Triptophenolide is a colorless crystalline plate isolated from ethyl acetate extracts of Tripterygium wilfordii. IC50 value: Target: In vitro: Triptophenolide can remarkably inhibit the delayed type hypersensitivity (DTH) reaction induced by DNCB and BSA; and diminished the peripheral blood ANAE+lymphocytes in rats and micc. Moreover, triptophenolide can dramatically increase the amount of total serum complement and significautly decrcase the serum antibody products (1gG ) of rats and mice. The phagocytosis of perioneal exudate macrophages in mice present double effects in vitro [1]. In vivo:
分子量
312.40
Formula
C20H24O3
CAS 号
74285-86-2
中文名称
雷酚内酯
运输条件
Room temperature in continental US; may vary elsewhere.
Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.
IC50 & Target[1]
NF-κB
Autophagy
Mitophagy
体外研究 (In Vitro)
Parthenolide (PTL) has a dose-dependent growth inhibition effect on NSCLC cells Calu-1, H1792, A549, H1299, H157, and H460. Parthenolide can induce cleavage of apoptotic proteins such as CASP8, CASP9, CASP3 and PARP1 both in concentration- and time-dependent manner in tested lung cancer cells, indicating that apoptosis is trigged after Parthenolide exposure. In addition to induction of apoptosis, Parthenolide also induces G0/G1 cell cycle arrest in a concentration-dependent manner in A549 cells and G2/M cell cycle arrest in H1792 cells[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Only Parthenolide, the HDAC inhibitor with anti-inflammatory features, displayed a potent anti-apoptotic effect in Phb1 KO hepatocytes. Indeed, TSA and Parthenolide-treated hepatocytes showed increased levels of FXR, and reduced levels of CYP7A1, HDAC4, TNFα, TRAIL and Bax suggesting a less toxic effect of bile acids as a results of specific HDAC inhibition, resulting in the attenuation of the Phb1 KO hepatocytes apoptotic response. Importantly, Parthenolide exerts a protective effect from the liver injury after BDL in Phb1 KO mice. Indeed, Parthenolide treatment results in a reduction of the mortality rate of this mice after BDL associated with a lower apoptotic response as revealed by a reduction of necrotic areas, Tunel-staining, as well as decreased ALT (8431±957 vs.4225±210 U/L) and AST (4805±300 vs.2242±438 U/L) activities compared to control Phb1 KO mice[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
248.32
Formula
C15H20O3
CAS 号
20554-84-1
中文名称
小白菊内酯;银胶菊内酯
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Nakshatri H, et al. NF-κB-dependent and -independent epigenetic modulation using the novel anti-cancer agent DMAPT. Cell Death Dis. 2015 Jan 22;6:e1608.
[2]. Zhao X, et al. Parthenolide induces apoptosis via TNFRSF10B and PMAIP1 pathways in human lung cancer cells. J Exp Clin Cancer Res. 2014 Jan 6;33:3.
[3]. Barbier-Torres L, et al. Histone deacetylase 4 promotes cholestatic liver injury in the absence of prohibitin-1. Hepatology. 2015 Oct;62(4):1237-48.
Cell Assay [2]
Human lung cancer cell lines are seeded in 96-well plates and treated on the second day with the given concentration of Parthenolide (0, 5, 10, 20 μM) for another 48 hours and then subjected to SRB or MTT assay. For SRB assay, live cell number is estimated as described earlier. After treatment, the medium is discarded firstly. In order to fix the adherent cells, 100 μL of cold trichloroacetic acid (10% (w/v)) are adding to each well and incubating at 4°C for at least 1 hour. The plates are then washed five times with deionized water and dried in the air. Each well are then added with 50 μL of SRB solution (0.4% w/v in 1% acetic acid) and incubated for 5 min at room temperature. The plates are washed five times with 1% acetic acid to remove unbound SRB and then air dried. The residual bound SRB is solubilized with 100 μL of 10 mM Tris base buffer (pH 10.5), and then read using a microtiter plate reader at 495 nm. The MTT assay is executed. 20 μL MTT (5 mg/mL) are added to each sample and incubate at 37°C for 4 h, then 100 μL solubilization solution are added. Cell viability is determined at 595 nm[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [3]
Mice[3] Phb1 KO mice are used. Males from 8-12 weeks of age are treated. Parthenolide is intraperitoneally injected at a dose of 3 mg/kg 24 h and 1h before bile duct ligation (BDL) or twice a week during two weeks. Liver specimens are snap-frozen for subsequent analysis[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Nakshatri H, et al. NF-κB-dependent and -independent epigenetic modulation using the novel anti-cancer agent DMAPT. Cell Death Dis. 2015 Jan 22;6:e1608.
[2]. Zhao X, et al. Parthenolide induces apoptosis via TNFRSF10B and PMAIP1 pathways in human lung cancer cells. J Exp Clin Cancer Res. 2014 Jan 6;33:3.
[3]. Barbier-Torres L, et al. Histone deacetylase 4 promotes cholestatic liver injury in the absence of prohibitin-1. Hepatology. 2015 Oct;62(4):1237-48.
Costunolide ((+)-Costunolide) is a naturally occurring sesquiterpene lactone, with antioxidative, anti-inflammatory, antiallergic, bone remodeling, neuroprotective, hair growth promoting, anticancer, and antidiabetic properties. Costunolide can induce cell cycle arrest and apoptosis on breast cancer cells[1][2][3].
IC50 & Target
Human Endogenous Metabolite
体外研究 (In Vitro)
Costunolide inhibits the colony formation, migrative and invasive abilities of the H1299 cells in a dose or time dependent manner[2]. Costunolide (6.7-215.2 μM; 24 hours) inhibits the viability of H1299 cells in a dose-dependent manner, with an IC50 of 23.93 µM[2]. Costunolide (12.0-48.0 µM; 48 hours) induces apoptosis in H1299 cells[2]. Costunolide (12-48.0 µM; 6-12 hours) regulates metastasis- and proliferation-associated mRNA expression[2]. Costunolide regulates epithelial-to-mesenchymal transition (EMT)-associated protein expression[2]. Costunolide regulates c-Myc mediated apoptosis signaling and 14-3-3-mediated signaling pathways in breast cancer cells[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[2]
Cell Line:
H1299 cells
Concentration:
6.7 μM, 13.5 μM, 26.9 μM, 107.6 μM, 215.2 μM
Incubation Time:
24 hours
Result:
Inhibited the viability of H1299 cells (MTT assay).
Apoptosis Analysis[2]
Cell Line:
H1299 cells
Concentration:
0 µM, 12.0 µM, 24.0 µM, 48.0 µM
Incubation Time:
48 hours
Result:
Significantly promoted apoptosis at 24.0 µM and 48.0 µM.
RT-PCR[2]
Cell Line:
H1299 cells
Concentration:
0 µM, 12.0 µM, 24.0 µM, 48.0 µM
Incubation Time:
6 hours, 12 hours
Result:
Regulated the metastasis- and proliferation-associated mRNA levels in a dose-dependent manner.
Western Blot Analysis[2]
Cell Line:
H1299 cells
Concentration:
0 µM, 12.0 µM, 24.0 µM, 48.0 µM
Incubation Time:
48 hours
Result:
Significantly inhibited the EMT of H1299 cells.
体内研究 (In Vivo)
Costunolide (20 mg/kg; i.p; daily; for 30 days) inhibits breast cancer through c-Myc/p53 and AKT/14-3-3 pathway[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
[1]. Dae Yong Kim, et al. Costunolide-A Bioactive Sesquiterpene Lactone with Diverse Therapeutic Potential. Int J Mol Sci. 2019 Jun; 20(12): 2926.
[2]. Minyan Wei, et al. Costunolide induces apoptosis and inhibits migration and invasion in H1299 lung cancer cells. Oncol Rep. 2020 Jun;43(6):1986-1994.
[3]. Zhangxiao Peng, et al. Costunolide and dehydrocostuslactone combination treatment inhibit breast cancer by inducing cell cycle arrest and apoptosis through c-Myc/p53 and AKT/14-3-3 pathway.Sci Rep. 2017; 7: 41254.
Bilobalide, a sesquiterpene trilactone constituent of Ginkgo biloba, inhibits the NMDA-induced efflux of choline with an IC50 value of 2.3 µM. Bilobalide prevents apoptosis through activation of the PI3K/Akt pathway in SH-SY5Y cells. Exerts protective and trophic effects on neurons[1][2].
IC50 & Target
Human Endogenous Metabolite
体外研究 (In Vitro)
Bilobalide (1-100 µM) completely suppresses the NMDA-evoked release of choline in a concentration-dependent manner with IC50 value of 2.3 µM[1]. Bilobalide (1, 5 and 10 μM) alone for 24 h does not affect cell viability of SH-SY5Y cells. Pre-treatment of cells with Bilobalide concentration-dependently prevents Aβ 1-42-, H2O2– and serum deprivation-induced decrease of cell viability, with the best protective effect obtained at 10 μM[2]. Bilobalide (5 and 10 μM; 24 h) treatment dose-dependently increases levels of p-Akt (Ser473 and Thr308) in SH-SY5Y cells[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis
Cell Line:
SH-SY5Y cells
Concentration:
5 and 10 μM
Incubation Time:
24 hours
Result:
Induced a significant increase in levels of p-Akt (Ser473 and Thr308).
体内研究 (In Vivo)
Bilobalide (20 mg/kg) completely suppresses the NMDA-induced release of choline in vivo while basal choline levels were not significantly affected. NMDA causes a release of choline in vivo when infused into the hippocampus of freely moving rats by retrograde dialysis. Bilobalide (20 mg/kg i.p.) completely inhibits the effect induced by NMDA[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male Wistar rats (250-350 g)[1]
Dosage:
20 mg/kg
Administration:
I.p. injection 60 min before NMDA infusion
Result:
Lowered basal choline efflux only slightly (by 7%) but fully antagonized the NMDA-induced increase of choline release. The convulsive effect of NMDA was almost completely suppressed.
分子量
326.30
Formula
C15H18O8
CAS 号
33570-04-6
中文名称
白果内酯
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. O Weichel, et al. Bilobalide, a constituent of Ginkgo biloba, inhibits NMDA-induced phospholipase A2 activation and phospholipid breakdown in rat hippocampus. Naunyn Schmiedebergs Arch Pharmacol. 1999 Dec;360(6):609-15.
[2]. Chun Shi, et al. Bilobalide prevents apoptosis through activation of the PI3K/Akt pathway in SH-SY5Y cells. Apoptosis. 2010 Jun;15(6):715-27.
ArnicolideC is a sesquiterpene lactone isolated Centipeda minima[1]. ArnicolideC exertes a cytotoxic effect on the panel of Nasopharyngeal carcinoma (NPC) cells, significantly inhibiting cell growth in a dose- and time- dependent manner. ArnicolideC also exhibits inhibitory effects on NPC proliferation[2].
分子量
334.41
Formula
C19H26O5
CAS 号
34532-67-7
中文名称
山金车内酯C
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Chan CO, et al. Qualitative and quantitative analysis of sesquiterpene lactones in Centipeda minima by UPLC-Orbitrap-MS & UPLC-QQQ-MS. J Pharm Biomed Anal. 2019 May 30;174:360-366.
[2]. Liu R, et al. Arnicolide D, from the herb Centipeda minima, Is a Therapeutic Candidate against Nasopharyngeal Carcinoma. Molecules. 2019 May 17;24(10).
Dehydrocostus Lactone is a major sesquiterpene lactone isolated from the roots of Saussurea lappa. IC50 value: Target: In vitro: Dehydrocostus Lactone promoted apoptosis with increased activation of caspases 8, 9, 7, 3, enhanced PARP cleavage, decreased Bcl-xL expression and increased levels of Bax, Bak, Bok, Bik, Bmf, and t-Bid. We have demonstrated that Dehydrocostus Lactone inhibits cell growth and induce apoptosis in DU145 cells [1]. Dehydrocostus Lactone inhibits NF-kappaB activation by preventing TNF-alpha-induced degradation and phosphorylation of its inhibitory protein I-kappaB alpha in human leukemia HL-60 cells and that dehydrocostus lactone renders HL-60 cells susceptible to TNF-alpha-induced apoptosis by enhancing caspase-8 and caspase-3 activities [2]. Dehydrocostus Lactone inhibited the production of NO in lipopolysaccharide (LPS)-activated RAW 264.7 cells by suppressing inducible nitric oxide synthase enzyme expression. In vivo: Dehydrocostus Lactone decreased the TNF-alpha level in LPS-activated systems in vivo [3].
分子量
230.30
Formula
C15H18O2
CAS 号
477-43-0
中文名称
去氢木香烃内酯
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Eun Ji Kim, et al. Apoptosis of DU145 human prostate cancer cells induced by dehydrocostus lactone isolated from the root of Saussurea lappa. Food and Chemical Toxicology Volume 46, Issue 12, December 2008, Pages 3651–3658
[2]. Oh GS, et al. Dehydrocostus lactone enhances tumor necrosis factor-alpha-induced apoptosis of human leukemia HL-60 cells. Immunopharmacol Immunotoxicol. 2004 May;26(2):163-75.
[3]. Lee HJ, et al. A sesquiterpene, dehydrocostus lactone, inhibits the expression of inducible nitric oxide synthase and TNF-alpha in LPS-activated macrophages. Planta Med. 1999 Mar;65(2):104-8.
[4]. Taniguchi M, et al. COSTUNOLIDE AND DEHYDROCOSTUS LACTONE AS INHIBITORS OF KILLING FUNCTION OF CYTOTOXIC T LYMPHOCYTES. Bioscience, Biotechnology, and Biochemistry, 1995, 59 (11): 2064-2067
Ginkgolide K, isolated from Ginkgo biloba, induces protective autophagy through the AMPK/mTOR/ULK1 signaling pathway. Ginkgolide K possesses neuroprotective activity[1].
分子量
406.38
Formula
C20H22O9
CAS 号
153355-70-5
中文名称
银杏内酯 K
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:
DMSO : 50 mg/mL (123.04 mM; ultrasonic and warming and heat to 80°C)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
2.4608 mL
12.3038 mL
24.6075 mL
5 mM
0.4922 mL
2.4608 mL
4.9215 mL
10 mM
0.2461 mL
1.2304 mL
2.4608 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
[1]. Zhang Y, et al. Ginkgolide K promotes astrocyte proliferation and migration after oxygen-glucose deprivation via inducing protective autophagy through the AMPK/mTOR/ULK1 signaling pathway. Eur J Pharmacol. 2018 Aug 5;832:96-103.