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. 2020 Sep 15;10(9):1321. doi: 10.3390/biom10091321

Table 3.

Regulatory Impacts of THM compounds for HNSCC Cell Drug Resistance.

Herbal Compounds Cell Types Cellular/Molecular Changes
Berberine OC2
(Human oral cancer cells)
↑Paclitaxel induced cytotoxicity
↓multidrug resistant gene pgp-170 [103]
Artesunate Eca109/Ec9706
(Human esophageal squamous carcinoma)
↓mitochondrial membrane potential [19]
Wogonin AMC-HN4R/AMC-HN9R
(CDDP resistant HNSCC cells)
↓cell number
↓Nrf2 and glutathione S-transferase P → ROS accumulation↑
→cell death pathways involving PUMA and PARP↑ [105]
EGCG K3, K4 and K5
(Cancer stem cells isolated from HNSCC patients)
↓sphere forming capacity
↓Oct4, Sox2, Nanog and CD44
↓ABCC2 and ABCG2 → ↑CDDP mediated chemosensitivity
↓xenografic tumor formation and induced apoptosis## [111]
(-)-Gossypol UM-SCC-5/UM-SCC-10B
(CDDP sensitive/resistant HNSCC cells)
→induced more cell apoptosis in CDDP resistant cells via regulation of Bcl-2 and Bcl-xL as well as p53 status [106,107]
Galiumverum aqueous extract Hep-2/HLaC79
(Paclitaxel sensitive/resistant
human laryngeal carcinoma)
↑MDR and p-gp protein expression in resistant cells
→more profoundly inhibited 3D spheroid mediated invasion [55]
Danshen extract KB-7D (etoposide resistant)
KB-tax (taxol resistant)
(Human oral cancer)
→significantly inhibited the proliferation of drug-resistant cells [112]
Celastrol SAS/SASV16
(vincristine-resistant
human tongue squamous carcinoma)
→G2/M cell cycle arrest
↑caspases-3, -8, -9 and PARP activity → apoptosis
→modulating BCL-2 and JNK1/2 signaling activity [113]
Cepharanthine (CEP) Eca109
(CDDP sensitive/resistant
human esophageal squamous cell carcinoma)
In vitro and in vivo ##
↓P-gp
→sensitivity of cell lines resistant to cisplatin↑ [14]

##: In vivo study. Abbreviations: P-gp: P-glycoprotein; MDR: Multidrug resistance; ABCG2: ATP-binding cassette super –family G member 2; JNK = c-Jun N-terminal kinase (JNK).