Kinetin riboside exhibits activities that hinder cell growth and induce apoptosis in a range of human cancer cell lines. It effectively curbs the proliferation of HCT-15 human colon cancer cells, with the inhibition becoming more pronounced with increasing doses (IC50=2.5 μM)[1]. Kinetin riboside triggers cell death processes in HeLa and B16F-10 melanoma cells. It compromises the mitochondrial membrane integrity, leading to cytochrome c release and caspase-3 activation. The exposure to kinetin riboside results in increased levels of Bad and decreased levels of Bcl-2[2].
To evaluate the effect of Kinetin riboside on mitophagy and mitochondrial fusion. Results showed that KR activated mitophagy and relaxed mitochondrial hyperfusion in a concentration-dependent manner.
Nat Commun. 2024 Feb 6;15(1):1124
MIO-M1 Müller cells
0.3 - 5 µM
72 hours
To evaluate the effect of Kinetin riboside on mitochondrial dynamics and function under diabetic conditions. Results showed that KR restored mitochondrial membrane potential, improved mitochondrial bioenergetics, and activated mitophagy.
Nat Commun. 2024 Feb 6;15(1):1124
HEK293 Flp-In TRex HEK293 cells
50 μM
3, 6, 12, 24, 48 hours
Time-dependent evaluation of PINK1 activation by KR ProTide 13, with the most significant activation observed at 24 hours.
J Med Chem. 2017 Apr 27;60(8):3518-3524
HEK293 Flp-In TRex HEK293 cells
50 μM
24 hours
To evaluate the activation of PINK1 by Kinetin riboside and its ProTides, results showed that KR and three ProTides (11, 13, 14) significantly activated PINK1 in the absence of CCCP, as evidenced by enhanced Parkin Ser65 phosphorylation.
J Med Chem. 2017 Apr 27;60(8):3518-3524
HeLa cells
50 μM
24 hours
Inhibited CCCP- and niclosamide-induced ubiquitin phosphorylation
J Med Chem. 2023 Jun 8;66(11):7645-7656
A172 cells
20, 40, 80 µM
6 hours
To evaluate the effect of KR on A172 cell apoptosis, results showed that KR induced apoptosis in a concentration-dependent manner.
Apoptosis. 2020 Dec;25(11-12):835-852
T47D cells
20, 40, 80 µM
6 hours
To evaluate the effect of KR on T47D cell apoptosis, results showed that KR induced apoptosis in a concentration-dependent manner.
Apoptosis. 2020 Dec;25(11-12):835-852
HepG2 cells
20, 40, 80 µM
6 hours
To evaluate the effect of KR on HepG2 cell proliferation, results showed that KR inhibited cell proliferation in a concentration- and time-dependent manner and induced apoptosis.
Apoptosis. 2020 Dec;25(11-12):835-852
Human dermal neonatal foreskin Hs27 fibroblasts
0.18 ± 0.01 μM
72 hours
To assess the antiproliferative activity of FAdo, results showed significant inhibition of cell proliferation at submicromolar concentrations.
Biochem Pharmacol. 2009 Apr 1;77(7):1125-38
Primary human epidermal keratinocytes
0.11 ± 0.03 μM
72 hours
To assess the antiproliferative activity of FAdo, results showed significant inhibition of cell proliferation at submicromolar concentrations.
Biochem Pharmacol. 2009 Apr 1;77(7):1125-38
HCT116 colon carcinoma cells
0.72 ± 0.02 μM
72 hours
To assess the antiproliferative activity of FAdo, results showed significant inhibition of cell proliferation at submicromolar concentrations.
Biochem Pharmacol. 2009 Apr 1;77(7):1125-38
HT29 colon carcinoma cells
3.00 ± 0.65 μM
72 hours
To assess the antiproliferative activity of FAdo, results showed significant inhibition of cell proliferation at micromolar concentrations.
Biochem Pharmacol. 2009 Apr 1;77(7):1125-38
LOX metastatic melanoma cells
0.16 ± 0.02 μM
72 hours
To assess the antiproliferative activity of FAdo, results showed significant inhibition of cell proliferation at submicromolar concentrations.
Biochem Pharmacol. 2009 Apr 1;77(7):1125-38
G361 Human melanoma cells
1.52 ± 0.52 μM
72 hours
To assess the antiproliferative activity of FAdo, results showed significant inhibition of cell proliferation at micromolar concentrations.
Biochem Pharmacol. 2009 Apr 1;77(7):1125-38
A375 melanoma cells
0.28 ± 0.01 μM
72 hours
To assess the antiproliferative activity of FAdo, results showed significant inhibition of cell proliferation at submicromolar concentrations.
Biochem Pharmacol. 2009 Apr 1;77(7):1125-38
MiaPaCa-2 pancreas carcinoma cells
0.27 ± 0.09 μM
72 hours
To assess the antiproliferative activity of FAdo, results showed significant inhibition of cell proliferation at submicromolar concentrations.
Biochem Pharmacol. 2009 Apr 1;77(7):1125-38
T98G cells
40, 80, 200 μM
24 hours
To evaluate the effects of KR and 7-deazaKR on proliferation and apoptosis in T98G cells. Results showed that KR and 7-deazaKR inhibited cell proliferation and induced apoptosis in a dose-dependent manner.
Antioxidants (Basel). 2021 Jun 12;10(6):950
Primary CD138+ myeloma cells
10 μM
16 hours
In 4 out of 5 primary myeloma cell samples, kinetin riboside significantly suppressed the major cyclin D protein expression, but had no effect in one plasma cell leukemia sample.
J Clin Invest. 2008 May;118(5):1750-64
U266 myeloma cells
10 μM
16 hours
Kinetin riboside significantly suppressed cyclin D1 protein expression but had no significant effect on cyclin D3.
J Clin Invest. 2008 May;118(5):1750-64
KMS11 myeloma cells
10 μM
16 hours
Kinetin riboside significantly suppressed cyclin D2 protein expression but had no significant effect on cyclin D3.
J Clin Invest. 2008 May;118(5):1750-64
H929 myeloma cells
10 μM
6 hours
Kinetin riboside significantly suppressed cyclin D1 and D2 protein expression within 6 hours, leading to cell cycle arrest at G0/G1 phase.
J Clin Invest. 2008 May;118(5):1750-64
Kinetin riboside/激动素核苷 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Ins2Akita diabetic mouse model
Oral (via drinking water)
60 mg/L (equalling 90 mg/kg/day)
Three times per week for 2 weeks or from 4 to 8 months
To evaluate the neuroprotective effects of Kinetin riboside in the diabetic mouse retina. Results showed that KR restored mitochondrial turnover, improved retinal neurodegeneration, and protected retinal function regardless of glycaemic status.
Nat Commun. 2024 Feb 6;15(1):1124
Nude mice
MY5 and 8226 myeloma xenograft models
Intraperitoneal and subcutaneous injection
85 mg/kg/dose, 4-5 times daily
4-5 times daily, continuous treatment
Kinetin riboside significantly inhibited tumor growth in MY5 and 8226 myeloma xenograft models, with tumor regression observed at 5 times daily dosing.
J Clin Invest. 2008 May;118(5):1750-64
Mice
Intranasal vesicular stomatitis virus (VSV) infection model
To study the effects of kinetin riboside and isopentenyladenosine on (polyrI)·(polyrC)-induced interferon production and antiviral protection. Results showed that these nucleoside analogs significantly reduced the interferon-inducing capacity and antiviral protection of (polyrI)·(polyrC).
J Clin Invest. 1970 Aug;49(8):1565-77
Kinetin riboside/激动素核苷 动物研究
Animal study
Kinetin riboside markedly inhibits the progression of tumors. It is observed that the strongest response against melanoma is achieved with a dosage of 40 mg/kg[2].
搜索
