Kaempferol 3-O-gentiobioside

Kaempferol 3-O-gentiobioside is an orally active flavonoid, with a K_a value of 57 µM against human NOTCH1 and an IC₅₀ value of 50 μM against α-glucosidase. Kaempferol 3-O-gentiobioside inhibits the NOTCH signaling pathway. It downregulates the expression of TLR4 and NLRP3, and suppresses the activation and nuclear translocation of NF-κB. Kaempferol 3-O-gentiobioside inhibits the expression of MUC5AC, reduces nitrite and ROS levels, and attenuates excessive mucus secretion. It exhibits antibacterial activity, reducing the formation and growth of MRSA biofilms. Kaempferol 3-O-gentiobioside blocks the TGF-β/ALK5/Smad signaling pathway and inhibits epithelial-mesenchymal transition. It suppresses the proliferation, migration, invasion and metastatic growth of tumor cells. Kaempferol 3-O-gentiobioside alleviates airway inflammation and mucus hypersecretion in mice with allergic asthma. It reduces the volume of ovarian cancer xenografts in mice. Kaempferol 3-O-gentiobioside can be used in research related to allergic asthma, diabetes, MRSA infection, breast cancer, gastric cancer and ovarian cancer^[1][2][3][4]. In Vitro:Kaempferol 3-O-gentiobioside binds to recombinant human NOTCH1 with a K_d value of 57 µM^[1].
Kaempferol 3-O-gentiobioside (0-100 µM; 24-72 h) exhibits dose- and time-dependent cytotoxicity in 16HBE cells, while concentrations of 5, 25 and 50 µM show no cytotoxicity at 24 h^[1].
Kaempferol 3-O-gentiobioside (0-50 µM; 1 h pretreatment, followed by 24 h IL-13 stimulation) dose-dependently reduces nitrite production, decreases ROS levels, inhibits the secretion of IgE, TNF-α, histamine, IL-1β, IL-6 and IL-8, and suppresses the mRNA and protein expression of MUC5AC in IL-13-stimulated 16HBE cells^[1].
Kaempferol 3-O-gentiobioside (0-50 µM; administered 24 h after IL-13 stimulation) dose-dependently inhibits IL-13-induced activation of the NOTCH pathway, including downregulating the expression of NOTCH1, NOTCH2, NOTCH3 and DLL4 in 16HBE cells, while also reducing the basal expression levels of these components^[1].
Kaempferol 3-O-gentiobioside (0-50 µM; administered 24 h after IL-13 stimulation) inhibits IL-13-induced activation of the TLR4/NF-κB/NLRP3 pathway in 16HBE cells, including downregulating the expression of TLR4, NLRP3, p-IκBα and p-P65, as well as suppressing the activation of NF-κB/P65^[1].
Kaempferol 3-O-gentiobioside moderately inhibits yeast α-glucosidase (derived from Saccharomyces cerevisiae) with an IC₅₀ value of 50 μM^[2].
Kaempferol 3-O-gentiobioside (0-100 μM; 24 h) exhibits concentration-dependent antibacterial activity against methicillin-resistant *Staphylococcus aureus* (ATCC 43300), with an MIC of 8.3 μM and an MBC of 16.5 μM, and inhibits biofilm formation^[3].
Kaempferol 3-O-gentiobioside (pretreated for 2 h, followed by stimulation with TGFβ1 for 24 h) potently inhibits the TGF-β/ALK5/Smad signaling pathway in HACAT cells, with an IC₅₀ of 2.589 μM^[4].
Kaempferol 3-O-gentiobioside (0-4 μM; 2 h) inhibits the TGF-β/ALK5/Smad signaling pathway in MDA-MB-231, AGS and SKOV3IP1 cells in a concentration-dependent manner by reducing the levels of p-Smad2 and Smad4^[4].
Kaempferol 3-O-gentiobioside (24 h) inhibits the proliferation of MDA-MB-231, AGS and SKOV3IP1 cells, with IC₅₀ values of 6.83 μM, 9.6 μM and 11.12 μM, respectively^[4].
Kaempferol 3-O-gentiobioside (0-4 μM; 24 h) reduces the colony-forming ability of MDA-MB-231, AGS and SKOV3IP1 cells in a concentration-dependent manner^[4].
Kaempferol 3-O-gentiobioside (2 μM; 24 h) inhibits TGFβ-induced migration and invasion of MDA-MB-231, AGS and SKOV3IP1 cells^[4].
Kaempferol 3-O-gentiobioside (0-4 μM; 2 h) concentration-dependently reverses TGFβ-induced epithelial-mesenchymal transition (EMT) in MDA-MB-231, AGS and SKOV3IP1 cells by restoring E-cadherin levels and reducing the levels of N-cadherin, vimentin and snail transcription factor (snail)^[4]. In Vivo:Kaempferol 3-O-gentiobioside (10-40 mg/kg; p.o.; once daily; for 7 consecutive days) dose-dependently alleviates airway inflammation and mucus hypersecretion in OVA (HY-W250978)-induced allergic asthma mice^[1].
Kaempferol 3-O-gentiobioside (40 mg/kg; p.o.; once daily; for 30 consecutive days) reduces the average volume of ovarian cancer xenograft tumors to 584 mm^3[4].