Tanshinone II-A: new perspectives for old remedies

Xu, Suowen; Liu, Peiqing

doi:10.1517/13543776.2013.743995

Cited by 128 publications

(105 citation statements)

References 23 publications

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“…However, its narrow effectiveconcentration range ( Figure 4D) and its sedative activity 22 as a potential side effect make the compound less attractive for further development. As noted earlier, 10,13,24 tanshinone IIA has been identified as a predominant bioactive constituent of danshen and developed as a prescription drug for cardio-and cerebrovascular disorders. We therefore chose to focus on this specific compound for additional experiments.…”

Section: ■ Results and Discussionmentioning

confidence: 82%

Tanshinone IIA Exhibits Anticonvulsant Activity in Zebrafish and Mouse Seizure Models

Buenafe

Orellana-Paucar

Maes

et al. 2013

ACS Chem. Neurosci.

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Danshen or Chinese red sage (Salvia miltiorrhiza, Bunge) is used by traditional Chinese medicine (TCM) practitioners to treat neurological, cardiovascular, and cerebrovascular disorders and is included in some TCM formulations to control epileptic seizures. In this study, acetonic crude extracts of danshen inhibited pentylenetetrazol (PTZ)-induced seizure activity in zebrafish larvae. Subsequent zebrafish bioassay-guided fractionation of the extract resulted in the isolation of four major tanshinones, which suppressed PTZ-induced activity to varying degrees. One of the active tanshinones, tanshinone IIA, also reduced c-fos expression in the brains of PTZ-exposed zebrafish larvae. In rodent seizure models, tanshinone IIA showed anticonvulsive activity in the mouse 6-Hz psychomotor seizure test in a biphasic manner and modified seizure thresholds in a complex manner for the mouse i.v. PTZ seizure assay. Interestingly, tanshinone IIA is used as a prescription drug in China to address cerebral ischemia in patients. Here, we provide the first in vivo evidence demonstrating that tanshinone IIA has anticonvulsant properties as well. KEYWORDS: Tanshinone IIA, Salvia miltiorrhiza, zebrafish PTZ model, mouse seizure models, pentylenetetrazol E pilepsy affects approximately 60 million people worldwide, of whom 30% suffer from pharmacoresistant seizures. The economics of maintaining a cost-effective therapeutic regimen hinge on its long-term efficacy and the probability of patients developing treatment-resistant seizures or possible side-effects ranging from sedation to Steven−Johnson syndrome.1 To address such issues, there is an ongoing hunt for new antiepileptic drugs (AEDs) with novel mechanisms of action and with minimal or no side-effects.There is a resurgence of interest in exploring plant, microbial, and marine resources used in traditional medicine for potential drug leads. According to the World Health Organization (WHO), 70−80% of the population in developing and developed countries have used, or depend on such therapies, which became the impetus for efforts in bioprospecting and drug development.2 Despite prevalent skepticism, as many as 25% of pharmaceutical drugs on the market are plant-based and were discovered through investigations on traditional or folk medicine practiced by different cultures.1,2 The rationale behind this approach in drug discovery is that small molecules isolated or derived from natural sources offer a more diverse set of structures compared with compounds synthesized through medicinal chemistry or combinatorial techniques. 2Each plant or marine extract can be treated as a library potential of hits, which can be screened using an appropriate medium-to high-throughput in vivo model such as zebrafish (Danio rerio), a freshwater teleost of the Cyprinidae family.3,4 In screening for potential hits and leads for AED development, we have previously described the use of larval zebrafish as a platform for pinpointing AED-like activity of small molecules isolated from plant sources.3,4 ...

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Section: ■ Results and Discussionmentioning

confidence: 82%

Tanshinone IIA Exhibits Anticonvulsant Activity in Zebrafish and Mouse Seizure Models

Buenafe

Orellana-Paucar

Maes

et al. 2013

ACS Chem. Neurosci.

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“…Tan, one of the most bioactive constituents isolated from Salvia miltiorrhiza Bunge, has long been clinically used in Asian countries for the prevention and treatment of CVDs (8)(9)(10). Accumulating evidence suggests that Tan prevents the development of atherosclerosis by inhibiting LDL oxidation ( 28 ), scavenger receptor expression ( 21 ), matrix metalloproteinase expression and activity ( 11 ), pro-infl ammatory cytokine expression ( 29 ), and smooth muscle cell proliferation ( 30 ) and migration ( 31 ).…”

Section: Discussionmentioning

confidence: 99%

“…I), a lipophilic pharmacologically active compound derived from the Chinese herb Salvia miltiorrhiza Bunge (Danshen), exerts multiple cardioprotective effects ( 8 ). Tan has long been used clinically in Asian countries for the prevention and treatment of several CVDs, such as coronary heart disease, angina pectoris, and myocardial infarction (8)(9)(10). We and others have demonstrated that Tan attenuates the initiation and progression of atherosclerosis in experimental animals ( 11,12 ).…”

Section: Oil Red O Stainingmentioning

confidence: 99%

Tanshinone IIA suppresses cholesterol accumulation in human macrophages: role of heme oxygenase-1

Liu

Wang

Huang

et al. 2014

Journal of Lipid Research

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“…Tanshinone IIA (Figure 1) is the most abundant active compound isolated from Danshen (Salvia miltiorrhiza), a traditional Chinese medicine, which has been used in preventing and treating cardiovascular diseases for more than 2000 years in China and other Asian countries (Gao et al, 2012;Xu et al, 2013). Moreover, new pharmacological roles of this compound have recently been reported.…”

Section: Introductionmentioning

confidence: 99%

A Potential Target of Tanshinone IIA for Acute Promyelocytic Leukemia Revealed by Inverse Docking and Drug Repurposing

Chen

2014

Asian Pacific Journal of Cancer Prevention

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Tanshinone IIA is a pharmacologically active ingredient extracted from Danshen, a Chinese traditional medicine. Its molecular mechanisms are still unclear. The present study utilized computational approaches to uncover the potential targets of this compound. In this research, PharmMapper server was used as the inverse docking tool andnd the results were verified by Autodock vina in PyRx 0.8, and by DRAR-CPI, a server for drug repositioning via the chemical-protein interactome. Results showed that the retinoic acid receptor alpha (RARα), a target protein in acute promyelocytic leukemia (APL), was in the top rank, with a pharmacophore model matching well the molecular features of Tanshinone IIA. Moreover, molecular docking and drug repurposing results showed that the complex was also matched in terms of structure and chemical-protein interactions. These results indicated that RARα may be a potential target of Tanshinone IIA for APL. The study can provide useful information for further biological and biochemical research on natural compounds.

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Tanshinone II-A: new perspectives for old remedies

Cited by 128 publications

References 23 publications

Tanshinone IIA Exhibits Anticonvulsant Activity in Zebrafish and Mouse Seizure Models

Tanshinone IIA Exhibits Anticonvulsant Activity in Zebrafish and Mouse Seizure Models

Tanshinone IIA suppresses cholesterol accumulation in human macrophages: role of heme oxygenase-1

A Potential Target of Tanshinone IIA for Acute Promyelocytic Leukemia Revealed by Inverse Docking and Drug Repurposing

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