2. MAPK/ERK Pathway Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Apoptosis Cell Cycle/DNA Damage Epigenetics TGF-beta/Smad Stem Cell/Wnt
  3. JNK p38 MAPK MMP NF-κB COX TNF Receptor Interleukin Related Reactive Oxygen Species (ROS) Apoptosis Mitochondrial Metabolism DNA/RNA Synthesis Keap1-Nrf2 Bcl-2 Family Caspase PARP TGF-beta/Smad
  4. Santamarine

Santamarine  (Synonyms: Santamarin; Balchanin)

Cat. No.: HY-N1326 Purity: 98.85%
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Santamarine (Santamarin; Balchanin) is a sesquiterpene lactone found in Artemisia scoparia. Santamarine shows anti-inflammatory, antioxidant, anticancer and anti-photoaging activities. Santamarine suppresses UVA-induced phosphorylation of JNK and p38 MAPK, nuclear translocation of phosphorylated c-Fos and c-Jun, and AP-1-mediated MMP-1 transcription and secretion. Santamarine suppresses NF-κB signaling, iNOS, COX-2, TNF-α, and IL-1β production. Santamarine inhibits thioredoxin reductase activity, induces ROS production, mitochondrial apoptosis, G2/M cell cycle arrest, and DNA damage, and reduces cancer cell growth. Santamarine can be used for the photoaging, inflammatory diseases and cancer.

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Santamarine

Santamarine Chemical Structure

CAS No. : 4290-13-5

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Santamarine Related Antibodies

Top Publications Citing Use of Products

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JNK1 JNK2 JNK3 JNK

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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COX COX-1 COX-2 COX-3

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

Santamarine (Santamarin; Balchanin) is a sesquiterpene lactone found in Artemisia scoparia. Santamarine shows anti-inflammatory, antioxidant, anticancer and anti-photoaging activities. Santamarine suppresses UVA-induced phosphorylation of JNK and p38 MAPK, nuclear translocation of phosphorylated c-Fos and c-Jun, and AP-1-mediated MMP-1 transcription and secretion. Santamarine suppresses NF-κB signaling, iNOS, COX-2, TNF-α, and IL-1β production. Santamarine inhibits thioredoxin reductase activity, induces ROS production, mitochondrial apoptosis, G2/M cell cycle arrest, and DNA damage, and reduces cancer cell growth. Santamarine can be used for the photoaging, inflammatory diseases and cancer[1][2][3][4].

IC50 & Target[1]

MMP-1

 

COX-2

 

IL-1β

 

Bax

 

Bcl-2

 

Caspase 3

 

Caspase 8

 

Caspase 9

 

Cellular Effect
Cell Line Type Value Description References
CCRF-CEM IC50
0.16 μg/mL
Compound: 1; STM
Growth inhibition of human CCRF-CEM cells incubated for 24 to 48 hrs by trypan blue exclusion assay
Growth inhibition of human CCRF-CEM cells incubated for 24 to 48 hrs by trypan blue exclusion assay
[PMID: 33775837]
KB IC50
0.16 μg/mL
Compound: 1; STM
Growth inhibition of human KB cells incubated for 72 hrs by methylene blue staining based assay
Growth inhibition of human KB cells incubated for 72 hrs by methylene blue staining based assay
[PMID: 33775837]
L1210 IC50
0.16 μg/mL
Compound: 1; STM
Growth inhibition of mouse L1210 cells incubated for 24 to 48 hrs by trypan blue exclusion assay
Growth inhibition of mouse L1210 cells incubated for 24 to 48 hrs by trypan blue exclusion assay
[PMID: 33775837]
LS174T IC50
0.16 μg/mL
Compound: 1; STM
Growth inhibition of human LS174T cells incubated for 72 hrs by methylene blue staining based assay
Growth inhibition of human LS174T cells incubated for 72 hrs by methylene blue staining based assay
[PMID: 33775837]
LX-2 IC50
>60 μM
Compound: 1; STM
Inhibition of hyaluronic acid deposition in human LX2 cells incubated for 72 hrs by ELISA
Inhibition of hyaluronic acid deposition in human LX2 cells incubated for 72 hrs by ELISA
[PMID: 33775837]
LX-2 IC50
16.5 μM
Compound: 1; STM
Cytotoxicity against human LX2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human LX2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 33775837]
LX-2 IC50
18.6 μM
Compound: 1; STM
Inhibition of laminin deposition in human LX2 cells incubated for 72 hrs by ELISA
Inhibition of laminin deposition in human LX2 cells incubated for 72 hrs by ELISA
[PMID: 33775837]
LX-2 IC50
7.3 μM
Compound: 1; STM
Inhibition of collagen type 1 deposition in human LX2 cells incubated for 72 hrs by ELISA
Inhibition of collagen type 1 deposition in human LX2 cells incubated for 72 hrs by ELISA
[PMID: 33775837]
MCF7 IC50
0.16 μg/mL
Compound: 1; STM
Growth inhibition of human MCF7 cells incubated for 72 hrs by methylene blue staining based assay
Growth inhibition of human MCF7 cells incubated for 72 hrs by methylene blue staining based assay
[PMID: 33775837]
Platelet IC50
84.93 μM
Compound: Santamarin
Antimigraine activity in bovine citreated platelet assessed as inhibition of [14C]serotonin release after 6 mins by scintillation counting
Antimigraine activity in bovine citreated platelet assessed as inhibition of [14C]serotonin release after 6 mins by scintillation counting
[PMID: 1431933]
Platelet IC50
84.93 μM
Compound: 23
Inhibition of serotonin release in bovine platelets
Inhibition of serotonin release in bovine platelets
[PMID: 18271521]
T-cell IC50
19.6 μM
Compound: 7
Immunosuppressant activity in human T lymphocytes assessed as inhibition of anti-human CD3 and anti-human CD28 monoclonal antibody-induced T lymphocyte proliferation incubated for 72 hrs by FACS analysis
Immunosuppressant activity in human T lymphocytes assessed as inhibition of anti-human CD3 and anti-human CD28 monoclonal antibody-induced T lymphocyte proliferation incubated for 72 hrs by FACS analysis
[PMID: 31181920]
T-cell IC50
5.56 μM
Compound: E1
Immunomodulatory activity in C57BL/6 mouse mesenteric lymph node T cells assessed as inhibition of concanavalin A stimulated T-cell proliferation incubated for 68 hrs by CCK-8 assay
Immunomodulatory activity in C57BL/6 mouse mesenteric lymph node T cells assessed as inhibition of concanavalin A stimulated T-cell proliferation incubated for 68 hrs by CCK-8 assay
[PMID: 37017305]
In Vitro

Santamarine (1-10 μM; 1 h) scavenges intracellular ROS in HDFs with an IC50 of 4.04 μM[1].
Santamarine (1-10 μM; 24 h) dose-dependently reduces UVA-induced MMP-1 secretion in HDFs, with a significant reduction to 33.00 ng/mL at 10 μM[1].
Santamarine (1-10 μM; 24 h) dose-dependently downregulates UVA-induced MMP-1, -3, -9 mRNA and protein expression in HDFs[1].
Santamarine (1-10 μM; 24 h) dose-dependently stimulates type I procollagen mRNA and protein expression in UVA-irradiated HDFs[1].
Santamarine (10 μM; 24 h) suppresses UVA-induced activation of the p38/JNK MAPK pathway and nuclear translocation of AP-1 complex components p-c-Fos and p-c-Jun in HDFs[1].
Santamarine (10 μM; 24 h) activates the TGF-β/Smad pathway in UVA-irradiated HDFs by restoring TGF-β levels, increasing Smad2/3 phosphorylation, reducing Smad7 levels, and elevating nuclear p-Smad2/3 and Smad4 levels[1].
Santamarine (1-10 μM; 24 h) dose-dependently stimulates Nrf2-dependent expression of antioxidant enzymes SOD-1 and HO-1 in UVA-irradiated HDF[1].
Santamarin (5-80 μM; 24 h) does not significantly reduce RAW264.7 cell viability at concentrations up to 40 μM[2].
Santamarin (5-40 μM; 12 h) concentration-dependently reduces iNOS and COX-2 protein expression in LPS (HY-D1056)-stimulated RAW264.7 cells[2].
Santamarin (5-40 μM; 12 h) concentration-dependently reduces nitrite, PGE2, TNF-α, and IL-1β production in LPS-stimulated RAW264.7 cells[2].
Santamarin (5-40 μM; 12 h) concentration-dependently inhibits LPS-induced IκB-α phosphorylation/degradation, p65 nuclear translocation, and NF-κB DNA binding activity in RAW264.7 cells[2].
Santamarin (5-40 μM; 12 h) concentration-dependently increases HO-1 mRNA and protein expression, and HO enzyme activity in RAW264.7 cells[2].
Santamarin (40 μM; 0.5-1.5 h) induces a time-dependent nuclear translocation of Nrf2 in RAW264.7 cells over 0.5 to 1.5 h of incubation[2].
Santamarine (10-100 μM; 24 h) dose-dependently inhibits the growth of A549 and NCI-H1650 lung adenocarcinoma cells (IC50 = 45 μM and 43 μM, respectively) and is far less toxic to NL-20 normal lung cells (IC50 = 85 μM)[3].
Santamarine (40-60 μM; 24 h) induces dose-dependent cell death, apoptosis and associated morphological changes in A549 and NCI-H1650 lung adenocarcinoma cells and these changes are reversed by the ROS scavenger NAC (HY-B0215)[3].
Santamarine (40-60 μM; 1-24 h) induces ROS generation (maximal at 4 h) in A549 lung adenocarcinoma cells, with no detectable change in ROS levels after 24 h treatment[3].
Santamarine (40-60 μM; 24 h) dose-dependently reduces the intracellular GSH/GSSG ratio in A549 lung adenocarcinoma cells and this effect is reversed by the ROS scavenger NAC[3].
Santamarine (40-60 μM; 24 h) dose-dependently inhibits thioredoxin reductase activity in A549 lung adenocarcinoma cells and this effect is reversed by the ROS scavenger NAC[3].
Santamarine (40-60 μM; 24 h) dose-dependently induces oxidative stress-mediated mitochondrial apoptosis in A549 lung adenocarcinoma cells via modulation of Bcl-2 family proteins, dissipation of mitochondrial membrane potential, and activation of caspase-3 and PARP cleavage, with all effects reversed by the ROS scavenger NAC[3].
Santamarine (40-60 μM; 24 h) dose-dependently inhibits constitutive and TNF-α-induced NF-κBp65 nuclear translocation and IκB-α phosphorylation in A549 lung adenocarcinoma cells via an oxidative stress-dependent mechanism[3].
Santamarine (0-25 μg/mL; 24 h) selectively inhibits viability of OC-2 and HSC-3 oral cancer cells, with IC50 values of 15.7 μg/mL and 18.49 μg/mL after 24 h treatment, while having minimal effect on normal S-G cells, and this selective activity is oxidative stress-dependent[4].
Santamarine (15-25 μg/mL; 24 h) induces G2/M cell cycle arrest in OC-2 and HSC-3 oral cancer cells after 24 h treatment at 15 and 25 μg/mL, while causing only minor changes in normal S-G cells[4].
Santamarine (15-25 μg/mL; 12-24 h) dose-dependently and time-dependently induces apoptosis and activates caspase 3, 8, 9 in OC-2 and HSC-3 oral cancer cells, while having minimal effect on normal S-G cells[4].
Santamarine (15-25 μg/mL; 12-24 h) dose-dependently and time-dependently induces ROS, mitochondrial superoxide generation and MMP, GSH depletion in OC-2 and HSC-3 oral cancer cells, while having minimal effect on normal S-G cells[4].
Santamarine (15-25 μg/mL; 12-24 h) dose-dependently and time-dependently induces γH2AX- and 8-OHdG-mediated DNA damage in OC-2 and HSC-3 oral cancer cells, while having minimal effect on normal S-G cells[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Santamarine Related Antibodies

ELISA Assay[1]

Cell Line: UVA-irradiated human dermal fibroblasts (HDFs)
Concentration: 1, 5, 10 μM
Incubation Time: 24 h
Result: Decreased UVA-induced MMP-1 secretion in a dose-dependent manner.
Reduced MMP-1 secretion from 40.74 ng/mL (UVA-only group) to 33.00 ng/mL at 10 μM.

Western Blot Analysis[1]

Cell Line: UVA-irradiated human dermal fibroblasts (HDFs)
Concentration: 1, 5, 10 μM
Incubation Time: 24 h
Result: Markedly suppressed UVA-induced MMP-1, -3, -9 protein expression.

Western Blot Analysis[1]

Cell Line: UVA-irradiated human dermal fibroblasts (HDFs)
Concentration: 10 μM
Incubation Time: 24 h
Result: Suppressed UVA-induced phosphorylation of p38 and JNK.
Upregulated ERK phosphorylation.
Significantly reduced UVA-induced increases in total p-c-Fos and p-c-Jun levels.
Reduced nuclear translocation of p-c-Fos and p-c-Jun.\nReversed UVA-induced suppression of TGF-β protein levels and Smad2/3 phosphorylation.
Reduced UVA-induced upregulation of Smad7 levels.
Reverted UVA-induced decreases in nuclear p-Smad2/3 and Smad4 levels.

Cell Viability Assay[2]

Cell Line: RAW264.7 murine macrophage cells
Concentration: 5, 10, 20, 40, 80 μM
Incubation Time: 24 h
Result: Did not significantly decrease cell viability at concentrations up to 40 μM.
Caused a significant reduction in viability at 80 μM.

Western Blot Analysis[2]

Cell Line: LPS-stimulated RAW264.7 murine macrophage cells
Concentration: 5, 10, 20, 40 μM
Incubation Time: 12 h (pre-incubation); 18 h (LPS stimulation)
Result: Reduced LPS-induced iNOS protein expression in a concentration-dependent manner.
Suppressed LPS-induced COX-2 protein expression in a concentration-dependent manner.

Cell Viability Assay[3]

Cell Line: A549, NCI-H1650, NL-20
Concentration: 10, 20, 40, 80, 100 μM
Incubation Time: 24 h
Result: Inhibited growth of A549 and NCI-H1650 cells in a dose-dependent manner, with IC50 values of 45 μM and 43 μM, respectively.
Exerted a significantly lower growth inhibitory effect on NL-20 cells, with an IC50 value of 85 μM.

Apoptosis Analysis[3]

Cell Line: A549
Concentration: 40, 60 μM
Incubation Time: 24 h
Result: Induced dose-dependent apoptotic cell death in A549 cells.
Reversed this apoptotic effect when cells were pretreated with 3 mM NAC.

Western Blot Analysis[3]

Cell Line: A549
Concentration: 40, 60 μM
Incubation Time: 24 h
Result: Increased Bax, Cl-Casp-3, Cl-PARP levels and reduced Bcl-2 levles.
Dose-dependently inhibited constitutive NF-κBp65 translocation into the nucleus.
Inhibited TNF-α-induced NF-κBp65 translocation into the nucleus.
Dose-dependently inhibited IκB-α phosphorylation without altering IκB-α expression.
Reversed the inhibitory effect on NF-κBp65 translocation when cells were pretreated with 3 mM NAC.

Cell Cycle Analysis[4]

Cell Line: oral squamous cell carcinoma OC-2 cells, oral squamous cell carcinoma HSC-3 cells, normal gingival epithelial S-G cells
Concentration: 15, 25 μg/mL
Incubation Time: 24 h
Result: Decreased G1 and S phase populations and increased G2/M phase populations in OC-2 and HSC-3 cells, inducing G2/M arrest, with a marginal elevation of subG1 phase.
Caused only minor changes in G1, S, and G2/M phase populations of S-G cells.
Suppressed differential cell cycle disturbance was observed with pre-treatment with NAC.

Apoptosis Analysis[4]

Cell Line: oral squamous cell carcinoma OC-2 cells, oral squamous cell carcinoma HSC-3 cells, normal gingival epithelial S-G cells
Concentration: 15, 25 μg/mL
Incubation Time: 12, 24 h
Result: Increased the percentage of Annexin V-positive apoptotic OC-2 and HSC-3 cells in a dose-dependent manner after 24 h treatment.
Increased the percentage of Annexin V-positive apoptotic OC-2 and HSC-3 cells in a time-dependent manner over 0, 12, 24 h at 25 μg/mL.
Caused only weak changes in the percentage of apoptotic S-G cells.
Suppressed differential apoptosis induction was observed with pre-treatment with NAC.
Molecular Weight

248.32

Formula

C15H20O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O[C@@]1([H])[C@@]2([H])CC[C@@]3(C)[C@H](O)CC=C(C)[C@@]31[H])C2=C
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: 98.85%

SDS (251 KB)

COA (259 KB)

Handling Instructions (2659 KB)
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Santamarine Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Santamarine4290-13-5Santamarin BalchaninJNKp38 MAPKMMPNF-κBCOXTNF ReceptorInterleukin RelatedReactive Oxygen Species (ROS)ApoptosisMitochondrial MetabolismDNA/RNA SynthesisKeap1-Nrf2Bcl-2 FamilyCaspasePARPTGF-beta/Smadc-Jun N-terminal kinaseMatrix metalloproteinasesNuclear factor-κBNuclear factor-kappaBCyclooxygenaseTumor Necrosis Factor ReceptorTNFRILpoly ADP ribose polymerase Transforming growth factor betaMycobacterium tuberculosisHSC-3 cellsNrf2SOD-1NCI-H1650 cellsHO-1HDFsRAW264.7 cellsOC-2 cellsA549 cellsInhibitorinhibitorinhibit

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