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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
Pristimerin is a natural product isolated and purified from the herb of Tripterygium wilfordii Hook.f. with anticancer activity. Treatment with Pristimerin may be a potential strategy for the suppression of hypoxia-induced metastasis through the reversal of hypoxia-induced stem cell characteristics and EMT in cancer cells. Pristimerin down-regulates the expression of pro-inflammatory mediators through blocking of NF-κB activation by inhibiting interconnected ROS/IKK/NF-κB signaling pathways, can effectively inhibit both arthritic inflammation and cartilage and bone damage in the joints.
Pristimerin/扁蒴藤素 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HTR-8/SVneo cells
0.25-4 µM
24 hours
Inhibited trophoblast cell proliferation
Drug Des Devel Ther. 2020 Nov 2;14:4659-4670
KBM5-T315I cells
135 nM (IC50)
72 hours
Inhibited growth and induced apoptosis
Mol Cancer. 2010 May 19;9:112
HTR-8/SVneo cells
0.5 µM
24 hours
Induced trophoblast cell apoptosis
Drug Des Devel Ther. 2020 Nov 2;14:4659-4670
HTR-8/SVneo cells
0.5 µM
24 hours
Inhibited trophoblast cell migration
Drug Des Devel Ther. 2020 Nov 2;14:4659-4670
KBM5 cells
199 nM (IC50)
72 hours
Inhibited growth and induced apoptosis
Mol Cancer. 2010 May 19;9:112
Panc-1 cells
0.625 to 5 µM
72 hours
Inhibited cell proliferation and induced apoptosis
Int J Oncol. 2014 May;44(5):1707-15.
Bone marrow-derived macrophages (BMMs)
75 nM
1, 3, 5 days
To determine the stage at which Pristimerin inhibits osteoclast formation, results showed that Pristimerin inhibited osteoclast formation at the early stage (1-3 days).
Front Pharmacol. 2021 Jan 15;11:621110
Bone marrow-derived macrophages (BMMs)
100 nM
1, 3, 5 days
To evaluate the effect of Pri on osteoclast-related gene expression, results showed Pri significantly downregulated the expression of TRAP, CTSK, c-Fos, NFATc1, DC-STAMP, and V-ATPase d2
Drug Des Devel Ther. 2020 Oct 9;14:4189-4203
Bone marrow-derived macrophages (BMMs)
0, 25, 50, 100 nM
10 days
To evaluate the effect of Pri on bone resorption function, results showed Pri significantly reduced the bone resorption ability of osteoclasts
Drug Des Devel Ther. 2020 Oct 9;14:4189-4203
Rat Brain Astrocytes (RBA-1)
0.1, 0.3, 0.5 µM
12 and 24 hours
Pristimerin inhibited LPS-induced MMP-9 expression and cell migration through attenuating NOX/ROS-dependent NF-κB activation.
J Inflamm Res. 2020 Jul 20;13:325-341
MDA-MB-231 cells
0.1, 0.2, 0.5, 1 mM
14 days
Pristimerin significantly inhibited the colony formation ability of MDA-MB-231 cells.
Biomed J. 2021 Dec;44(6 Suppl 1):S84-S92
BV2 cells
10 µM
15 minutes
To evaluate the inhibitory effect of Pristimerin on 2-AG hydrolysis. Results showed that 10 μM Pristimerin inhibited [3H]-2-OG hydrolysis by 25%.
Br J Pharmacol. 2012 Dec;167(8):1596-608
Mouse chondrocytes
50 nM, 100 nM, 200 nM
24 and 48 hours
To assess the effect of Pristimerin on chondrocyte viability, results showed no apparent effect on cell viability at concentrations below 400 nmol
Drug Des Devel Ther. 2024 Nov 27;18:5445-5459
Human brain vascular pericytes (HBVPs)
125, 250, 500 nM
24 hours
To evaluate the inhibitory effect of Pristimerin on Shh-induced pericyte adhesion and migration
Cell Death Dis. 2020 Apr 14;11(4):232
NCI-H446 cells
0.25 µM
24 hours
Inhibited cell proliferation, induced G0/G1 arrest and cell apoptosis
Int J Mol Med. 2019 Mar;43(3):1382-1394
A549 cells
0.25 µM
24 hours
Inhibited cell proliferation, induced G0/G1 arrest and cell apoptosis
Int J Mol Med. 2019 Mar;43(3):1382-1394
D-407 cells
30 µM
24 hours
D-407 cells showed higher resistance to the cytotoxic effect of Pristimerin, displaying only 20% cytotoxicity upon treatment with 30 µM Pristimerin.
J Cell Mol Med. 2020 Jun;24(11):6208-6219
RGC-5 cells
30 µM
24 hours
RGC-5 cells showed higher resistance to the cytotoxic effect of Pristimerin, displaying only 20% cytotoxicity upon treatment with 30 µM Pristimerin.
J Cell Mol Med. 2020 Jun;24(11):6208-6219
UM-1 cells
1-30 µM
24 hours
Pristimerin inhibited UM-1 cell viability in a dose-dependent manner, reaching 80% cell death at 30 µM. Moreover, Pristimerin inhibited the migration and invasion of UM-1 cells, caused a rapid increase of ROS, decreased mitochondrial membrane potential, induced the accumulation of cells in G0/G1 phase, ending with apoptotic cell death.
J Cell Mol Med. 2020 Jun;24(11):6208-6219
Human uveal melanoma cells (UM cells)
1 µM
24 hours
To assess the effect of PRI on UM cell cycle distribution, results showed that PRI induced G1 phase accumulation and reduced G2 phase accumulation.
J Cell Mol Med. 2019 Nov;23(11):7545-7553
Human uveal melanoma cells (UM cells)
0-10 µM
24 hours
To evaluate the inhibitory effect of PRI on UM cell proliferation, results showed that PRI inhibited cell proliferation in a dose-dependent manner.
J Cell Mol Med. 2019 Nov;23(11):7545-7553
MDA-MB-231 cells
0.1, 0.2, 0.3 mM
24 hours
Pristimerin significantly reduced the numbers of invasion and adhesion of MDA-MB-231 cells, and its inhibitory effects were dose-dependent.
Biomed J. 2021 Dec;44(6 Suppl 1):S84-S92
Lymph node cells (LNC)
0.1/0.3 µM
24 hours
To test the effect of Pristimerin on transcription factors STAT3 and ROR-γt. Results showed Pristimerin reduced the expression of ROR-γt and pSTAT3.
Oncol Rep. 2015 Jul;34(1):518-24
GL261 cells
0, 0.25, 0.5, 1, 2 µM
24 hours
To evaluate the effect of Pristimerin on GL261 cell viability. Results showed that Pristimerin at 0.25 μM severely inhibited GL261 cell viability.
Biosci Rep. 2019 May 14;39(5):BSR20182389
U373 cells
0, 0.25, 0.5, 1, 2 µM
24 hours
To evaluate the effect of Pristimerin on U373 cell viability. Results showed that Pristimerin at 0-1 μM did not significantly affect U373 cell viability, but at 2 μM, it remarkably inhibited cell proliferation.
Biosci Rep. 2019 May 14;39(5):BSR20182389
Mouse chondrocytes
50 nM, 100 nM, 200 nM
24 hours
To assess the effect of Pristimerin on ECM degradation, results showed Pristimerin could concentration-dependently reverse IL-1β-induced ECM degradation
Drug Des Devel Ther. 2024 Nov 27;18:5445-5459
Mouse chondrocytes
50 nM, 100 nM, 200 nM
24 hours
To assess the effect of Pristimerin on IL-1β-induced inflammatory factor expression, results showed Pristimerin could partially reverse the upregulation of inflammatory factors induced by IL-1β
Drug Des Devel Ther. 2024 Nov 27;18:5445-5459
Lymph node cells (LNC)
0.1/0.3 µM
24 hours
To test the effect of Pristimerin on transcription factors STAT3 and ROR-γt. Results showed Pristimerin reduced the expression of ROR-γt and pSTAT3.
Clin Immunol. 2014 Dec;155(2):220-30
Human umbilical vascular endothelial cells (HUVECs)
Pristimerin inhibited VEGF-induced HUVECs proliferation, migration, and tube formation in a concentration-dependent manner. 0.5 μM significantly inhibited proliferation, 1 μM significantly inhibited migration, and 0.5 μM significantly inhibited tube formation.
Molecules. 2012 Jun 5;17(6):6854-68
Bone marrow-derived macrophages (BMMs)
0, 10, 25, 50, 75 nM
3 days
To evaluate the effect of Pristimerin on osteoclast function, results showed that Pristimerin significantly inhibited bone resorption and actin ring formation.
Front Pharmacol. 2021 Jan 15;11:621110
Bone-marrow dendritic cells (BMDCs)
0.1-0.4 µM
30 min
Inhibited caspase-1 activation and IL-1β secretion
Acta Pharmacol Sin. 2021 Jun;42(6):975-986
Mouse peritoneal macrophages
0.1-0.4 µM
30 min
Inhibited caspase-1 activation and IL-1β secretion
Acta Pharmacol Sin. 2021 Jun;42(6):975-986
Bone-marrow-derived macrophages (BMDMs)
0.1-0.4 µM
30 min
Inhibited caspase-1 activation and IL-1β maturation
Acta Pharmacol Sin. 2021 Jun;42(6):975-986
Bacillus subtilis
10 µg/mL
30 minutes
Evaluation of the antimicrobial activity of Pristimerin against B. subtilis, showing weaker inhibitory effects on DNA and RNA synthesis.
Foods. 2021 Mar 11;10(3):591
Human uveal melanoma cells (UM cells)
0.1-3 µM
40 minutes
To evaluate the effect of PRI on IGF-1-induced IGF-1R and its downstream signaling pathways, results showed that PRI inhibited the phosphorylation of IGF-1R and its downstream pathways in a dose-dependent manner.
J Cell Mol Med. 2019 Nov;23(11):7545-7553
Human microvascular endothelial cell line (HMEC-1)
125, 250, 500 nM
48 hours
To evaluate the inhibitory effect of Pristimerin on Shh-induced endothelial cell proliferation
Cell Death Dis. 2020 Apr 14;11(4):232
Human umbilical vein endothelial cells (HUVEC)
125, 250, 500 nM
48 hours
To evaluate the inhibitory effect of Pristimerin on Shh-induced endothelial cell proliferation
Cell Death Dis. 2020 Apr 14;11(4):232
A549 cells
1.91 µM (IC50)
48 hours
Evaluate the synergistic inhibitory effects of Pristimerin and paclitaxel on the viability of A549 cells, results showed that Pristimerin significantly enhanced the chemosensitivity of paclitaxel
Nano Converg. 2022 Nov 24;9(1):52
MDA-MB-231 cells
0.1, 0.2, 0.5, 1 mM
48 hours
Pristimerin significantly inhibited cell proliferation, and its inhibitory effect was dose-dependent.
Biomed J. 2021 Dec;44(6 Suppl 1):S84-S92
Bone marrow-derived macrophages (BMMs)
0, 25, 50, 100 nM
48 or 96 hours
To evaluate the effect of Pri on BMMs cell viability, results showed no significant effect on cell viability at concentrations below 100 nM
Drug Des Devel Ther. 2020 Oct 9;14:4189-4203
Bone marrow-derived macrophages (BMMs)
0, 25, 50, 100 nM
5 days
To evaluate the effect of Pri on F-actin ring formation, results showed Pri reduced the size and number of F-actin rings in a dose-dependent manner
Drug Des Devel Ther. 2020 Oct 9;14:4189-4203
U937 cells
10 µM
5 minutes
To assess the effect of Pristimerin on 2-AG uptake and degradation. Results showed that 10 μM Pristimerin increased intracellular [3H]-2-AG accumulation by 125% and inhibited [3H]-glycerol formation by 25%.
Br J Pharmacol. 2012 Dec;167(8):1596-608
Bone marrow macrophages (BMMs)
0.3125, 0.625, 1.25 µM
6 days
To evaluate the inhibitory effect of PRI on RANKL-induced osteoclastogenesis. Results showed that PRI dose-dependently inhibited the formation of TRAP-positive multinucleated osteoclasts, with 1.25 μM PRI treatment group predominantly showing TRAP-positive mononuclear cells.
Drug Des Devel Ther. 2021 Jan 7;15:61-74
U373 cells
4-16 µM
6 hours
To evaluate the effect of Pristimerin on U373 cell apoptosis. Results showed that Pristimerin at 4-16 μM significantly induced cell apoptosis.
Biosci Rep. 2019 May 14;39(5):BSR20182389
32D-Bcr-Abl-T315I cells
387 nM (IC50)
72 hours
Inhibited growth and induced apoptosis
Mol Cancer. 2010 May 19;9:112
32D-Bcr-Abl cells
242 nM (IC50)
72 hours
Inhibited growth and induced apoptosis
Mol Cancer. 2010 May 19;9:112
K562 cells
450 nM (IC50)
72 hours
Inhibited growth and induced apoptosis
Mol Cancer. 2010 May 19;9:112
Bone marrow-derived macrophages (BMMs)
0, 5, 10, 25, 50, 75 nM
6-7 days
To evaluate the effect of Pristimerin on osteoclast formation, results showed that Pristimerin significantly inhibited RANKL-induced osteoclast differentiation.
Front Pharmacol. 2021 Jan 15;11:621110
Bone marrow-derived macrophages (BMMs)
0, 25, 50, 100 nM
7 days
To evaluate the effect of Pri on RANKL-induced osteoclast differentiation, results showed Pri reduced the number and size of TRAP-positive multinucleated osteoclasts in a dose-dependent manner
Drug Des Devel Ther. 2020 Oct 9;14:4189-4203
MiaPaCa-2 cells
0.625 to 5 µM
72 hours
Inhibited cell proliferation and induced apoptosis
Int J Oncol. 2014 May;44(5):1707-15.
Bone marrow-derived macrophages (BMMs)
100 nM
Different time stages (D0-D2, D2-D4, D4-D6, D0-D6)
To evaluate the effect of Pri on osteoclast differentiation at different time stages, results showed Pri significantly inhibited osteoclastogenesis at the mid-stage (D2-D4)
Drug Des Devel Ther. 2020 Oct 9;14:4189-4203
Pristimerin/扁蒴藤素 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c nude mice
NCI-H1299 xenograft model
Intraperitoneal injection
0.2, 0.4 mg/kg
Every two days for a total of 16 days
To evaluate the inhibitory effect of Pristimerin on tumor growth and angiogenesis
Cell Death Dis. 2020 Apr 14;11(4):232
Male Swiss albino mice
Autoimmune hepatitis model
Intravenous injection
0.4 and 0.8 mg/kg
5 consecutive days
To evaluate the ability of Pris to protect against autoimmune hepatitis (AIH). Results showed that Pris pretreatment significantly ameliorated Con A-induced hepatic damage, reduced serum indices of hepatic damage (ALT, AST, ALP, and LDH), improved liver histopathology, decreased neutrophil infiltration and CD4+T-cell infiltration in hepatic tissue, enhanced antioxidant capacity, inhibited NF-κB activation and inflammatory cytokine release, and reduced hepatocyte apoptosis.
Front Pharmacol. 2018 Mar 28;9:292
Nude mice
MDA-MB-231 xenograft model
Intraperitoneal injection
0.5 mg/kg
Daily for 14 days
Pristimerin significantly suppressed tumor volume and weight, increased expression of cleaved caspase-3, LC-3 II, and phosphorylation-JNK
Cell Death Discov. 2019 Aug 5;5:125
BALB/c mice
Subcutaneous xenograft tumor model
Intraperitoneal injection
1 mg/kg
Every other day for a total of 7 times
To investigate the effect of pristimerin on TNBC growth in vivo, results showed that pristimerin effectively hindered the growth of TNBC, with no significant toxic side effects observed.
Adv Sci (Weinh). 2025 Mar;12(10):e2413174
C57BL/6 mice
Ovariectomized (OVX) osteoporosis model
Intraperitoneal injection
1 mg/kg
5 days per week for 8 weeks
To evaluate the protective effect of Pristimerin on osteoporosis, results showed that Pristimerin significantly ameliorated ovariectomy-induced bone loss and reduced serum inflammatory factor levels.
Front Pharmacol. 2021 Jan 15;11:621110
BALB/C nude mice
MDA-MB-231 xenograft model
Oral gavage
1 mg/kg
Every 2 days for 6 weeks
Pristimerin significantly inhibited tumor growth and reversed EMT by downregulating integrin b3 expression.
Biomed J. 2021 Dec;44(6 Suppl 1):S84-S92
Lewis rats
Adjuvant arthritis (AA)
Intraperitoneal injection
1 mg/kg
Once daily for 5 days
To evaluate the therapeutic effect of Pristimerin on arthritis. Results showed Pristimerin significantly reduced arthritis inflammation and joint damage, decreased pro-inflammatory cytokines (IL-6, IL-17, IL-18, IL-23) expression, and increased immunomodulatory cytokine IL-10 and IFN-γ expression.
Oncol Rep. 2015 Jul;34(1):518-24
Lewis rats
Adjuvant arthritis (AA)
Intraperitoneal injection
1 mg/kg
Once daily for 5 days
To evaluate the therapeutic effect of Pristimerin on arthritis. Results showed Pristimerin significantly reduced arthritis inflammation and joint damage, decreased pro-inflammatory cytokines (IL-6, IL-17, IL-18, IL-23) expression, and increased immunomodulatory cytokine IL-10 and IFN-γ expression.
Clin Immunol. 2014 Dec;155(2):220-30
Nude mice
KBM5-T315I xenograft model
Intratumoral injection
1.0 mg/kg
Daily for 14 days
Inhibited tumor growth
Mol Cancer. 2010 May 19;9:112
C57BL/6 mice
Ovariectomy (OVX) model
Intragastric administration
10 mg/kg
Every 2 days for 2 months
To evaluate the protective effect of Pri on OVX-induced bone loss, results showed Pri significantly prevented OVX-induced reduction in bone mass and trabecular structure damage
Drug Des Devel Ther. 2020 Oct 9;14:4189-4203
Mice
Destabilization of the medial meniscus (DMM) model
Intra-articular injection
200 nmol
Once a week for four consecutive weeks
To assess the effect of Pristimerin on OA progression in vivo, results showed Pristimerin could reduce cartilage degradation and slow OA progression
Drug Des Devel Ther. 2024 Nov 27;18:5445-5459
BALB/c nude mice
Human breast cancer xenograft model
Subcutaneous injection
3 mg/kg
Every other day for 16 days
Pristimerin significantly reduced both tumor volume and tumor weight, and decreased angiogenesis in a xenograft mouse tumor model in vivo. The mean number of blood vessels in the treated group was significantly lower than in the control group.
Molecules. 2012 Jun 5;17(6):6854-68
C57BL/6 mice
Ovariectomy (OVX)-induced osteoporosis model
Intraperitoneal injection
5 mg/kg
Once every two days for 6 weeks
To evaluate the protective effect of PRI against OVX-mediated bone loss. Results showed that PRI treatment significantly improved bone parameters such as bone volume (BV/TV), trabecular number (Tb.N), bone mineral density (BMD), and reduced the number of TRAP-positive osteoclasts.
Drug Des Devel Ther. 2021 Jan 7;15:61-74
C57BL/6J mice
LPS-induced systemic inflammation model
Intraperitoneal injection
500 μg/kg
Single injection
Significantly reduced serum IL-1β and IL-18 levels
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