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Chemical Structure| 568-73-0 Chemical Structure| 568-73-0

Structure of Tanshinone I
CAS No.: 568-73-0

Chemical Structure| 568-73-0

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Tanshinone I, an active principle isolated from the roots of Salvia miltiorrhiza (Danshen), is an inhibitor of type IIA human recombinant sPLA2 and rabbit recombinant cPLA2 with IC50s of 11 μM and 82 μM, respectively, is structurally similar to tanshinone IIA and may possess similar cytotoxic effects on tumor cells. Tanshinone I showed inhibitory effect on PL(pro) with IC50 value of 8.8μM and less inhibitory effect on 3CLpro with IC50 value of 38.7μM.

Synonyms: Tanshinone A

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Product Citations

Product Citations

Krueger, Nadine ; Kronenberger, Thales ; Xie, Hang ; Rocha, Cheila ; Poehlmann, Stefan ; Su, Haixia , et al.

Abstract: The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has forced the development of direct-acting antiviral drugs due to the coronavirus disease 2019 (COVID-19) pandemic. The main protease of SARS-CoV-2 is a crucial enzyme that breaks down polyproteins synthesized from the viral RNA, making it a validated target for the development of SARS-CoV-2 therapeutics. New chem. phenotypes are frequently discovered in natural goods. In the current study, we used a fluorogenic assay to test a variety of natural products for their ability to inhibit SARS-CoV-2 Mpro. Several compounds were discovered to inhibit Mpro at low micromolar concentrations It was possible to crystallize robinetin together with SARS-CoV-2 Mpro, and the X-ray structure revealed covalent interaction with the protease's catalytic Cys145 site. Selected potent mols. also exhibited antiviral properties without cytotoxicity. Some of these powerful inhibitors might be utilized as lead compounds for future COVID-19 research.

Keywords: COVID-19 ; antivirals ; coronavirus ; covalent drugs ; dynamic light scattering ; inhibitors ; main protease ; natural products

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Product Details of Tanshinone I

CAS No. :568-73-0
Formula : C18H12O3
M.W : 276.29
SMILES Code : O=C(C1=C2C=CC3=C1C=CC=C3C)C(C4=C2OC=C4C)=O
Synonyms :
Tanshinone A
MDL No. :MFCD00210563
InChI Key :AIGAZQPHXLWMOJ-UHFFFAOYSA-N
Pubchem ID :114917

Safety of Tanshinone I

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HaCaT keratinocytes 5 μM 4 h To examine the effect of Tanshinone I on Nrf2 protein levels, results showed that Tanshinone I significantly upregulated Nrf2 protein levels. PMC3836278
Hs27 human dermal fibroblasts 5 μM 16 h To examine the effect of Tanshinone I on Nrf2 transcriptional activity, results showed that Tanshinone I significantly upregulated Nrf2 transcriptional activity. PMC3836278
Cardiomyocytes 10, 30, 100 μM 48 h Tanshinone IIA pretreatment significantly attenuated ISO-induced cardiomyocyte hypertrophy, as evidenced by reduced cell surface area and decreased mRNA and protein expression levels of ANP, BNP, and β-MHC. PMC3076506

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Memory impairment model Oral 2 or 4 mg/kg Single dose Tanshinone I ameliorates the learning and memory impairments induced by diazepam and MK-801 through activation of ERK signalling. PMC2785534

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02524964 Left Ventricular Remodeling ... More >> Acute Myocardial Infarction Less << Phase 4 Unknown July 2017 China, Guangdong ... More >> Guangdong Provincial Hospital of Chinese Medicine Recruiting Guangzhou, Guangdong, China, 510120 Contact: Minzhou Zhang, Dr.    86-20-81887233 ext 32801    minzhouzhang@yeah.net    Contact: Liheng Guo, Dr.    86-8187236 ext 32907    lihengguo1@yeah.net Less <<
NCT01452477 Polycystic Ovary Syndrome Not Applicable Unknown July 2014 China, Heilongjiang ... More >> Heilongjiang University of Chinese Medicine Recruiting Harbin, Heilongjiang, China, 150040 Contact: Wenjuan Shen, doctor    +86-045182118464    shenwenjuankx@163.com    Contact: Yuehui Zhang, doctor    +86-045182118464    manbingPCOS@163.com    Principal Investigator: Wenjuan Shen, doctor          China, Jiangsu Huaian Maternal and Child Health Hospital Recruiting Huaian, Jiangsu, China, 223001 Contact: Huiying Xue, Scholar    +8613505238015    haxuehuiying@126.com    Principal Investigator: Huiying Xue, bachlor          Lianyungang Maternal and Child Health Hospital Active, not recruiting Lianyungang, Jiangsu, China, 222000 China, Jiangxi JiangXi University of Traditional Chinese Medicine Completed Nanchang, Jiangxi, China, 330000 Less <<
NCT01637675 Pulmonary Hypertension ... More >> Pulmonary Arterial Hypertension Cardiovascular Diseases Lung Diseases Tanshinone IIA Sulfonate Less << Phase 2 Phase 3 Unknown December 2014 China, Guangdong ... More >> The First Affiliated Hospital of Guangzhou Medical University Recruiting Guangzhou, Guangdong, China, 510120 Contact: Jian Wang, MD    +8615013388183    jwang31@jhmi.edu Less <<
NCT02200978 Childhood Acute Promyelocytic ... More >>Leukemia Less << Phase 4 Recruiting September 2022 China, Guangdong ... More >> The First Affiliated Hospital of Sun Yat-Sen University Recruiting Guangzhou, Guangdong, China, 510080 Contact: Xue-Qun Luo, professor       L-xuequn@126.com    Principal Investigator: Xue-Qun Luo, professor Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.62mL

0.72mL

0.36mL

18.10mL

3.62mL

1.81mL

36.19mL

7.24mL

3.62mL

References

 

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