Kaempferitrin (KM) is a natural flavonoid, possesses antinociceptive, anti-inflammatory, anti-diabetic, antitumoral and chemopreventive effects, and activates insulin signaling pathway. Kaempferitrin causes survival rates higher than 90% at 1-20 μM in matured 3T3-L1 adipocyte, and the survival rates decline rapidly at 25 and 50 μM. Kaempferitrin (15 μM) increases insulin receptor beta tyrosine phosphorylation and tyrosine phosphorylation of the insulin receptor substrate 1, and such effects are similar to that of 10 nM insulin. In addition, Kaempferitrin increases the total levels of Glu4 protein in differentiated cells and secreted adiponectin in mature 3T3-L1 adipocytes[3]. KM induces high cytotoxic effects in vitro and in vivo against HeLa cells. Kaempferitrin (2.5, 10 and 25 mg/kg, i.p.) markedly suppresses the growth of tumor by 40%, 87% and 97%, and decreases tumor weight by 37%, 81% and 95%, respectively in nu/nu mice bearing HeLa tumor[4]. Kaempferitrin decreased the levels of interleukin (IL)-1β, IL-6, tumor necrosis factor (TNF)-α, matrix metalloproteinase (MMP)-1, and MMP-3 in MH7A cells. Moreover, kaempferitrin blocked the activation of nuclear factor-κB (NF-κB) and protein kinase B (Akt)/mammalian target of rapamycin (mTOR) pathways. Furthermore, treatment with kaempferitrin decreased paw thickness and arthritis scores, and reduced the serum levels of IL-1β, IL-6, and TNF-α in a collagen-induced arthritis mouse model[5]. KM effectively increased SOD (Superoxide dismutase) activity, decreased MDA (malondialdehyde) levels, suppressed ROS (Reactive oxygen species) generation, and protected against OS (oxidative stress) in AGE-induced (Advanced glycation end products) GMCs[6].
Kaempferitrin/山奈苷 细胞实验
Cell Line
Concentration
Treated Time
Description
References
SH-SY5Y cells (undifferentiated and differentiated)
5–50 µM
24 hours
Evaluation of the protective effect of Kaempferitrin against doxorubicin (Dox)-induced cell damage showed that at 5–50 µM, Krg was ineffective in counteracting Dox-induced cytotoxicity.
Int J Mol Sci. 2021 Sep 26;22(19):10363
SH-SY5Y cells (differentiated)
1–50 µM
24 hours
Evaluation of the protective effect of Kaempferitrin against 6-OHDA-induced cell damage showed that in differentiated SH-SY5Y cells, Krg did not exhibit significant neuroprotective activity.
Int J Mol Sci. 2021 Sep 26;22(19):10363
SH-SY5Y cells (undifferentiated)
1 and 50 µM
24 hours
Evaluation of the protective effect of Kaempferitrin against 6-OHDA-induced cell damage showed that at 1 and 50 µM, Krg partially protected undifferentiated SH-SY5Y cells from 6-OHDA-induced toxicity.
Int J Mol Sci. 2021 Sep 26;22(19):10363
SH-SY5Y cells (undifferentiated)
50 µM
18 hours
Evaluation of the effect of Kaempferitrin on H2O2-induced cathepsin D activity showed that Krg (50 µM) significantly reduced the elevated cathepsin D activity induced by H2O2.
Int J Mol Sci. 2021 Sep 26;22(19):10363
SH-SY5Y cells (differentiated)
50 µM
24 hours
Evaluation of the protective effect of Kaempferitrin against H2O2-induced cell damage showed that in differentiated SH-SY5Y cells, Krg did not exhibit significant neuroprotective activity.
Int J Mol Sci. 2021 Sep 26;22(19):10363
SH-SY5Y cells (undifferentiated)
50 µM
24 hours
Evaluation of the protective effect of Kaempferitrin against H2O2-induced cell damage showed that at the highest concentration (50 µM), Krg partially protected undifferentiated SH-SY5Y cells from H2O2-induced damage.
Int J Mol Sci. 2021 Sep 26;22(19):10363
SH-SY5Y cells (undifferentiated and differentiated)
50 µM
24 hours
Biosafety assessment of Kaempferitrin showed that at the highest tested concentration (50 µM), Krg did not significantly affect the viability of undifferentiated and differentiated SH-SY5Y cells.
Int J Mol Sci. 2021 Sep 26;22(19):10363
SH-SY5Y cells (undifferentiated)
5–50 µM
48 and 72 hours
Evaluation of the effect of Kaempferitrin on cell proliferation showed that Krg at 5–50 µM had no significant impact on the proliferation rate of undifferentiated SH-SY5Y cells under 10% FBS conditions.
Int J Mol Sci. 2021 Sep 26;22(19):10363
rat glomerular mesangial cells (GMCs)
10, 20, 35 μM
24 hours
KM effectively increased SOD activity, decreased MDA levels, suppressed ROS generation, and protected against OS in AGE-induced GMCs
Int J Mol Sci. 2018 Oct 26;19(11):3334
CHO-K1 cells
100 μM
24 hours
Evaluate the effect of KO and KR on PD-1/PD-L1 blockade, results showed that KO and KR blocked PD-1/PD-L1 interaction at non-cytotoxic concentrations
Int J Mol Sci. 2020 May 3;21(9):3239
Jurkat T cells
100 μM
24 hours
Evaluate the effect of KO and KR on PD-1/PD-L1 blockade, results showed that KO and KR blocked PD-1/PD-L1 interaction at non-cytotoxic concentrations
Int J Mol Sci. 2020 May 3;21(9):3239
human small cell lung cancer cells H446
125, 250, 500 µg/mL
48 hours
LLF significantly inhibited the proliferation of H446 cells.
Biol Res. 2021 Mar 2;54(1):7
human lung cancer A549 cells
125, 250, 500 µg/mL
48 hours
LLF significantly inhibited the proliferation of A549 cells, induced apoptosis, upregulated the expression of p38 MAPK, caspase-3, caspase-9, and Bax, and downregulated the expression of Cu/Zn SOD, CAT, Nrf2, NQO1, HO-1, and Bcl-2 via the ROS/p38 MAPK pathway.
Biol Res. 2021 Mar 2;54(1):7
HepG2 cells
10 μM
24 hours
To study the effect of Kaempferitrin on the secretome of HepG2 cells, it was found that 33 genes were consistently up/down-regulated in two biological samples, and finally 18 genes were screened. Among them, 5 proteins were exosomal markers or reported with high frequency in exosomes/secretory vesicles. In addition, the conditioned medium of Kaempferitrin-treated cells showed increased vesicle size and reduced number of small vesicles.
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