Platycodin D (PLD) is a natural product isolated and purified from the root of Platycodon grandiflorum., which may stimulate TNF-α synthesis or inhibit degradation of TNF-α mRNA, and is an Hsp90 inhibitor which disrupting the co-chaperone interaction of Hsp90/cell division cycle protein 37 (Cdc37) and subsequently degrading multiple Hsp90 client proteins without the feedback increase of Hsp70[3]. Platycodin D repressed the osteoclast activity and enhanced bone mineral density in the mouse model. In C3H10T1/2 cells, platycodin D upregulated osteogenic markers including alkaline phosphatase (ALP), bone sialoprotein, and collagen type 1 alpha 1, and transcription factors, such as Runx2 and osterix, subsequently enhancing the bone mineralization. Furthermore, platycodin D upregulated the ALP activity and enhanced the mineralization process in osteoblast cells via the sirtuin 1/β-catenin pathways[4]. Platycodin D reduces the protein level of PD-L1 in lung cancer cells via triggering its release into the cell culture medium[5]. PLD protected BV-2 cells from MPP+(1-methyl-4-phenylpyridinium) -induced inflammatory response via regulating the TLR4-MyD88-NF-κB signaling pathway[6]. PLD executes its protective effects on OGD/R(oxygen-glucose deprivation/reperfusion)-induced cell injury via regulating the PI3K/Akt/mTOR pathway in cortical neurons[7].
Platycodin D/桔梗皂苷D 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Calu-3 cells
4.76 μM
24 hours
To evaluate the inhibitory effect of PD on the infection of authentic SARS-CoV-2 virus in Calu-3 cells, results showed that PD effectively inhibited viral infection
Exp Mol Med. 2021 May;53(5):956-972.
Vero cells
1.19 μM
24 hours
To evaluate the inhibitory effect of PD on the infection of authentic SARS-CoV-2 virus in Vero cells, results showed that PD effectively inhibited viral infection
Exp Mol Med. 2021 May;53(5):956-972.
HEK293T cells
0.72 μM
1 hour
To evaluate the inhibitory effect of PD on the entry of SARS-CoV-2 pseudovirus into HEK293T cells, results showed that PD effectively inhibited viral entry
Exp Mol Med. 2021 May;53(5):956-972.
H1299 cells
0.69 μM
1 hour
To evaluate the inhibitory effect of PD on the entry of SARS-CoV-2 pseudovirus into H1299 cells, results showed that PD effectively inhibited viral entry
Exp Mol Med. 2021 May;53(5):956-972.
Human platelets
0, 1, 10, 20 μM
30 min
To evaluate the effect of PD on platelet apoptosis, results showed that PD did not induce platelet apoptosis.
J Transl Med. 2018 Nov 15;16(1):311.
Human platelets
0, 1, 10, 20 μM
15 min
To evaluate the effect of PD on phosphorylation of Syk and PLCγ2, results showed that PD significantly reduced phosphorylation levels of Syk and PLCγ2.
J Transl Med. 2018 Nov 15;16(1):311.
Human platelets
0, 1, 10, 20 μM
90 min
To evaluate the effect of PD on platelet spreading on fibrinogen, results showed that PD dose-dependently inhibited platelet spreading.
J Transl Med. 2018 Nov 15;16(1):311.
PC-9
10 μmol/L
24 hours
PD treatment led to an increase in cytoplasmic vacuoles, suggesting the induction of autophagy.
Int J Nanomedicine. 2025 Feb 6;20:1661-1678.
A549
10 μmol/L
24 hours
PD treatment led to an increase in cytoplasmic vacuoles, suggesting the induction of autophagy.
Int J Nanomedicine. 2025 Feb 6;20:1661-1678.
Peripheral blood mononuclear cells (PBMCs)
0.25 mM
72 hours
To assess the effect of G1-S4 and G2-S16 dendrimers in combination with Platycodin D on PBMC proliferation. Results indicated that the combinations did not significantly affect PBMC proliferation.
Int J Nanomedicine. 2019 Apr 2;14:2371-2381.
TZM-bl cells
0.25 mM
48 hours
To evaluate the cytotoxicity of G1-S4 and G2-S16 dendrimers in combination with Platycodin D. Results showed that G1-S4 and G2-S16 were nontoxic at 10 µM in TZM-bl cells.
Int J Nanomedicine. 2019 Apr 2;14:2371-2381.
A549 lung epithelial cells
5, 10, 20 µM
1-hour pretreatment followed by 24-hour LPS stimulation
To investigate the inhibitory effect of PLD on LPS-induced inflammatory response. Results showed PLD significantly suppressed LPS-induced IL-6 and IL-8 production and inhibited NF-κB and IRF3 activation.
Front Immunol. 2017 Jan 3;7:644.
Primary rat microglia cells
5, 10, 20 µM
12 hours
Inhibited LPS-induced production of ROS, TNF-α, IL-6, and IL-1β, and suppressed NF-κB activation
Front Immunol. 2018 Jan 9;8:1929.
MDA-MB-231 cells
1.25 μM, 2.5 μM, 5 μM, 10 μM, 20 μM
48 hours
To evaluate the anti-proliferative effects of Platycodin D on MDA-MB-231 cells, results showed PD enhanced the anti-proliferative effects of DOX
Chin Med. 2014 Jun 9;9:16.
MCF-7 cells
1.25 μM, 2.5 μM, 5 μM, 10 μM, 20 μM
48 hours
To evaluate the anti-proliferative effects of Platycodin D on MCF-7 cells, results showed PD enhanced the anti-proliferative effects of DOX
Chin Med. 2014 Jun 9;9:16.
Human hepatocellular carcinoma BEL-7402 cells
5–40 μmol/L
24, 48, 72 hours
To evaluate the antiproliferative effect of Platycodin D on BEL-7402 cells, results showed that Platycodin D inhibited cell proliferation in a concentration- and time-dependent manner with IC50 values of 37.70±3.99, 24.30±2.30, and 19.70±2.36 μmol/L at 24, 48, and 72 h, respectively.
Acta Pharmacol Sin. 2015 Dec;36(12):1503-13.
Platycodin D/桔梗皂苷D 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
Thrombocytopenic mouse model
Ex vivo treatment followed by infusion
20 μM
Single treatment
To evaluate the effect of PD on in vivo hemostasis and arterial thrombosis, results showed that PD significantly prolonged tail bleeding time and delayed arterial thrombus formation.
J Transl Med. 2018 Nov 15;16(1):311.
BALB/c nude mice
Lung cancer metastasis model
Intraperitoneal injection
7.5 mg/kg or 15 mg/kg
3 times per week for 3 weeks
PD significantly inhibited tumor growth and migration, and its therapeutic efficacy and safety in vivo were markedly enhanced through a homologous cell delivery system.
Int J Nanomedicine. 2025 Feb 6;20:1661-1678.
BALB/c mice
Vaginal irritation model
Vaginal administration
250 µM
Once daily for 7 consecutive days
To assess the toxicity of G1-S4/PD and G2-S16/PD combinations on vaginal tissue. Results showed no significant changes or damage to the vaginal epithelium after 7 consecutive days of application.
Int J Nanomedicine. 2019 Apr 2;14:2371-2381.
Mice
Non-small cell lung cancer model
7.5 mg/kg
Not used
PD significantly inhibited the formation of microvessels and VM, and reduced the expression levels of VEGFA/VEGFR
J Pharm Anal. 2024 Jan;14(1):152-155
BALB/c mice
LPS-induced acute lung injury model
Intraperitoneal injection
20, 40, 80 mg/kg
Administered 1 hour before LPS challenge, evaluated 7 hours post-LPS
To evaluate the protective effects of PLD against LPS-induced acute lung injury. Results demonstrated PLD significantly alleviated lung histopathological changes, myeloperoxidase activity, and pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) levels.
Front Immunol. 2017 Jan 3;7:644.
BALB/cA nude mice
BEL-7402 xenograft tumor model
Intraperitoneal injection
5 and 10 mg/kg/d
Once daily for 21 days
To evaluate the antitumor effect of Platycodin D on BEL-7402 xenograft tumor growth, results showed that 10 mg/kg Platycodin D significantly reduced relative tumor volume with decreased body weight.
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