Tetrandrine is a high-affinity blocker of the type II, maxi-Ca(2+)-activated K+ channel of the rat neurohypophysial terminals. The non-inactivating component of ICa was inhibited by external tetrandrine in a voltage- and dose-dependent manner, with an IC50 = 10.1 microM. IKCa was elicited by depolarizations when approximately 10 microM Ca2+ was present on the cytoplasmic side. Only externally applied tetrandrine, at 1 microM, decreased the amplitude of IKCa, whereas the fast inward Na+ current and transient outward K+ current were not affected[3]. Tetrandrine enhanced the ubiquitination and degradation of Syk (spleen tyrosine kinase) and consequently repressed the osteoclastogenesis and bone destruction through the AhR-c-src-c-Cbl (aryl hydrocarbon receptor) pathway[4]. Furthermore, Tetrandrine is a bisbenzylisoquinoline alkaloid known to exhibit anticancer activity against different cancers. Dose- and time-dependant cytotoxic effect of tetradrine on both MDA-MB-231 and PANC-1 cells (pancreatic PANC-1 and breast MDA-MB-231 cancer cells) with IC50 values ranging between 51 and 54 μM and 22 and 27 μM for 24 h and 48 h of incubation respectively[5].
Tetrandrine/粉防己碱 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HepG2 cells
2 μg/mL
12 hours
To detect TET-CTM/L induced apoptosis in HepG2 cells, results showed that TET-CTM/L significantly induced apoptosis.
Int J Nanomedicine. 2024 Jan 23;19:727-742.
Huh7 cells
0, 0.5, 1, 2 or 4 µM
24 hours
Tetrandrine significantly inhibited the migration and invasion of Huh7 cells
J Exp Clin Cancer Res. 2018 Jan 15;37(1):7.
HCCLM9 cells
0, 0.5, 1, 2 or 4 µM
24 hours
Tetrandrine significantly inhibited the migration and invasion of HCCLM9 cells
J Exp Clin Cancer Res. 2018 Jan 15;37(1):7.
Hep3B cells
0, 0.5, 1, 2 or 4 µM
24 hours
Tetrandrine significantly inhibited the migration and invasion of Hep3B cells
J Exp Clin Cancer Res. 2018 Jan 15;37(1):7.
HepG2 cells
0.675-20 μg/mL
24 hours
To evaluate the cytotoxicity of TET-CTM/L against HepG2 cells, results showed that TET-CTM/L has significant anti-tumor efficacy.
Int J Nanomedicine. 2024 Jan 23;19:727-742.
Murine peritoneal macrophages
100 µM
3 hours
Tetrandrine inhibited NLRP3 inflammasome activation and reduced the release of IL-1β and IL-18.
Acta Pharmacol Sin. 2022 May;43(5):1274-1284.
Cardiac myocytes
10 µM
30 minutes
Tetrandrine significantly inhibited Ang II-induced ROS generation
Br J Pharmacol. 2010 Feb;159(4):970-81.
K562
2 µM
48 hours
Tetrandrine inhibited the proliferation of K562 cells and induced cell cycle arrest at the G0/G1 phase.
Cell Death Dis. 2018 May 1;9(5):473.
THP-1
2 µM
48 hours
Tetrandrine inhibited the proliferation of THP-1 cells and induced cell cycle arrest at the G0/G1 phase.
Cell Death Dis. 2018 May 1;9(5):473.
HL60
2 µM
48 hours
Tetrandrine inhibited the proliferation of HL60 cells and induced cell cycle arrest at the G0/G1 phase.
Cell Death Dis. 2018 May 1;9(5):473.
U937
2 µM
48 hours
Tetrandrine inhibited the proliferation of U937 cells and induced cell cycle arrest at the G0/G1 phase.
Cell Death Dis. 2018 May 1;9(5):473.
K562 cells
2 µM
48 hours
Tetrandrine induced cell cycle arrest and megakaryocyte differentiation in K562 cells via activation of autophagy.
Br J Pharmacol. 2017 Dec;174(23):4308-4328.
6133 cells
2 µM
48 hours
Tetrandrine induced cell cycle arrest and megakaryocyte differentiation in 6133 cells via activation of autophagy.
Br J Pharmacol. 2017 Dec;174(23):4308-4328.
CMK cells
2 µM
48 hours
Tetrandrine induced cell cycle arrest and megakaryocyte differentiation in CMK cells via activation of autophagy.
Br J Pharmacol. 2017 Dec;174(23):4308-4328.
HEL cells
2 µM
48 hours
Tetrandrine induced cell cycle arrest and megakaryocyte differentiation in HEL cells via activation of autophagy.
Br J Pharmacol. 2017 Dec;174(23):4308-4328.
RAW264.7 cells
0.3 µM
6 hours
Tetrandrine significantly inhibited RANKL-induced osteoclastogenesis and enhanced the ubiquitination and degradation of Syk through the AhR/c-src/c-Cbl signaling pathway.
Cell Death Dis. 2019 Jan 15;10(2):38.
BMMs
0.3 µM
6 hours
Tetrandrine significantly inhibited RANKL-induced osteoclastogenesis and enhanced the ubiquitination and degradation of Syk through the AhR/c-src/c-Cbl signaling pathway.
Cell Death Dis. 2019 Jan 15;10(2):38.
Human breast cancer cells (MDA-MB-231, MDA-MB-468, MCF-7)
0-5 µM
72 hours
Tetrandrine alone or in combination with H89 exhibited antitumor effects on various cancer cells, and the combination showed synergistic effects.
J Exp Clin Cancer Res. 2018 Jun 4;37(1):114.
Human hepatoma cells (Hep3B, Huh7)
0-5 µM
72 hours
Tetrandrine alone or in combination with H89 exhibited antitumor effects on various cancer cells, and the combination showed synergistic effects.
J Exp Clin Cancer Res. 2018 Jun 4;37(1):114.
Human renal carcinoma cells (769-P, ACHN, 786-O)
0-5 µM
72 hours
Tetrandrine alone or in combination with H89 exhibited antitumor effects on various cancer cells, and the combination showed synergistic effects.
J Exp Clin Cancer Res. 2018 Jun 4;37(1):114.
Human colon cancer cells (LOVO, HCT116)
0-5 µM
72 hours
Tetrandrine alone or in combination with H89 exhibited antitumor effects on various cancer cells, and the combination showed synergistic effects.
J Exp Clin Cancer Res. 2018 Jun 4;37(1):114.
Tetrandrine/粉防己碱 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
HepG2 xenograft tumor model
Intraperitoneal injection
1.5 mg/kg
Once every two days for 24 days
To evaluate the in vivo anti-tumor efficacy of TET-CTM/L, results showed that TET-CTM/L significantly inhibited tumor growth.
Int J Nanomedicine. 2024 Jan 23;19:727-742.
Mice
Thy1-hTau.P301S transgenic mice
Intraperitoneal injection
2.5 mg/kg, 5 mg/kg, 10 mg/kg
Every two days for two months
To study the effect of Tetrandrine on tau aggregation and cognitive dysfunction, results showed that Tetrandrine reduced tau aggregation in a dose-dependent manner and improved memory function in mice.
J Biomed Sci. 2022 Oct 22;29(1):85
Nude mice (BALB/c)
MDA-MB-231 xenograft model
Oral and intraperitoneal injection
25 mg/kg
Every other day for 28 days
The combination of Tetrandrine and H89 significantly inhibited tumor growth in vivo, showing synergistic effects.
J Exp Clin Cancer Res. 2018 Jun 4;37(1):114.
Nude mice
Subcutaneous tumor xenograft model
Oral
25 mg/kg or 50 mg/kg
Once daily for 13 days
Tetrandrine significantly inhibited tumor growth and promoted tumor cell differentiation.
Cell Death Dis. 2018 May 1;9(5):473.
Nude mice
HCCLM9 subcutaneous tumor xenograft model
Oral
30 mg/kg
Every other day for 37 days
Tetrandrine significantly inhibited lung metastasis of HCCLM9 cells in vivo
J Exp Clin Cancer Res. 2018 Jan 15;37(1):7.
Nude mice
K562 tumor xenograft model
Oral
50 mg/kg
Once daily for 23 days
Tetrandrine significantly inhibited the growth of K562 tumors, reducing tumor volume and weight.
Br J Pharmacol. 2017 Dec;174(23):4308-4328.
C57BL/6J mice
Silicosis model
Gavage
50 mg/kg or 100 mg/kg
Once daily for 4 weeks
Tetrandrine alleviated pulmonary inflammation and fibrosis, and improved lung function in silicosis mice.
Acta Pharmacol Sin. 2022 May;43(5):1274-1284.
C57/B6 mice
Aortic banding (AB) model
Oral gavage
50 mg/kg/day
Three times a day for one week
Tetrandrine significantly attenuated AB-induced cardiac hypertrophy, reduced heart weight/body weight and lung weight/body weight ratios, and inhibited fibrosis and inflammatory response
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