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BPPA promotes head and neck cancer cell death via mitochondrial damage induced by reactive oxygen species
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Ye-qian ZENG1, Xin-zhuo ZHOU1, Yu-fei FENG1, Yan TANG1, Yong-de WANG2, Chun-sheng HU1, 2
Chinese Journal of Clinical Pharmacology | 2025, 41(3) : 340 - 344
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Chinese Journal of Clinical Pharmacology | 2025, 41(3): 340-344
Clinical and Basic Bridging Research
BPPA promotes head and neck cancer cell death via mitochondrial damage induced by reactive oxygen species
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Ye-qian ZENG1, Xin-zhuo ZHOU1, Yu-fei FENG1, Yan TANG1, Yong-de WANG2, Chun-sheng HU1, 2
Affiliations
  • 1.College of Pharmacy, International Academy of Targeted Therapeutics and Innovation, National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, Chongqing University of Arts and Sciences, Chongqing 402160, China
  • 2.Chongqing Key Laboratory of Chinese Medicine & Health Science, Chongqing Academy of Chinese Materia Medica, Chongqing 400065, China
Published: 2025-02-17 doi: 10.13699/j.cnki.1001-6821.2025.03.009
Outline
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Objective

To investigate the antitumor activity and mechanism of a pyrazole [1,5-a]pyrimidine derivative (BPPA) on human tongue squamous cell carcinoma Cal33 cells.

Methods

Cal33 cells were divided into blank group (normal culture), experimental-L, -M, -H groups (1, 2.5 and 5 μmol·L-1BPPA) and combined group [2.5 μmol·L-1BPPA and 5 mmol·L-1 N-acety-L-cysteine (NAC)]. Cell viability was determined by thiazole blue assay. Cell apoptosis was measured using flow cytometry, while apoptosis-related protein expression levels were determined by Western blot analysis. Changes in reactive oxygen species and mitochondrial membrane potential were evaluated using immunofluorescence assay.

Results

The survival rates of Cal33 cells in blank, experimental-L,-M,-H and combined groups were (99.56±0.91)%, (58.31±2.31)%, (47.93±1.67)%, (29.35±4.11)% and (70.27±1.21)%, respectively; cell apoptotic rates were (8.07±1.01)%, (44.04±0.94)%, (49.85±1.75)%, (66.79±0.83)% and (24.33±1.04)%, respectively; the relative fluorescence intensities of reactive oxygen species (ROS) were 1.23±0.21, 3.37±0.35, 15.53±1.46, 20.28±1.24 and 5.59±0.52, respectively; the mitochondrial membrane potential red fluorescence/green fluorescence values were 4.69±0.11, 4.24±0.12, 0.86±0.16, 0.46±0.05 and 2.99±0.11, respectively. Compared with blank group, the above indexes in the experimental-L, -M, -H groups were statistically significant (P<0.01, P<0.001). Compared with experimental-M group, the above indexes in combined group were statistically significant (P<0.01, P<0.001). The relative levels of pro-apoptotic B-cell lymphoma-2 (Bcl-2)-Associated X protein (Bax) in blank, experimental-L,-M,-H groups were 1.00±0.02, 1.94±0.03, 3.73±0.06 and 4.64±0.08, respectively; the relative levels of anti-apoptotic protein Bcl-2 were 1.00±0.02, 0.75±0.04, 0.62±0.02 and 0.46±0.03, respectively. Compared with blank group, the above indexes in the experimental-L, -M, -H groups were statistically significant (P<0.01, P<0.001).

Conclusion

BPPA exhibits anti-head and neck cancer activity by ROS mediating the decrease in mitochondrial membrane potential, thereby inducing apoptosis.

pyrazole derivative  /  head and neck cancer  /  cell apoptosis  /  reactive oxygen species  /  mitochondrial membrane potential
Ye-qian ZENG, Xin-zhuo ZHOU, Yu-fei FENG, Yan TANG, Yong-de WANG, Chun-sheng HU. BPPA promotes head and neck cancer cell death via mitochondrial damage induced by reactive oxygen species[J]. Chinese Journal of Clinical Pharmacology, 2025 , 41 (3) : 340 -344 . DOI: 10.13699/j.cnki.1001-6821.2025.03.009
Year 2025 volume 41 Issue 3
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doi: 10.13699/j.cnki.1001-6821.2025.03.009
  • Receive Date:2024-08-17
  • Online Date:2026-08-04
  • Published:2025-02-17
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  • Received:2024-08-17
Funding
Affiliations
    1.College of Pharmacy, International Academy of Targeted Therapeutics and Innovation, National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, Chongqing University of Arts and Sciences, Chongqing 402160, China
    2.Chongqing Key Laboratory of Chinese Medicine & Health Science, Chongqing Academy of Chinese Materia Medica, Chongqing 400065, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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