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Chemical Structure| 32507-66-7 Chemical Structure| 32507-66-7

Structure of Isorhapontigenin
CAS No.: 32507-66-7

Chemical Structure| 32507-66-7

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Isorhapotogenin is a natural product isolated and purified from the herbs of Gnetum montanum Markgr..

Synonyms: ISOR

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Product Details of Isorhapontigenin

CAS No. :32507-66-7
Formula : C15H14O4
M.W : 258.27
SMILES Code : OC1=CC(/C=C/C2=CC=C(O)C(OC)=C2)=CC(O)=C1
Synonyms :
ISOR
MDL No. :MFCD12407151
InChI Key :ANNNBEZJTNCXHY-NSCUHMNNSA-N
Pubchem ID :5318650

Safety of Isorhapontigenin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Patient-derived glioblastoma spheres JX6 20 μM 24 hours To evaluate the inhibitory effect of ISO on anchorage-independent growth in JX6 cells. Results showed that ISO significantly inhibited growth in JX6 cells. Neuro Oncol. 2016 Jun;18(6):830-9
Patient-derived glioblastoma spheres D456 20 μM 24 hours To evaluate the inhibitory effect of ISO on anchorage-independent growth and induction of G0-G1 cell cycle arrest in D456 cells. Results showed that ISO significantly inhibited growth and induced G0-G1 arrest in D456 cells. Neuro Oncol. 2016 Jun;18(6):830-9
human cervical cancer HeLa cells 2.5-10 μM 24 hours Induced autophagy and inhibited anchorage-independent growth Autophagy. 2016 Aug 2;12(8):1229-39
human bladder cancer T24T cells 2.5-10 μM 24 hours Induced autophagy and inhibited anchorage-independent growth Autophagy. 2016 Aug 2;12(8):1229-39
human bladder cancer UMUC3 cells 2.5-10 μM 24 hours Induced autophagy and inhibited anchorage-independent growth Autophagy. 2016 Aug 2;12(8):1229-39
Neonatal rat cardiomyocytes (NRCMs) 1-40 μmol/L 12 hours Isor effectively alleviated Dox-induced cardiomyocyte apoptosis in a dose-dependent manner. Acta Pharm Sin B. 2021 Mar;11(3):680-693
Primary human airway epithelial cells 1-100 μM 1 hour To evaluate the inhibitory effects of isorhapontigenin on IL-6 and CXCL8 release, results showed that isorhapontigenin concentration-dependently inhibited IL-6 and CXCL8 release, with IC50 values at least twofold lower than those of resveratrol. Br J Pharmacol. 2017 Jul;174(13):2043-2059
A549 cells 1-100 μM 1 hour To evaluate the inhibitory effects of isorhapontigenin on IL-6 and CXCL8 release, results showed that isorhapontigenin concentration-dependently inhibited IL-6 and CXCL8 release, with IC50 values at least twofold lower than those of resveratrol. Br J Pharmacol. 2017 Jul;174(13):2043-2059
UMUC3 cells 10 μM 24 hours ISO treatment upregulated RAC1 protein translation and MKK7/JNK phosphorylation/activation, thereby promoting autophagic responses and inhibiting bladder cancer cell invasion. Cell Death Dis. 2022 Aug 31;13(8):753
T24T cells 20 μM 24 hours ISO inhibits invasion of bladder cancer cells by upregulating METTL14 Cancer Lett. 2021 Nov 1;520:400-408
U5637 cells 20 μM 24 hours ISO inhibits invasion of bladder cancer cells by upregulating METTL14 Cancer Lett. 2021 Nov 1;520:400-408
UMUC3 cells 5 μM 12 hours ISO treatment increased miR-137 expression and specifically inhibited the invasion ability of UMUC3 cells Mol Ther Nucleic Acids. 2018 Sep 7;12:337-349
T24T cells 10 μM 12 hours ISO treatment increased miR-137 expression and specifically inhibited the invasion ability of T24T cells Mol Ther Nucleic Acids. 2018 Sep 7;12:337-349
SH-SY5Y cells 1, 5, 10, and 20 μM 24 hours To evaluate the neuroprotective effects of isorhapontigenin against Aβ peptide (25-35)-induced cell death. Results showed that pre-treatment with isorhapontigenin for 24 hours significantly elevated cell viabilities and produced significant differences as compared to the control (p < 0.05*, 0.01**, 0.001***). Antioxidants (Basel). 2023 Jun 29;12(7):1362
T24T bladder cancer cells 20 μM 12 hours ISO significantly inhibited sphere formation and invasivity of T24T cells by down-regulating CD44 protein expression Cell Mol Life Sci. 2020 Jan;77(2):351-363
Cl41 cells 5 μM 24 hours To study the effect of ISO on Cyclin D1 expression in normal Cl41 cells, results showed that ISO had minimal effect on Cyclin D1 expression. Mol Cancer Ther. 2013 Aug;12(8):1492-503
RT4 cells 5 μM 24 hours To study the effect of ISO on Cyclin D1 expression in RT4 cells, results showed that ISO slightly inhibited Cyclin D1 expression. Mol Cancer Ther. 2013 Aug;12(8):1492-503
RT112 cells 5 μM 24 hours To study the effect of ISO on Cyclin D1 expression in RT112 cells, results showed that ISO significantly inhibited Cyclin D1 expression. Mol Cancer Ther. 2013 Aug;12(8):1492-503
UMUC3 cells 5-60 μM 48 hours To evaluate the inhibitory effect of ISO on the proliferation of human bladder cancer cells, results showed that ISO significantly reduced the viability of UMUC3 and RT4 cells in a concentration-dependent manner. Mol Cancer Ther. 2013 Aug;12(8):1492-503

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Xenograft model with human bladder cancer T24T cells 150 mg/kg/d Once daily, duration Markedly inhibited xenograft tumor growth Autophagy. 2016 Aug 2;12(8):1229-39
C57BL/6 mice Dox-induced cardiotoxicity model Intraperitoneal injection 30 mg/kg/day Once daily for 3 weeks Isor significantly protected mice against Dox-induced cardiotoxicity and improved cardiac function. Acta Pharm Sin B. 2021 Mar;11(3):680-693
Sprague-Dawley rats Intravenous injection and oral 30 μmol/kg (i.v.) and 600 μmol/kg (p.o.) Single dose To evaluate the pharmacokinetic profile of isorhapontigenin, results showed that its oral bioavailability was approximately 50% higher than resveratrol. Br J Pharmacol. 2017 Jul;174(13):2043-2059
Mice BBN-induced muscle-invasive bladder cancer model 150 mg/kg/day Daily administration ISO significantly inhibited BBN-induced muscle-invasive bladder cancer formation in mice, with an inhibition rate of over 90%. Cell Death Dis. 2022 Aug 31;13(8):753
Wistar male mice Gastric gavage 150 mg/kg Single dose, observation time points included 0.033h, 0.083h, 0.17h, 0.25h, 0.5h, 0.75h, 1h, 1.5h, 2h and 4h To study the pharmacokinetics of ISO in mice, results showed that the maximum observed concentration (Cmax) of ISO in mouse serum was 12.35 μg/ml (47.9 μM), reached at 0.17 h (10 min). Mol Cancer Ther. 2013 Aug;12(8):1492-503

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.87mL

0.77mL

0.39mL

19.36mL

3.87mL

1.94mL

38.72mL

7.74mL

3.87mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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