Bruceine D is an effective botanical insect antifeedant with outstanding systemic properties, causing potent pest growth inhibitory activity[3]. Bruceine D is a Notch inhibitor with anti-cancer activity and induces apoptosis in several human cancer cells. BD significantly inhibited liver tumor growth and enhanced the therapeutic effects of sorafenib in various murine HCC (Hepatocellular carcinoma) models[4]. Bruceine D exhibited potent cytotoxicity to K562 cells with IC50 of 6.37 ± 0.39 μM. In addition, bruceine D inhibited the phosphorylation of AKT and ERK. It's indicative that the potent anticancer activity of bruceine D be related to MAPK and PI3K pathways[5]. Bruceine D markedly inhibited the proliferation of wild‑type NSCLC (non‑small‑cell lung cancer) cells and epidermal growth factor receptor‑mutant cells in a dose‑ and time‑dependent manner, and significantly decreased the colony‑forming ability and migration of A549 cells[6].
Bruceine D/鸦胆子苦素D 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MDA-MB-453
3.13–25 μM
48 h
BD inhibited MDA-MB-453 cell viability with an IC50 of 9.919 μM.
J Adv Res. 2024 Apr;58:193-210
MCF-7
0.78–25 μM
48 h
BD inhibited MCF-7 cell viability with an IC50 of 2.805 μM.
J Adv Res. 2024 Apr;58:193-210
MDA-MB-231
0.78–25 μM
48 h
BD inhibited MDA-MB-231 cell viability with an IC50 of 2.328 μM.
J Adv Res. 2024 Apr;58:193-210
MDA-MB-468
0.39–25 μM
48 h
BD inhibited MDA-MB-468 cell viability with an IC50 of 1.092 μM.
J Adv Res. 2024 Apr;58:193-210
SGC7901 cells
1.2 μM
2 weeks
BD significantly inhibited the clonogenicity of SGC7901 cells.
Front Pharmacol. 2020 Nov 24;11:584960
NCI-H292
2.5, 5, 10, 20, 30, and 40 µM
24 h and 48 h
BD inhibited human lung cancer cell growth in a dose- and time-dependent manner. The IC50 (24 h) values for A549 and NCI-H292 cells were 36.76 and 31.22 μM, respectively, and the IC50 (48 h) values were 17.89 and 14.42 μM, respectively.
Cell Death Dis. 2020 Feb 18;11(2):126
A549 cells
2.5, 5, 10, 20, 30, and 40 µM
24 h and 48 h
BD inhibited human lung cancer cell growth in a dose- and time-dependent manner. The IC50 (24 h) values for A549 and NCI-H292 cells were 36.76 and 31.22 μM, respectively, and the IC50 (48 h) values were 17.89 and 14.42 μM, respectively.
Cell Death Dis. 2020 Feb 18;11(2):126
A549 cells
0.05, 0.5, 1, 5, 25, 50 µg/ml
24, 48, 72 h
Evaluate the effect of Bruceine D on the proliferation of A549 cells, results showed that Bruceine D significantly inhibited the proliferation of A549 cells, with an IC50 value of 1.01±0.11 µg/ml
Int J Mol Med. 2019 Dec;44(6):2015-2026
MCF-10A
3.13–25 μM
48 h
BD inhibited MCF-10A cell viability with an IC50 of 12.200 μM.
J Adv Res. 2024 Apr;58:193-210
PANC-1
0.5-1.5 μM
24-48 h
To evaluate the inhibitory effect of BD on PDAC cell proliferation and its enhancement of GEM chemosensitivity. Results showed that BD significantly inhibited PDAC cell proliferation and enhanced GEM chemosensitivity by downregulating the Nrf2 pathway.
J Exp Clin Cancer Res. 2022 Mar 10;41(1):90
Capan-2
0.5-1.5 μM
24-48 h
To evaluate the inhibitory effect of BD on PDAC cell proliferation and its enhancement of GEM chemosensitivity. Results showed that BD significantly inhibited PDAC cell proliferation and enhanced GEM chemosensitivity by downregulating the Nrf2 pathway.
J Exp Clin Cancer Res. 2022 Mar 10;41(1):90
Miapaca-2
0.5-1.5 μM
24-48 h
To evaluate the inhibitory effect of BD on PDAC cell proliferation and its enhancement of GEM chemosensitivity. Results showed that BD significantly inhibited PDAC cell proliferation and enhanced GEM chemosensitivity by downregulating the Nrf2 pathway.
J Exp Clin Cancer Res. 2022 Mar 10;41(1):90
BT474
3.13–25 μM
48 h
BD inhibited BT474 cell viability with an IC50 of 12.100 μM.
J Adv Res. 2024 Apr;58:193-210
Huh7 cells
1.89 μM (IC50)
48 h
To evaluate the inhibitory effect of BD on Huh7 cell proliferation under hypoxic conditions. Results showed that BD dose-dependently inhibited Huh7 cell viability.
Acta Pharm Sin B. 2021 Nov;11(11):3481-3492
HepG2 cells
8.34 μM (IC50)
48 h
To evaluate the inhibitory effect of BD on HepG2 cell proliferation under hypoxic conditions. Results showed that BD dose-dependently inhibited HepG2 cell viability.
Acta Pharm Sin B. 2021 Nov;11(11):3481-3492
Bruceine D/鸦胆子苦素D 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c-nu mice
Lung cancer xenograft model
Intraperitoneal injection
40 mg/kg
Every 2 days for 15 days
BD significantly reduced the growth of xenograft tumors without significant changes in body weight. An increase in the number of TUNEL-positive cells and upregulation of LC3-II, cleaved caspase-9, p-ERK and p-JNK were observed following BD treatment. H&E staining results suggested that BD exhibited no significant toxicity in vivo.
Cell Death Dis. 2020 Feb 18;11(2):126
BALB/c nude mice
Xenograft model of gastric cancer cells SGC7901 and MKN45
Intraperitoneal injection
1.5 mg/kg
Every two days for 14 days
BD significantly inhibited tumor growth and reduced tumor weight in gastric cancer cells.
Front Pharmacol. 2020 Nov 24;11:584960
BALB/c nude mice
Orthotopic xenograft and genetically engineered KPC mouse models of PDAC
Oral gavage
2 mg/kg
Once daily for 4 weeks
To evaluate the inhibitory effect of BD alone or in combination with GEM on PDAC tumor growth. Results showed that BD significantly inhibited tumor growth and enhanced GEM chemosensitivity by inhibiting the Nrf2 pathway.
J Exp Clin Cancer Res. 2022 Mar 10;41(1):90
NCG mice
MDA-MB-231 xenograft model
Intraperitoneal injection
2.5 mg/kg
Daily for 21 days
BD significantly inhibited tumor growth in the Trop2-OE group with an inhibition rate of 70.81%.
J Adv Res. 2024 Apr;58:193-210
BALB/c nude mice
Huh7 xenograft model
Tail vein injection
0.75 and 1.5 mg/kg
Once daily for 14 days
To evaluate the anti-tumor activity of BD in the Huh7 xenograft model. Results showed that BD at 1.5 mg/kg/day significantly inhibited tumor growth without significant body weight loss or side effects.
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