Dehydrocostus Lactone is a major sesquiterpene lactone isolated from the roots of Saussurea lappa. Dehydrocostus Lactone a naturally occuring sesquiterpene lactone in the roots of Saussurea lappa with anti-inflammatory activity[3]. Dehydrocostus lactone) isolated from the medicinal plant, Saussurea lappa, inhibited the production of NO in lipopolysaccharide (LPS)-activated RAW 264.7 cells by suppressing inducible nitric oxide synthase enzyme expression. This compound also decreased the TNF-alpha level in LPS-activated systems in vitro and in vivo[4]. DHCL (Dehydrocostus Lactone) promoted apoptosis with increased activation of caspases 8, 9, 7, 3, enhanced PARP cleavage, decreased Bcl-xL expression and increased levels of Bax, Bak, Bok, Bik, Bmf, and t-Bid[5]. DHL (Dehydrocostus Lactone) inhibited LPS-induced production of proinflammatory mediators such as iNOS, NO, and cytokines including TNF-α, IL-6, IL-1β, and IL-12 p35 by suppressing the activity of NF-κB via p38 MAPK/MK2 and Akt signaling pathway in macrophages. DHL significantly attenuated LPS-induced pathological injury and reduced cytokines expression in the lung in vivo[6]. Dehydrocostus lactone can suppress the proliferation of K562 cells and induce the apoptosis of K562 cells through BCR/ABL-STAT signaling pathways[7]. DHC protected against ovariectomy (OVX)-induced bone loss in mice and the protective effect was mediated at least in part through the attenuation of NF-κB signaling pathway[8].
Dehydrocostus Lactone/去氢木香内酯 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Bone-marrow-derived macrophages (BMDMs)
0, 0.3, 1, 3, 10 µM
0.5 hours pretreatment followed by 0.5 hours LTA stimulation
To evaluate the effect of DHL on LTA-induced phosphorylation of p38 MAPK and NF-κB, results showed that DHL inhibited LTA-induced phosphorylation of p38 MAPK and NF-κB in a dose-dependent manner.
Int J Mol Sci. 2021 Sep 9;22(18):9754.
RAW264.7 cells
0, 0.3, 1, 3, 10 µM
0.5 hours pretreatment followed by 0.5 hours LTA stimulation
To evaluate the effect of DHL on LTA-induced phosphorylation of p38 MAPK and NF-κB, results showed that DHL inhibited LTA-induced phosphorylation of p38 MAPK and NF-κB in a dose-dependent manner.
Int J Mol Sci. 2021 Sep 9;22(18):9754.
RAW264.7 macrophages
1, 3, 9 µM
2 hours pretreatment followed by LPS/IFNγ stimulation for 5 min to 24 hours
To evaluate the anti-inflammatory effects of DCL. Results showed DCL significantly inhibited LPS/IFNγ-induced NO and PGE2 production, downregulated iNOS and COX-2 expression, and suppressed NF-κB signaling (reduced phosphorylation of IKKα/β and IκBα, prevented NF-κB p65 nuclear translocation). Additionally, DCL directly bound to IKKα/β and Keap1, inhibiting NF-κB while activating the Nrf2 pathway.
Front Pharmacol. 2022 Mar 7;13:817596.
AGS cells
0, 5, 10, 15, 20, 25 µM
24 and 48 hours
To evaluate the antiproliferative activity of Dehy, results showed that Dehy inhibited human GC cell proliferation in a dose- and time-dependent manner.
J Adv Res. 2025 Jan;67:331-348.
MKN-28 cells
0, 5, 10, 15, 20, 25 µM
24 and 48 hours
To evaluate the antiproliferative activity of Dehy, results showed that Dehy inhibited human GC cell proliferation in a dose- and time-dependent manner.
J Adv Res. 2025 Jan;67:331-348.
Primary mouse peritoneal macrophages (PMs)
1, 3, 9 µM
24 hours
To validate anti-inflammatory effects in primary immune cells. DCL dose-dependently inhibited LPS/IFNγ-induced NO production.
Front Pharmacol. 2022 Mar 7;13:817596.
Bone-marrow-derived macrophages (BMDMs)
0, 0.3, 1, 3, 10 µM
24 hours
To evaluate the effect of DHL on the viability of BMDMs, results showed that DHL did not cause cytotoxicity at concentrations up to 10 μM.
Int J Mol Sci. 2021 Sep 9;22(18):9754.
RAW264.7 cells
0, 0.3, 1, 3, 10 µM
24 hours
To evaluate the effect of DHL on the viability of RAW264.7 cells, results showed that DHL did not cause cytotoxicity at concentrations up to 10 μM.
Int J Mol Sci. 2021 Sep 9;22(18):9754.
Rat nucleus pulposus cells
2.5 µM
24 hours
To evaluate the effects of dehydrocostus lactone on cytotoxicity and proliferation of nucleus pulposus cells. Results showed that 2.5 μM DHE slightly promoted cell proliferation, while concentrations ≥20 μM exhibited cytotoxicity.
Front Pharmacol. 2021 Apr 14;12:641098.
Huh7
8.311 µM (IC50)
24 hours
Evaluation of cytotoxic potential of dehydrocostus lactone on Huh7 cells with IC50 value of 8.311 µM
Molecules. 2022 Aug 11;27(16):5104.
Hep3B
4.97 µM (IC50)
24 hours
Evaluation of cytotoxic potential of dehydrocostus lactone on Hep3B cells with IC50 value of 4.97 µM
Molecules. 2022 Aug 11;27(16):5104.
HepG2
7.8 µM (IC50)
24 hours
Evaluation of cytotoxic potential of dehydrocostus lactone on HepG2 cells with IC50 value of 7.8 µM
Molecules. 2022 Aug 11;27(16):5104.
SW1353 human chondrocytes
10 and 20 µM
24 hours
DHC inhibited TNF-α-induced oxidative stress by suppressing the production of reactive oxygen species (ROS); decreased the expression of pro-inflammatory cytokines IL-1β and IL-6 induced by TNF-α; prevented the degradation of type II collagen and aggrecan by inhibiting the overexpression of MMP-1, MMP-3, MMP-13, ADAMTS-4, and ADAMTS-5; ameliorated the inflammatory response and degeneration of the articular extracellular matrix (ECM) by suppressing nuclear factor-κB (NF-κB) activation.
To evaluate the effects of dehydrocostus lactone on TNF-α-induced senescence of nucleus pulposus cells. Results showed that DHE treatment reversed TNF-α-induced senescence.
Front Pharmacol. 2021 Apr 14;12:641098.
RAW264.7 cells
0, 3, 5, 10, 30 µM
30 min pretreatment, 24 hours LPS stimulation
Inhibited LPS-induced NO and iNOS production, reduced pro-inflammatory cytokines TNF-α, IL-1β, IL-6, and IL-12 expression
Molecules. 2019 Apr 17;24(8):1510.
Primary lung macrophages
0, 3, 5, 10, 30 µM
30 min pretreatment, 8 or 16 hours LPS stimulation
Inhibited LPS-induced NO and iNOS production, reduced pro-inflammatory cytokines TNF-α, IL-1β, IL-6, and IL-12 expression
Molecules. 2019 Apr 17;24(8):1510.
RAW264.7 cells
4 µM
4 hours pretreatment followed by RANKL stimulation for 0-60 minutes
To investigate the effect of DHE on RANKL-induced signaling pathways. Results showed that DHE suppressed RANKL-induced activation of NF-κB signaling pathway but had little effect on the phosphorylation of MAPK pathway.
J Cell Mol Med. 2019 Aug;23(8):5762-5770.
Bone marrow-derived macrophages (BMMs)
0, 0.5, 1, 2, 4 µM
5 days
To evaluate the effect of DHE on the differentiation of BMMs into osteoclasts. Results showed that DHE inhibited the formation of TRAP-positive multinucleated osteoclasts in a dose-dependent manner, with almost complete inhibition at 4 μmol/L concentration without affecting cell viability.
J Cell Mol Med. 2019 Aug;23(8):5762-5770.
HBE cells
0, 2, 4, 6, 8 and 10 μg/mL
6, 12, 24 hours
DHL showed low toxicity to HBE cells with IC50 > 25 μg/mL.
J Cell Mol Med. 2020 Jun;24(11):6028-6042.
TU212 cells
0, 2, 4, 6, 8 and 10 μg/mL
6, 12, 24 hours
DHL inhibited the proliferation of TU212 cells in a dose- and time-dependent manner and induced apoptosis.
J Cell Mol Med. 2020 Jun;24(11):6028-6042.
Hep-2 cells
0, 2, 4, 6, 8 and 10 μg/mL
6, 12, 24 hours
DHL inhibited the proliferation of Hep-2 cells in a dose- and time-dependent manner and induced apoptosis.
J Cell Mol Med. 2020 Jun;24(11):6028-6042.
Dehydrocostus Lactone/去氢木香内酯 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Wistar rats
Benign prostatic hyperplasia model
Oral
0.075 mg/kg
Daily administration for 8 weeks
Dehydrocostus lactone significantly reduced prostate weight, prostate index, and prostate volume, and decreased epithelial cell thickness. Additionally, the BCL-2 mRNA expression level in the DCL group was significantly lower than that in the disease-induced group.
World J Mens Health. 2021 Apr;39(2):315-323
BALB/c nude mice
Hep-2 nude mouse xenograft model
Intraperitoneal injection
10 and 15 mg/kg
Every 2 days for 3 weeks
DHL inhibited the growth of Hep-2 xenograft tumours and induced apoptosis in tumour cells without significant toxicity to the organs of nude mice.
J Cell Mol Med. 2020 Jun;24(11):6028-6042.
BALB/c nude mice
MKN-28 cell xenograft model
Intraperitoneal injection
15 and 30 mg/kg/day
Once daily for two weeks
To evaluate the anti-GC effect of Dehy in vivo, results showed that high-dose Dehy significantly inhibited the growth of MKN-28 xenografts.
J Adv Res. 2025 Jan;67:331-348.
C57BL/6 mice
MRSA-induced acute lung injury model
Intraperitoneal injection
2.5 and 5 mg/kg
Single dose, lasted for 24 hours
To evaluate the effect of DHL on MRSA-induced acute lung injury, results showed that DHL significantly alleviated MRSA-induced lung injury, reducing inflammatory cell infiltration and alveolar structure destruction.
Int J Mol Sci. 2021 Sep 9;22(18):9754.
C57BL/6 mice
Spinal instability model
Intraperitoneal injection
20 mg/kg
Once daily for 8 weeks
To evaluate the effects of dehydrocostus lactone on intervertebral disc degeneration. Results showed that DHE treatment partially ameliorated the loss of disc height and structural destruction.
Front Pharmacol. 2021 Apr 14;12:641098.
Rats
Oral administration model
Oral
300 mg/kg
Single dose, 24-hour sample collection
Study the metabolic network of Dehydrocostus Lactone in rats
Molecules. 2022 Nov 9;27(22):7688
ICR mice
DSS-induced colitis model
Intragastric administration
5, 10, 15 mg/kg
Once daily for 8 days
To assess the therapeutic effects of DCL on DSS-induced colitis. Results demonstrated DCL significantly alleviated weight loss, colon shortening, increased spleen index, and colonic tissue damage (reduced CD68+ macrophage infiltration and MPO+ neutrophil accumulation), while restoring intestinal barrier function (upregulated ZO-1 and Occludin expression).
Front Pharmacol. 2022 Mar 7;13:817596.
C57BL/6 mice
LPS-induced acute lung injury model
Intraperitoneal injection
5, 10, 20 mg/kg
Single administration, evaluated after 24 h
Attenuated LPS-induced lung pathological injury, reduced inflammatory cell infiltration and pro-inflammatory cytokine expression, inhibited phosphorylation of p38 MAPK/MK2, Akt, and NF-κB
Molecules. 2019 Apr 17;24(8):1510.
Nude mice
EJ xenograft model
Oral gavage
50 mg/kg
Every other day for 20 days
To evaluate antitumor activity, results showed 81% tumor growth inhibition
Sci Rep. 2018 Jun 11;8(1):8807
C57BL/6 mice
DSS-induced ulcerative colitis model
Oral administration
6, 12, 24 mg/kg/day
Once daily for 10 days
Dehydrocostus lactone alleviated DSS-induced weight loss, colon shortening, and pathological changes in mice by downregulating the expression of TLR4, PIK3R1, and RELA, thereby mitigating ulcerative colitis.
Sci Rep. 2024 Nov 30;14(1):29777
C57BL/6 mice
LPS-induced bone loss model and titanium particle-induced calvarial osteolysis model
Intraperitoneal injection
7.5 μg/g and 15 μg/g
Started 1 day before LPS injection, administered every other day for up to 8 days
To evaluate the protective effect of DHE on LPS-induced bone loss and titanium particle-induced calvarial osteolysis. Results showed that DHE partially restored LPS-induced bone loss and titanium particle-induced calvarial osteolysis in a dose-dependent manner.
J Cell Mol Med. 2019 Aug;23(8):5762-5770.
BALB/c nude mice
DSS-induced colitis model
Tail vein injection
8 mg/mL, 100 μL
Single injection, observed for 72 hours
Evaluated the biodistribution of dehydrocostus lactone, showing higher accumulation in the lung and gastrointestinal tract
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