Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM. Loureirin B (1, 0.1, and 0.01 µM) increases insulin secretion in Ins-1 cells. Loureirin B (0.01 µM) almost causes no toxicity on cells. Loureirin B improves the level of expressions of MafA and Pdx-1 and ATP level. Loureirin B inhibits the KATP current but increases the [Ca2+]i level in Ins-1 cells[1]. Loureirin B directly inhibited STIM1/Orai1 channel in a dose-dependent manner. Loureirin B inhibits Ca2+ influx and IL-2 secretion in Jurkat T cells by inhibiting both KV1.3 and STIM1/Orai1 channels[2]. Loureirin B inhibits the expression of Col1 and FN, as well as the TGF-β1-mediated up regulation of p-JNK. Loureirin B also inhibits the up regulation of p-ERK that is induced by TGF-β1. Moreover, Loureirin B inhibits the contraction of TGF-β1-stimulated fibroblasts through the down regulation of p-ERK and p-JNK. However, Loureirin B does not suppress the up regulation of p-p38 that is induced by TGF-β1[3]. LrB (Loureirin B) represses osteoclastogenesis, bone resorption, F-actin belts formation, osteoclast specific gene expressions, ROS activity and calcium oscillations through preventing NFATc1 translocation and expression as well as affecting MAPK-NFAT signaling pathways in vitro. In vivo, LrB prevents OVX-induced osteoporosis and preserves bone volume by repressing osteoclast activity and function[4].
Loureirin B/龙血素B 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HEK293T cells
10 µM
To study the inhibitory effect of LrB on Kv1.3 currents
Front Immunol. 2023 Apr 24;14:1094649
RAW264.7 cells
10 μM
24 hours
Loureirin B inhibits RANKL-induced NFATc1 transcriptional activity.
Theranostics. 2019 Jul 3;9(16):4648-4662
Bone marrow macrophages (BMMs)
1 μM to 10 μM
5 days
Loureirin B inhibits RANKL-induced osteoclast differentiation and F-actin belt formation without cytotoxicity.
Theranostics. 2019 Jul 3;9(16):4648-4662
PBMCs
10 µM
60 minutes
To study the inhibitory effect of LrB on inflammatory cytokine release in PBMCs
Front Immunol. 2023 Apr 24;14:1094649
Jurkat T cells
10 µM
60 minutes
To study the inhibitory effect of LrB on IL-2 release in Jurkat T cells
Front Immunol. 2023 Apr 24;14:1094649
HEK293 T cells
3, 10, 30 μM
To investigate the inhibitory effects of Loureirin B on STIM1/Orai1 currents. Results showed that Loureirin B inhibited STIM1/Orai1 currents in a concentration-dependent manner with an IC50 of 17.11 ± 2.17 μM.
Front Pharmacol. 2021 Jun 25;12:685092
Jurkat T cells
0.01, 0.1, 1 μM
1 hour
To investigate the inhibitory effects of Loureirin B on Ca2+ influx and IL-2 secretion in Jurkat T cells. Results showed that Loureirin B significantly inhibited Ca2+ influx and IL-2 secretion.
Front Pharmacol. 2021 Jun 25;12:685092
rat liver microsome (RLM)
30 μg/mL
45 minutes
To investigate the metabolic features of LB in rat liver microsome, including metabolites identification, elimination kinetics and metabolizing CYP450.
Front Pharmacol. 2018 Oct 12;9:1130
Ins-1 cells
10^-5-10^-9 mol/L
4 hours
To investigate the effect of LB on insulin secretion in Ins-1 cells, the results showed that LB significantly promoted insulin secretion in Ins-1 cells.
J Cell Mol Med. 2021 Jan;25(2):855-866
KKU-M156
21.26 ± 3.17 µg/mL
72 hours
Evaluate the cytotoxicity of Loureirin B against KKU-M156 cells, showing moderate cytotoxicity
BMC Complement Med Ther. 2022 Aug 11;22(1):217
HepG2
20.02 ± 0.46 µg/mL
72 hours
Evaluate the cytotoxicity of Loureirin B against HepG2 cells, showing moderate cytotoxicity
BMC Complement Med Ther. 2022 Aug 11;22(1):217
bone marrow macrophages (BMMs)
10 mM
1 hour
To investigate the inhibitory effect of Loureirin B on the differentiation of BMMs into osteoclasts, it was found that Loureirin B inhibits the differentiation of BMMs by suppressing the phosphorylation of JNK and p38 kinases in the MAPK signaling pathway.
Sci Rep. 2022 Aug 23;12(1):14382
Rat hepatic stellate cells
50 and 100 ng/μl
48 hours
Loureirin B significantly promoted the apoptosis of HSCs in a dose-dependent manner.
Cell Mol Biol Lett. 2018 Aug 2;23:35
Rat hepatic stellate cells
100 ng/μl
24, 48 and 72 hours
Loureirin B significantly inhibited the proliferation of HSCs in a time-dependent manner.
Cell Mol Biol Lett. 2018 Aug 2;23:35
Rat hepatic stellate cells
12.5, 25, 50, 100, 200 or 400 ng/μl
48 hours
Loureirin B significantly inhibited the proliferation of HSCs in a dose-dependent manner.
Cell Mol Biol Lett. 2018 Aug 2;23:35
Primary human dermal fibroblast cells
0-350 µM
24 and 48 hours
Evaluate the cytotoxicity of Loureirin B on primary human dermal fibroblast cells, showing no cytotoxic effects.
Life (Basel). 2025 Mar 3;15(3):396
H1299 cells
0-140 µM
24 hours
Evaluate the effect of Loureirin B on the viability of H1299 cells, showing no toxicity at 0-140 µM.
Life (Basel). 2025 Mar 3;15(3):396
A549 cells
0-140 µM
24 hours
Evaluate the effect of Loureirin B on the viability of A549 cells, showing no toxicity at 0-140 µM.
Life (Basel). 2025 Mar 3;15(3):396
Loureirin B/龙血素B 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J mice
Ovariectomy (OVX)-induced osteoporosis model
Intraperitoneal injection
4 mg/kg
Every 2 days for 6 weeks
Loureirin B prevents OVX-induced osteoporosis and preserves bone volume by repressing osteoclast activity and function.
Theranostics. 2019 Jul 3;9(16):4648-4662
Wistar rats
Collagen-induced arthritis (CIA) model
Intraperitoneal injection
30 mg/kg
Once daily for 15 days
To study the therapeutic effect of LrB on CIA rats
Front Immunol. 2023 Apr 24;14:1094649
Sprague-Dawley rats
TNBS-induced Crohn's disease rat model
Oral gavage
25, 50 and 100 mg/kg
Once daily for 28 days
LB prolonged the survival time of TNBS-induced rats and alleviated colonic damage in a dose dependent manner. Besides, LB remarkably ameliorated TNBS-induced inflammatory response, reversed the established fibrosis, and improved the apoptosis induced by TNBS.
Chin Med. 2020 Jan 6;15:2
SD rats
PCOS-IR rat model
Intraperitoneal injection
10, 20, 40 mg/kg·d
Once daily for 4 weeks
Loureirin B upregulated GPR120, LKB1, and AMPK protein expression, downregulated NLRP3 and Caspase-1 protein expression, reduced insulin resistance and chronic inflammation, and ameliorated histopathological changes in ovarian tissues in PCOS rats, suggesting its potential as a treatment for PCOS.
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