Hinokiflavone, a natural product isolated and purified from the leaves of Platycladus orientalis, with significant cytotoxicity, can inhibit the activity of MMP-9.
Hinokiflavone/扁柏双黄酮 细胞实验
Cell Line
Concentration
Treated Time
Description
References
LO2
0, 10, 20, 40, 80, 120, 160, 240, 320 µmol/L
24, 48, 72 hours
HF showed much lower cytotoxicity against LO2 cells, with IC50 values of 159.1 ± 5.6 µmol/L (24 hours), 104.7 ± 4.5 µmol/L (48 hours), and 75.7 ± 2.8 µmol/L (72 hours).
J Cell Mol Med. 2020 Jul;24(14):8151-8165
HepG2
0, 10, 20, 30, 40, 60, 80, 100 µmol/L
24, 48, 72 hours
HF significantly inhibited the proliferation of HepG2 cells, with IC50 values of 80.8 ± 2.6 µmol/L (24 hours), 57.5 ± 5.3 µmol/L (48 hours), and 28.1 ± 2.7 µmol/L (72 hours). HF induced G0/G1 phase cell cycle arrest by up-regulating the p53/p21Cip1 signaling pathway and down-regulating G0/G1 phase-related cell cycle regulatory proteins.
J Cell Mol Med. 2020 Jul;24(14):8151-8165
SMMC-7721
0, 10, 20, 30, 40, 60, 80, 100 µmol/L
24, 48, 72 hours
HF significantly inhibited the proliferation of SMMC-7721 cells, with IC50 values of 74.4 ± 8.1 µmol/L (24 hours), 60.3 ± 2.9 µmol/L (48 hours), and 33.0 ± 2.6 µmol/L (72 hours). HF induced G0/G1 phase cell cycle arrest by up-regulating the p53/p21Cip1 signaling pathway and down-regulating G0/G1 phase-related cell cycle regulatory proteins.
J Cell Mol Med. 2020 Jul;24(14):8151-8165
Human lung adenocarcinoma A549 cells
20 μg/mL
24 hours
To measure mitochondrial membrane potential, the mitochondrial membrane potential in the HF hybrid micelles group was significantly decreased compared with that in the free HF group, indicating that HF hybrid micelles could induce mitochondria-mediated apoptosis.
Drug Deliv. 2020 Dec;27(1):565-574
Human lung adenocarcinoma A549 cells
0.78 μg/mL to 50 μg/mL
24 hours
To evaluate the cytotoxicity of HF hybrid micelles on A549 cells, the results showed that the IC50 value of HF hybrid micelles (7.81 μg/mL) was lower than that of free HF (19.34 μg/mL), indicating that HF hybrid micelles had higher cytotoxicity.
Drug Deliv. 2020 Dec;27(1):565-574
HeLa cells
500 μM
90 minutes
Inhibited splicing of Ad1 and HPV18 E6 pre-mRNAs, preventing formation of the B complex
Elife. 2017 Sep 8;6:e27402
AML-2 cells
0–25 μM
24 hours
Hinokiflavone attenuated the ubiquitination levels of MDM2 and p53 in AML-2 cells.
Biomolecules. 2022 Apr 27;12(5):643
Klebsiella pneumoniae clinical isolates
0.25-0.5 µg/mL
Evaluate the antibacterial activity of Hinokiflavone against Klebsiella pneumoniae, showing the highest antibacterial activity
Pharmaceuticals (Basel). 2021 Aug 1;14(8):756
HT-29 cells
1-10 μM
24 hours
To evaluate the inhibitory effect of Hinokiflavone on LPS-induced inflammatory responses, results showed that Hinokiflavone suppressed the production of IL-8 and downregulated the expression of iNOS and COX-2.
Molecules. 2018 Apr 17;23(4):926
RAW 264.7 cells
1-10 μM
24 hours
To evaluate the inhibitory effect of Hinokiflavone on LPS-induced inflammatory responses, results showed that Hinokiflavone suppressed the production of NO, IL-6, TNF-α, and downregulated the expression of iNOS and COX-2.
Molecules. 2018 Apr 17;23(4):926
S. aureus USA300
64 μg/mL
Assess the effect of Hinokiflavone on the growth of S. aureus USA300, showing no effect on bacterial growth at 64 mg/mL.
Antimicrob Agents Chemother. 2022 Aug 16;66(8):e0024022
HEK293T cells
256 μg/mL
24 hours
Evaluate the cytotoxicity of Hinokiflavone on HEK293T cells, showing no cytotoxicity at 256 mg/mL.
Antimicrob Agents Chemother. 2022 Aug 16;66(8):e0024022
3T3-L1 cells
10 μM
Assessed the effect of HF on apoptosis in differentiated 3T3-L1 cells, showing HF induced apoptosis via mitochondrial pathway
J Biol Chem. 2024 Sep;300(9):107721
Hinokiflavone/扁柏双黄酮 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c-nu mice
HCC xenograft model
Intraperitoneal injection
4 or 8 mg/kg
Every other day for ten times
HF significantly inhibited the growth of HCC xenografts, with the average tumour size reduced to 831.8 mm3 and 523 mm3 in the 4 mg/kg and 8 mg/kg groups, respectively, compared to 1604 mm3 in the control group. HF up-regulated the expression levels of cleaved PARP, cleaved caspase-3, and p-JNK, and apoptosis was confirmed by TUNEL assay.
J Cell Mol Med. 2020 Jul;24(14):8151-8165
BALB/c nude mice
A549 xenograft tumor model
Oral administration
80 mg/kg
Administered on days 2, 4, 6, 8, 10, and 12, lasting for 12 days
To evaluate the in vivo antitumor effect of HF hybrid micelles, the results showed that the tumor volume and weight in the HF hybrid micelles group were significantly lower than those in the free HF group and the control group, with a tumor inhibition rate of 64.76%, significantly higher than that in the free HF group (45.92%).
Drug Deliv. 2020 Dec;27(1):565-574
C57BL/6J mice
MRSA-induced lethal pneumonia model
Subcutaneous injection
100 mg/kg/d
Every 12 hours for 96 hours
Evaluate the protective effect of Hinokiflavone against MRSA-induced lethal pneumonia, showing more potent than vancomycin alone when combined with vancomycin.
Antimicrob Agents Chemother. 2022 Aug 16;66(8):e0024022
C57BL/6J mice
High-fat diet-induced obesity model
Intraperitoneal injection
5 mg/kg, 10 mg/kg, 20 mg/kg
Administered every other day for 6 weeks
HF suppressed obesity by inducing apoptosis in adipose tissue, improving glucose tolerance and insulin sensitivity
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