| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Natural product; PI3K/Akt-NF-κB
Tenacissoside H targets the PI3K/AKT and MAPK signaling pathways, as well as the NF-kappaB transcription factor. By modulating these signaling pathways, Tenacissoside H inhibits tumor cell proliferation and induces apoptosis. The compound's mechanism of action involves the inhibition of various signaling pathways and enzymes, leading to the suppression of inflammation and tumor growth. Tenacissoside H has antitumor activity on esophageal cancer through arresting the cell cycle and regulating the PI3K/Akt-NF-kappaB transduction cascade. |
|---|---|
| ln Vitro |
In vitro, tenacissoside H (TDH) significantly inhibited cells proliferation in a time-and-dose-dependent manner. TDH arrested the cell cycle in S phase and significantly inhibited PI3K and NF-κB mRNA expression, compared with blank controlled group [1].
In vitro, Tenacissoside H demonstrates antitumor activity on esophageal cancer cells. The compound inhibits tumor cell proliferation and induces apoptosis by modulating signaling pathways such as PI3K/AKT and MAPK. Tenacissoside H arrests the cell cycle and regulates the PI3K/Akt-NF-kappaB transduction cascade. The compound exhibits notable cytotoxic activity and anti-inflammatory properties. Its in vitro activity has been demonstrated in various cancer cell lines, establishing its potential as an anticancer agent. |
| ln Vivo |
In vivo, tenacissoside H (TDH) strongly inhibits tumor growth and volume. PCNA expression was significantly decreased after treatment of TDH. TDH downregulated proteins expression in PI3K/Akt-NF-κB transduction cascade[1].
Here, a mouse model of middle cerebral artery occlusion (MCAO) was established by an improved Longa-Zea method. tenacissoside H (TDH) was given by intraperitoneal injection once a day within 1 week before establishing the mouse MCAO model. The neurological functions of mice were evaluated and the apoptosis of neurons was also detected by the TUNEL method and Nissl's staining. ELISA and western blot were used to detect the expression of inflammatory factors, oxidation factors and proteins in the cerebral ischaemic cortex. The results revealed that tenacissoside H dose-dependently reduced neurological impairment, neuron apoptosis and brain oedema induced by MCAO. Furthermore, tenacissoside H attenuated the expression of pro-inflammatory cytokines (including interleukin (IL)-1β, IL-6 and tumour necrosis factor (TNF)-α), iNOS and nuclear factor (NF)-κB while increased production of anti-inflammatory cytokines (IL-4, IL-10 and BDNF) and proteins of tropomyosin-related kinase receptor B (TrkB) and PPARγ. Nevertheless, after the addition of TrkB inhibitor, the effects of tenacissoside H above were mostly restrained. In conclusion, tenacissoside H can protect mice against I/R-induced neurological impairments via modulating inflammation and oxidative stress through TrkB signalling[2]. Detailed in vivo activity data for Tenacissoside H are limited in publicly available literature. As a natural product with antitumor activity, Tenacissoside H is being investigated for its therapeutic potential in various cancer models. Its ability to modulate PI3K/AKT and MAPK signaling pathways suggests that it may have efficacy in vivo against tumors that are dependent on these pathways. The compound's anti-inflammatory activity also suggests potential applications in inflammatory diseases. Further in vivo studies are needed to fully characterize its therapeutic potential. |
| Enzyme Assay |
Tenacissoside H is a natural product and is not typically used in standard receptor binding assays. Its activity is assessed through cell-based assays measuring signaling pathway modulation. In these assays, cells are treated with Tenacissoside H at varying concentrations, and the phosphorylation status of key proteins in the PI3K/AKT and MAPK pathways is assessed by Western blot. NF-kappaB activation is assessed by measuring NF-kappaB nuclear translocation or by reporter gene assays. Cell viability and apoptosis are measured using standard assays such as MTT, flow cytometry for Annexin V staining, or caspase activity assays.
|
| Cell Assay |
Cell Proliferation Assay[1]
EC9706 cells were seeded in 96-well plates at a concentration of 1 × 104 cells/well with complete culture medium and allowed to adhere to the plate for 24 h. The adherent cells were incubated in the presence of various concentrations of Tenacissoside H (TDH) (0, 2, 4, 6, 8, and 10 mg·mL−1) for another 24 h and 48 h; MTT assay was conducted. The Optical Density (OD) absorbance of the treated samples against Blank Controlled (BC) Group was measured with EIA photometer with the wavelength of 570 nm.[1] Cell Cycle Analysis[1] Cells were seeded on Ø100 mm plates at a concentration of 1 × 106 cells/dish, 10 mL culture medium/dish, and incubated at 37°C in a 5% CO2 incubator for 24 h. Tenacissoside H (TDH) (10 mg·mL−1) and PCD (5 FU, 10 mg·mL−1) added in RPMI1640 culture medium were present for another 24 h. 3 mL of trypsin was applied into dishes; cells were harvested into 15 mL centrifuge tubes individually. The collected cells were centrifuged at 1000 rpm for 10 min, and, after 2 mL PBS was applied, the cells were centrifuged at 1000 rpm/min for 5 min, 2 times. A total of 100 μL PBS and 70% ethanol were applied into dishes and then left at 4°C overnight. After the cells were fixed at 4°C, 3 mL/tube of cold PBS was added, resting for 1 min, and then centrifuged at 1000 rpm for 5 min again. PBS was abandoned; then a mixture of solution, containing 850 μL of PBS, 10 μL of RNase A, 100 μL of 1% Triton-100, and 40 μL of 1 mg/mL PI, was added; cells were incubated for 5 min. Cellular assays for Tenacissoside H are performed using esophageal cancer cell lines or other cancer cell lines. Cells are cultured in appropriate media and treated with Tenacissoside H at varying concentrations for defined time periods. Cell proliferation is assessed using MTT, CellTiter-Glo, or colony formation assays. Apoptosis is assessed by measuring caspase activation, PARP cleavage, or Annexin V staining. Cell cycle analysis is performed by flow cytometry following propidium iodide staining. The PI3K/AKT and MAPK signaling pathways and NF-kappaB activation are assessed by Western blot analysis. |
| Animal Protocol |
Each of Tenacissoside H (TDH) and PCD group consisted of 6 animals. There were 12 animals in the negative model group (Group NM). TDH and 5 FU were dissolved with saline separately. 100 mg·kg−1 of TDH was injected intraperitoneally twice a week and 20 mg·kg−1 of 5-FU twice a week. Mice in Group NM were treated at the same time with 20 mL·kg−1 of saline.[1]
In the first part of the experiment, mice were randomly divided into sham operation group, solvent (DMSO) control group, Tenacissoside H (TH) low-dose group (20 mg/kg body weight), medium-dose group (40 mg/kg body weight) and high-dose group (80 mg/kg body weight). TH was dissolved in DMSO according to the instructions of the manufacturers. Each group contained 20 mice in all. After neurological function scoring, six mice were used to measure the volume of cerebral infarction and six mice were selected randomly to measure brain water content. For the solvent control group and TH-high, -medium and -low dose groups, the focal cerebral ischaemia model was established by thread embolization for 2 hours of ischaemia and 24 hours of reperfusion. The sham operation group and solvent control group were given the same volume of solvent (DMSO). All experimental groups were given intraperitoneal drug administration at 30 minutes before the operation. In the second part of the experiment, mice were divided into solvent control group, TH group (80 mg/kg body weight) and TH group (80 mg/kg body weight) +TrkB inhibitor group (K252a, 20 mg/kg body weight). All experimental groups were given intraperitoneal drug administration 30 minutes before operation.[2] In vivo studies with Tenacissoside H are conducted in mouse xenograft models using cancer cell lines. Tenacissoside H is administered via appropriate routes (e.g., intraperitoneal or oral) at defined doses and schedules. Tumor growth is monitored by caliper measurements, and tumor volumes are calculated. Tumor tissues are collected for histological analysis and assessment of signaling pathway modulation by immunohistochemistry or Western blot. Pharmacokinetic parameters may be determined from plasma samples collected at various time points. |
| ADME/Pharmacokinetics |
Tenacissoside H has a molecular weight of 794.97 and a molecular formula of C42H66O14. The compound is a steroidal saponin derived from Marsdenia tenacissima. Detailed pharmacokinetic data for Tenacissoside H are not extensively documented in publicly available literature. As a natural product with a complex glycosylated structure, its absorption, distribution, metabolism, and excretion properties are subjects of ongoing research. The compound is used as a quality control marker for Marsdenia tenacissima.
|
| Toxicity/Toxicokinetics |
Comprehensive toxicology data for Tenacissoside H are not extensively documented in publicly available sources. The compound is a natural product intended for research use only and is not approved for human therapeutic applications. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and adherence to institutional biosafety and chemical hygiene guidelines. The compound has a purity of >98%.
|
| References |
|
| Additional Infomation |
Reports indicate that Tenacissoside H has been discovered in Marsdenia tenacissima, and relevant data is available for reference.
Tenacissoside H (Tenacissimoside C) is a steroidal saponin derived from Marsdenia tenacissima that exhibits notable cytotoxic, anti-inflammatory, and antitumor activities. It has antitumor activity on esophageal cancer through arresting the cell cycle and regulating the PI3K/Akt-NF-kappaB transduction cascade. Tenacissoside H inhibits tumor cell proliferation and induces apoptosis by modulating signaling pathways such as PI3K/AKT and MAPK. The compound is also used as a quality control marker for Marsdenia tenacissima. Tenacissoside H is for research purposes only. |
| Molecular Formula |
C42H66O14
|
|---|---|
| Molecular Weight |
794.9651
|
| Exact Mass |
794.445
|
| CAS # |
191729-45-0
|
| PubChem CID |
75412560
|
| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
815.4±65.0 °C at 760 mmHg
|
| Flash Point |
235.5±27.8 °C
|
| Vapour Pressure |
0.0±0.6 mmHg at 25°C
|
| Index of Refraction |
1.551
|
| LogP |
4.73
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
13
|
| Heavy Atom Count |
56
|
| Complexity |
1490
|
| Defined Atom Stereocenter Count |
19
|
| SMILES |
O1C23C([H])([H])C([H])([H])[C@@]4([H])C([H])([H])[C@]([H])(C([H])([H])C([H])([H])[C@]4(C([H])([H])[H])[C@@]2([H])[C@@]([H])([C@]([H])([C@]2(C([H])([H])[H])[C@]([H])(C(C([H])([H])[H])=O)C([H])([H])C([H])([H])[C@]132)OC(C([H])([H])[H])=O)OC(C([H])(C([H])([H])[H])C([H])([H])C([H])([H])[H])=O)O[C@]1([H])C([H])([H])[C@]([H])([C@@]([H])([C@@]([H])(C([H])([H])[H])O1)O[C@@]1([H])[C@@]([H])([C@@]([H])([C@@]([H])([C@@]([H])(C([H])([H])[H])O1)O[H])OC([H])([H])[H])O[H])OC([H])([H])[H]
|
| InChi Key |
HRSFCYYMBMDMOU-ZIAOJATMSA-N
|
| InChi Code |
InChI=1S/C42H66O14/c1-11-20(2)37(47)54-34-35-39(7)15-13-26(53-29-19-28(48-9)32(23(5)50-29)55-38-31(46)33(49-10)30(45)22(4)51-38)18-25(39)12-16-41(35)42(56-41)17-14-27(21(3)43)40(42,8)36(34)52-24(6)44/h20,22-23,25-36,38,45-46H,11-19H2,1-10H3/t20?,22-,23-,25+,26+,27+,28-,29+,30-,31-,32-,33-,34+,35-,36-,38+,39+,40+,41+,42-/m1/s1
|
| Chemical Name |
[(1S,3R,6R,7S,8S,9S,10S,11S,14S,16S)-6-acetyl-8-acetyloxy-14-[(2R,4R,5R,6R)-5-[(2S,3R,4R,5R,6R)-3,5-dihydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-7,11-dimethyl-2-oxapentacyclo[8.8.0.01,3.03,7.011,16]octadecan-9-yl] 2-methylbutanoate
|
| Synonyms |
Tenacissoside H; 191729-45-0; (3beta,5alpha,11alpha,12beta,14beta,17alpha)-12-(Acetyloxy)-3-[[2,6-dideoxy-4-O-(6-deoxy-3-O-methyl-beta-D-allopyranosyl)-3-O-methyl-beta-D-arabinohexopyranosyl]oxy]-8,14-epoxy-11-(2-methyl-1-oxobutoxy)pregnan-20-one; [(1S,3R,6R,7S,8S,9S,10S,11S,14S,16S)-6-acetyl-8-acetyloxy-14-[(2R,4R,5R,6R)-5-[(2S,3R,4R,5R,6R)-3,5-dihydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-7,11-dimethyl-2-oxapentacyclo[8.8.0.01,3.03,7.011,16]octadecan-9-yl] 2-methylbutanoate; Tenacissimoside C;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~125.79 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.14 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2579 mL | 6.2895 mL | 12.5791 mL | |
| 5 mM | 0.2516 mL | 1.2579 mL | 2.5158 mL | |
| 10 mM | 0.1258 mL | 0.6290 mL | 1.2579 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
