ward, Di An City, Binh Duong Province, 75308, Viet Nam., Vo HT; University of Health Sciences, Vietnam National University Ho Chi Minh City, YA1 Administrative Building, Hai Thuong Lan Ong Street, Dong Hoa Ward, Di An City, Binh Duong Province, 75308, Viet Nam.; Vietnam National University Ho Chi Minh City, Quarter 6, Linh Trung Ward, Thu Duc District, Ho Chi Minh City, 70000, Viet Nam., Yen CH; Graduate Institute of Natural Products, College of Pharmacy, Kaohsiung Medical University, No.100, Shih-Chuan 1st Road, Sanmin District, Kaohsiung City, 80708, Taiwan.; National Natural Product Libraries and High-Throughput Screening Core Facility, Kaohsiung Medical University, No.100, Shih-Chuan 1st Road, Sanmin District, Kaohsiung City, 80708, Taiwan.
Jazyk: angličtina
Zdroj: Heliyon [Heliyon] 2024 Sep 26; Vol. 10 (19), pp. e38411. Date of Electronic Publication: 2024 Sep 26 (Print Publication: 2024).
DOI: 10.1016/j.heliyon.2024.e38411
Abstrakt: Background: Drug resistance is one of the leading causes attributed to the failure of cancer treatment by chemotherapy. Nuclear factor erythroid 2-related factor 2 (Nrf2) is a transcription factor regulating gene expression in cell defense against oxidative stress or hazardous factors. Taking advantage of this feature, Nrf2 also serves as the bodyguard for both normal and cancer cells. Many pieces of evidence have reported that inhibiting Nrf2 activity in cancer cells can reverse chemotherapy drug resistance. In addition, secondary metabolites from medicinal plants have been reported to inhibit Nrf2 activity in the in vitro study. This study aimed to preliminarily investigate fractions from medicinal herbs that inhibit Nrf2 activity in Huh7 liver cancer cells, thereby establishing a basis for subsequent isolation and extraction processes.
Materials and Methods: Sub-fractions from five medicinal plants have been evaluated the Nrf2 inhibitor activity on Huh7 cells through luciferase-reported genes assay. Thin-layer chromatography (TLC) was also performed to quantify the extracts' main phytochemistry components. Combining the half-maximal inhibitory concentration (IC 50 ) and half-maximal cytotoxicity concentration (CC 50 ) enables us to determine which extracts have the potential for further isolation steps.
Results: Ten over 30 crude extracts and sub-fractions showed the inhibition of Nrf2 activity with the percentage ranging from 30 to 97 %. The methanol and n -hexane sub-fractions from Helicteres hirsuta Lour. leaves showed the strongest inhibition ability on Nrf2 activity with the IC 50  = 20.98 ± 3.67 and 42.22 ± 2.10 μg/mL, respectively. The TLC results showed the presence of steroids and terpenoids in the promising sub-fractions.
Conclusions: Combining the TLC results with the in vitro screening on Nrf2 activity screening of medicinal plants, the outcomes suggest the steroids and terpenoids in the methanol extract and hexane sub-fraction from Helicteres hirsuta Lour. leaves show promise towards inhibiting Nrf2 activity in liver cancer cell lines without toxicity in the normal cells.
Competing Interests: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(© 2024 The Authors.)
Databáze: MEDLINE