Salvia miltiorrhiza Burge (Danshen) is an eminent medicinal herb that possesses broad cardiovascular and cerebrovascular protective actions and has been used in Asian countries for many centuries. Accumulating evidence suggests that Danshen and its components prevent vascular diseases, in particular, atherosclerosis and cardiac diseases, including myocardial infarction, myocardial ischemia/reperfusion injury, arrhythmia, cardiac hypertrophy and cardiac fibrosis. The published literature indicates that lipophilic constituents (tanshinone I, tanshinone IIa, tanshinone IIb, cryptotanshinone, dihydrotanshinone, etc) as well as hydrophilic constituents (danshensu, salvianolic acid A and B, protocatechuic aldehyde, etc) contribute to the cardiovascular protective actions of Danshen, suggesting a potential synergism among these constituents. Herein, we provide a systematic up-to-date review on the cardiovascular actions and therapeutic potential of major pharmacologically active constituents of Danshen. These bioactive compounds will serve as excellent drug candidates in small-molecule cardiovascular drug discovery. This article also provides a scientific rationale for understanding the traditional use of Danshen in cardiovascular therapeutics.

/pdf/salvia-miltiorrhizaburge-danshen-a-golden-herbal-medicine-in-44a11r5kxf.pdf

Salvia miltiorrhizaBurge (Danshen): a golden herbal medicine in cardiovascular therapeutics.

Tanshinone IIA protects cardiac myocytes against oxidative stress-triggered damage and apoptosis.

Tanshinones are a class of abietane diterpene compound isolated from Salvia miltiorrhiza (Danshen or Tanshen in Chinese), a well-known herb in Traditional Chinese Medicine (TCM). Since they were first identified in the 1930s, more than 40 lipophilic tanshinones and structurally related compounds have been isolated from Danshen. In recent decades, numerous studies have been conducted to investigate the isolation, identification, synthesis and pharmacology of tanshinones. In addition to the well-studied cardiovascular activities, tanshinones have been investigated more recently for their anti-cancer activities in vitro and in vivo. In this review, we update the herbal and alternative sources of tanshinones, and the pharmacokinetics of selected tanshinones. We discuss anti-cancer properties and identify critical issues for future research. Whereas previous studies have suggested anti-cancer potential of tanshinones affecting multiple cellular processes and molecular targets in cell culture models, data from in vivo potency assessment experiments in preclinical models vary greatly due to lack of uniformity of solvent vehicles and routes of administration. Chemical modifications and novel formulations had been made to address the poor oral bioavailability of tanshinones. So far, human clinical trials have been far from ideal in their design and execution for the purpose of supporting an anti-cancer indication of tanshinones.

https://www.mdpi.com/1422-0067/13/10/13621/pdf

Tanshinones: Sources, Pharmacokinetics and Anti-Cancer Activities

Inclusion of terpenes in cyclodextrins: Preparation, characterization and pharmacological approaches.

In this study, solid lipid nanoparticles (SLNs) were successfully prepared by an ultrasonic and high-pressure homogenization method to improve the oral bioavailability of the poorly water-soluble drug cryptotanshinone (CTS). The particle size and distribution, drug loading capacity, drug entrapment efficiency, zeta potential, and long-term physical stability of the SLNs were characterized in detail. A pharmacokinetic study was conducted in rats after oral administration of CTS in different SLNs, and it was found that the relative bioavailability of CTS in the SLNs was significantly increased compared with that of a CTS-suspension. The incorporation of CTS in SLNs also markedly changes the metabolism behavior of CTS to tanshinone IIA. These results indicate that CTS absorption is enhanced significantly by employing SLN formulations, and SLNs represent a powerful approach for improving the oral absorption of poorly soluble drugs.

/pdf/preparation-and-enhanced-oral-bioavailability-of-2entvqmglm.pdf

Preparation and enhanced oral bioavailability of cryptotanshinone-loaded solid lipid nanoparticles.

The nature of intestinal absorption of most herbal medicine is unknown. Cryptotanshinone (CTS) is the principal active constituent of the widely used cardiovascular herb Salvia miltiorrhiza (Danshen). We investigated the oral bioavailability of CTS in rats and the mechanism for its intestinal absorption using several in vitro and in vivo models: 1) Caco-2 cell monolayers; 2) monolayers of MDCKII cells overexpressing P-glycoprotein (PgP); and 3) single-pass rat intestinal perfusion with mesenteric vein cannulation. The systemic bioavailabilities of CTS after oral and intraperitoneal administration at 100 mg/kg were 2.05 and 10.60%, respectively. In the perfused rat intestinal model, permeability coefficients based on CTS disappearance from the luminal perfusate ( P lumen) were 6.7- to 10.3-fold higher than permeability coefficients based on drug appearance in venous blood ( P blood). P blood significantly increased in the presence of the P-gP inhibitor, verapamil. CTS transport across Caco-2 monolayers was pH-, temperature- and ATP-dependent. The transport from the apical (AP) to the basolateral (BL) side was 3- to 9-fold lower than that from the BL to the AP side. Inclusion of verapamil (50 μM) in both AP and BL sides abolished the polarized CTS transport across Caco-2 cells. Moreover, CTS was significantly more permeable in the BL to AP than in the AP to BL direction in MDCKII and MDR1-MDCKII cells. The permeability coefficients in the BL to AP direction were significantly higher in MDCKII cells overexpressing PgP. These findings indicate that CTS is a substrate for PgP that can pump CTS into the luminal side.

A mechanistic study of the intestinal absorption of cryptotanshinone, the major active constituent of Salvia miltiorrhiza.

A liquid chromatography/tandem mass spectrometry (LC/MS/MS) method was developed and validated for determining tanshinone IIA in rat tissues. After a single step liquid-liquid extraction with diethyl ether, tanshinone IIA and loratadine (internal standard) was subjected to LC/MS/MS analysis using positive electro-spray ionization under selected reaction monitoring mode. Chromatographic separation of tanshinone IIA and loratadine was achieved on a Hypersil BDS C(18) column (i.d. 2.1 x 50 mm, 5 microm) with a mobile phase consisting of methanol-1% formic acid (90:10, v/v) at a flow rate of 300 microL/min. The intra-day and inter-day precision of the method were less than 10.2 and 12.4%, respectively. The intra-day and inter-day accuracies ranged from 99.7 to 109.7%. The lowest limit of quantification for tanshinone IIA was 1 ng/mL. The method was applied to a tanshinone IIA tissue distribution study after an oral dose of 60 mg/kg to rats. Tanshinone IIA tissue concentrations decreased in the order of stomach > small intestine > lung > liver > fat > muscle > kidneys > spleen > heart > plasma > brain > testes. Tanshinone IIA still could be detected in most of the tissues at 20 h post-dosing. These results indicate that the LC/MS/MS method was rapid and sensitive to quantify tanshinone IIA in different rat tissues.

Study of tanshinone IIA tissue distribution in rat by liquid chromatography-tandem mass spectrometry method.

Cryptotanshinone is the major active component from the root of Salvia miltiorrhiza which has been widely used for the management of coronary heart disease. The aims of this study were to develop and validate an HPLC method for the determination of cryptotanshinone in the human intestinal cell line Caco-2 monolayers, and to investigate the transport kinetics of cryptotanshinone. The developed HPLC method was sensitive and reliable, with acceptable accuracy (90–110% of true values) and precision (intra- and inter-assay CV  0.999. The validated HPLC method was applied to examine the epithelial transport of cryptotanshinone by Caco-2 monolayers. The transport across the monolayers from the apical (B) to basolateral (A) side was significantly higher than that from A to B side. The structural analog of cryptotanshinone and a known substrate of P-glycoprotein, tanshinone IIA, dramatically inhibited the B to A transport of cryptotanshinone in the monolayers. These results indicate that the developed HPLC method was suitable for the study of transport of cryptotanshinone by Caco-2 monolayers and cryptotanshinone is a substrate of P-glycoprotein.

Determination of Cryptotanshinone, a Major Active Component in Salvia miltiorrhiza , in Caco-2 Monolayers by HPLC with UV Detection

1. The study aimed to investigate the pharmacokinetics of cryptotanshinone in a hydroxylpropyl-β-cyclodextrin-included complex in dogs and rats.2. Animals were administrated the inclusion complex of cryptotanshinone and the concentrations of cryptotanshinone and its major metabolite tanshinone IIA were determined by a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method.3. Cryptotanshinone in inclusion complex was absorbed slowly after an oral dose, and the Cmax and AUC0–t were dose-proportional. The bioavailability of cryptotanshinone in rats was (6.9% ± 1.9%) at 60 mg kg−1and (11.1% ± 1.8%) in dogs at 53.4 mg kg−1. The t1/2 of the compound in rats and dogs was 5.3–7.4 and 6.0–10.0 h, respectively. Cryptotanshinone showed a high accumulation in the intestine, lung and liver after oral administration, while the lung, liver and heart had the highest level following intravenous dose. Excretion data in rats showed that cryptotanshinone and its metabolites were mainly eliminated from faeces and bi...

Pharmacokinetic characterization of hydroxylpropyl-β-cyclodextrin-included complex of cryptotanshinone, an investigational cardiovascular drug purified from Danshen (Salvia miltiorrhiza)

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Papers

A mechanistic study of the intestinal absorption of cryptotanshinone, the major active constituent of Salvia miltiorrhiza.

Study of tanshinone IIA tissue distribution in rat by liquid chromatography-tandem mass spectrometry method.

Determination of Cryptotanshinone, a Major Active Component in Salvia miltiorrhiza , in Caco-2 Monolayers by HPLC with UV Detection

Pharmacokinetic characterization of hydroxylpropyl-β-cyclodextrin-included complex of cryptotanshinone, an investigational cardiovascular drug purified from Danshen (Salvia miltiorrhiza)