Home Transmembrane Transporters P-gp inhibitor (20S)-Protopanaxadiol For research use only.

(20S)-Protopanaxadiol

Synonyms: 20-Epiprotopanaxadiol

20(S)-Protopanaxadiol (PPD, 20-Epiprotopanaxadiol), the main intestinal metabolite of ginsenosides, is one of the active ingredients in ginseng. 20(S)-Protopanaxadiol inhibits P-glycoprotein in multidrug resistant cancer cells.

(20S)-Protopanaxadiol Chemical Structure

(20S)-Protopanaxadiol Chemical Structure

CAS No. 30636-90-9

Purity & Quality Control

(20S)-Protopanaxadiol Related Products

Signaling Pathway

P-gp Signaling Pathways

P-gp Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SF188 cells Cytotoxicity assay 24 h Cytotoxicity against human SF188 cells after 24 hrs 17261067
U87MG cells Cytotoxicity assay 24 h Cytotoxicity against human U87MG cells after 24 hrs 17261067
U87MG cells Function assay 2 h Increase in superoxide anion level in human U87MG cells after 2 hrs 17261067
U87MG cells Function assay 43.4 μM 4 h Induction of autophagy in human U87MG cells by MDC staining at 43.4 uM after 4 hrs 17261067
U87 cell Cytotoxicity assay 72 h Cytotoxicity against human U87 cells after 72 hrs by MTT assay 22342101
Hep3B cells Cytotoxicity assay 72 h Cytotoxicity against human Hep3B cells after 72 hrs by MTT assay 22342101
MDA-MB-231 cells Function assay 2.5-5.8 μM 24 h Induction of apoptosis in human MDA-MB-231 cells assessed as increase in expression of cleaved PARP at 2.5 to 5.8 uM after 24 hrs by SDS-polyactylamide gel electrophoresis 25453798
LLC-PK1 Cytotoxicity assay 4 h Cytotoxicity against pig LLC-PK1 cells after 4 hrs by MTT assay 25453798
MDA-MB-231 cells Proliferation assay 4 h Antiproliferative activity against human MDA-MB-231 cells after 4 hrs by MTT assay 25453798
COLO205 cells Cytotoxicity assay 72 h Cytotoxicity against human COLO205 cells after 72 hrs by MTT assay 21216145
HL60 cells Cytotoxicity assay 72 h Cytotoxicity against human HL60 cells after 72 hrs by MTT assay 21216145
HepG2 cells Cytotoxicity assay 72 h Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay 21216145
MCF7 cells Cytotoxicity assay 72 h Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay 21216145
SF188 cells Function assay 108.4 μM 4 h Induction of autophagy in human SF188 cells by MDC staining at 108.4 uM after 4 hrs 17261067
SF188 cells Function assay 108.4 μM Activation of caspase 3 in human SF188 cells at 108.4 uM 17261067
SF188 cells Function assay 2 h Increase in superoxide anion level in human SF188 cells after 2 hrs 17261067
SF188 cells Function assay 108.4 μM Activation of caspase 7 in human SF188 cells at 108.4 uM 17261067
SF188 cells Function assay 43.4 μM 4 h Induction of autophagy in human SF188 cells by MDC staining at 43.4 uM after 4 hrs 17261067
HepG2 cells Cytotoxicity assay 48 h Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay 26420067
HL60 cells Cytotoxicity assay 48 h Cytotoxicity against human HL60 cells after 48 hrs by MTT assay 26420067
Click to View More Cell Line Experimental Data

Biological Activity

Description 20(S)-Protopanaxadiol (PPD, 20-Epiprotopanaxadiol), the main intestinal metabolite of ginsenosides, is one of the active ingredients in ginseng. 20(S)-Protopanaxadiol inhibits P-glycoprotein in multidrug resistant cancer cells.
In vitro
In vitro

Concentrations causing growth inhibition of 50% of cells (LC50) for the compounds PPD is 23 μg/ml, for Int-407 cells. The the LC50 for PPD is determined to be 24 μg/ml in Caco-2 cells. In the Int-407 cell line, PPD produces great percentage of sub-G1 (apoptotic) cells(The Int-407 cell line is a human embryonic nonmalignant cell line originating from fetal tissue of approximately 2 months gestation, whereas Caco-2 is a human colon adenocarcinoma cell line). This response is attributed to differences in individual ginsenoside glycosylation and, thus, the hydrophobic-hydrophilic balance [2]. Incubation with PPD also significantly reduces the viability of U251-MG and U87-MG cells in a dose- and time-dependent manner. The cytotoxic effect of PPD is accompanied by reduced expression of cell adhesion proteins, including N-cadherin and integrin β1, which leads to reduced phosphorylation of focal adhesion kinase. Furthermore, incubation with PPD reduces the expression of cyclin D1 and subsequently induces cell-cycle arrest at the G1 phase[3].
Cell Research Cell lines Int-407 and Caco-2 cell lines
Concentrations 23 μg/ml(Int-407 cells); 24 µg/mL(Caco-2 cells)
Incubation Time 24, 48, 72 h
Method

Int-407 and Caco-2 cells are seeded at a concentration of 1×106 cells/mL in 24-well plates in separate experiments. Test ginsenosides (PPD, PPT, Rh2) are added to wells to the LC50 concentration determined previously from the MTT assays. The ginsenoside concentrations used for Int-407 cells are 23, 26, and 53 µg/mL, respectively, for PPD, PPT, and Rh2. In a similar experiment using Caco-2 cells, 24 µg/mL for both PPD and PPT and 55 µg/mL for Rh2 is used. Untreated cells represented the control. Cells are incubated at 37℃ in a 5% CO2 humidified incubator for 24, 48, and 72 h. Cell-free supernatant are obtained by centrifugation(400g) for 10 min, and the lactate dehydrogenase (LDH) assay is conducted as previously reported.
In Vivo
In vivo

Treatment with PPD(20(S)-Protopanaxadiol) and PPT(20(S)-Protopanaxatriol) prior to immobilization stress increase the time spent in open arms and open arm entries in the elevated plus-maze (EPM) test. Treatment with PPD potently suppresses immobilization stress-induced serum levels of corticosterone and interleukin (IL)-6 by the enzyme-linked immunosorbent assay. PPD and PPT may exhibit the anxiolytic effect via γ-aminobutyrateA (GABAA) receptor(s) and serotonergic receptor(s), respectively, and PPD may have an anti-inflammatory effect that is more potent than that of PPT[1].
Animal Research Animal Models Male ICR mice
Dosages 5 or 10 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 460.73 Formula

C30H52O3
CAS No. 30636-90-9 SDF Download (20S)-Protopanaxadiol SDF
Smiles CC(=CCCC(C)(C1CCC2(C1C(CC3C2(CCC4C3(CCC(C4(C)C)O)C)C)O)C)O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 92 mg/mL ( (199.68 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 33 mg/mL

Water : Insoluble


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