OBJECTIVETo analyze the content of tanshinone IIA in Radix Salviae Miltiorrhizae from different habitats are regularly altered and find out the deviation between the studies.

METHODThe data of the content of tanshinone IIA in samples of Radix Salviae Miltiorrhizae from different areas and related information since 1997 was collected and statistically analyzed.

RESULT AND CONCLUSIONThe content of tanshinone IIA in wild Salvia was generally higher than that in the cultivated Salvia, and the content in nearly half cultivated Salvia was less than 0.2%. There existed a big difference between the used statistical model, and the data related the content in samples from Sichuan was the most divisive. The coefficient of variation of wild Salvia was below the cultivated Salvia, and the cultivated Salvia from different areas showed different coefficients of variation. The content of tanshinone IIA was lower when samples were extracted using the heating reflux method.

Diterpenes, Abietane ; Phenanthrenes ; analysis ; Salvia miltiorrhiza ; chemistry

OBJECTIVETo compare the influence on the dissolution of tanshinone IIA (TS IIA) solid dispersions in complex carriers and single, which used in preparation of TS IIA solid dispersions, and further enhance the dissolution of TS IIA.

METHODThe TS IIA solid dispersions were prepared by solvent technique with polyvinylpyrrolidone K30 (PVPK30), poloxamer188 (F68) and combination of PVPK30 and F68 as carriers, respectively. The physical characteristics of TS IIA solid dispersions was studied using differential scanning calorimetry (DSC). Dissolution rates were studied using small cup method (CHP XC III). The solubility of TS IIA with the solid dispersions and pure drug form were determined by HPLC method.

RESULTThe DSC analysis suggested that TS IIA was dispersed as an amorphous form in the combination of PVPK30 and F68. Dissolution profile of the prepared solid dispersions could be described by Weibull equation (R>0.99). For tested three carries, Td value (calculated time to 63.2% of total drug release according to Weibull equation) were (90.40 +/- 2.82) min, (204.5 +/- 8.20) min and (25.83 +/- 0.13) min, respectively. The PVPK30/F68-TS IIA solid dispersion resulted in a significant increase of TS IIA solubility compared with prepared PVPK30-TS IIA and F68-TS IIA solid dispersions (P<0.01).

CONCLUSIONAs compared to single use of PVPK30 or F68, the combination of PVPK30 and F68 improve the dissolution rate and solubility of TS IIA significantly in the prepared solid dispersions (P<0.01). The application of complex carriers in solid dispersion technology should be paid more attention to improvement of poorly soluble drugs dissolution in the future.

Diterpenes, Abietane ; Phenanthrenes ; chemistry ; Solubility ; Temperature

The technique of liquisolid compress is a new technique developed in 1990s, which was considered to be the most promising technique to improve the dissolution of water-insoluble drugs. In this article, tanshinone II(A) and the extracts of the ester-solubility fractions were chosen as the model drugs to evaluate the effects of the liquisolid technique for enhancement of dissolution properties of tanshinone II(A). Several liquisolid tablets (LS) formulations containing different dosage of drugs and various liquid vehicle were pre-pared and for all the formulations, microcrystalline cellulose and silica were chosen as the carrier and coating materials to evaluate their flow properties, such as angle of repose, Carr's compressibility index and Hausner's ratio. The interaction between drug and excipients in prepared LS compacts were studied by differential scanning calorimetry(DSC) and X-ray powder diffraction (XRPD). The dissolution curves of tanshinone II(A) from liquisolid compacts were investigated to determine the technique's effect in improving the dissolution of tanshinone II(A) and its impacting factors. According to the results, the dissolution increased with the rise in the dissolution of the liquid-phase solvent. The R-value and drug dosage can significantly affect the drug release, but with less impact on active fractions. This indicated that liquisolid technique is a promising alternative for improvement of dissolution property of water-soluble drugs, and can make a synergistic effect with other ester-soluble constituents and bettern improve the release of tanshinone II(A). Therefore, the technique of liquisolid compress will have a better development prospect in traditional Chinese medicines.
Calorimetry, Differential Scanning ; Diterpenes, Abietane ; chemistry ; Solubility ; X-Ray Diffraction

OBJECTIVETo study chemical constituents from pine cone of Pinus annandii.

METHODThe constituents were isolated by chromatographic method and the structures were identified on the basis of spectral analysis.

RESULTSeven compounds were identified as sandaracopimaric acid (I), isodextropimaric acid (II), 12-hydroxyabietic acid (III), dehydroabietic acid (IV), 15-hydroxydehydroabietic acid (V), beta-sitosterol (VI) and daucosterol (VII).

CONCLUSIONCompounds I-IV were isolated from this plant for the first time.

Diterpenes ; chemistry ; isolation & purification ; Diterpenes, Abietane ; chemistry ; isolation & purification ; Fruit ; chemistry ; Pinus ; chemistry ; Plants, Medicinal ; chemistry ; Sitosterols ; chemistry ; isolation & purification

BACKGROUND/AIMS: Ecabet sodium is known for its bactericidal effect against H. pylori. It was reported that a supplement of ecabet sodium to conventional triple therapy showed good results in Asia. The Aim of this study was to ascertain the efficacy of additional ecabet sodium on conventional triple therapy for eradication of H. pylori. METHODS: We reviewed the cases of 111 patients (Group A) with H. pylori infection who received ecabet sodium with triple therapy (20 mg of rabeprazole, 1 g of amoxicillin, 500 mg of clarithromycin and 1 g of ecabet sodium, twice daily for 7 days). Another 186 patients (Group B) received PPI-based triple therapy (same as the above, except without the ecabet sodium). Eradication was evaluated 4 weeks later after completion of treatment by 13C-UBT. RESULTS: Eradication rates were 74.8% (83/111) in group A and 70.4% (131/186) in group B by intention-to-treat analysis (p=0.420), and 75.2% (82/109) in group A and 70.7% (128/181) in group B by per protocol analysis (p=0.405). CONCLUSIONS: The addition of ecabet sodium to conventional triple therapy did not increase the eradication rate of H. pylori in this study. These findings imply that ecabet sodium as an additional agent cannot overcome antibiotic resistance, which is the most important cause of failure of triple therapy.
2-Pyridinylmethylsulfinylbenzimidazoles ; Amoxicillin ; Asia ; Clarithromycin ; Diterpenes, Abietane ; Drug Resistance, Microbial ; Helicobacter ; Helicobacter pylori ; Humans ; Korea ; Sodium

OBJECTIVETo study the relationship between functional gene expression in Salvia miltiorrhiza from different producing areas and active principles, which might provide scientific basis for the gene regulation of tanshinones.

METHODThe quantitative determination of cryptotanshinone and tanshinone II A was carried out by using HPLC method, expression level of 3 functional genes of SmAACT, SmCMK and SmIPPI were investigated by real-time PCR method.

RESULTThe content of active principles together with expression level of SmAACT and SmCMK were higher in S. miltiorrhiza from genuine producing areas including Henan and Shanxi, but lower in samples from Beijing which was non-genuine producing area.

CONCLUSIONExpression level of SmAACT and SmCMK had close relationships involving tanshinones' accumulation, but the SmIPPI gene had not.

Diterpenes, Abietane ; metabolism ; Gene Expression ; Real-Time Polymerase Chain Reaction ; Salvia miltiorrhiza ; genetics ; metabolism

The fibrous roots are the residues of production of cut crude drug of Danshen (Salvia miltiorrhiza). Enzymatic pretreatment and ultrasonic extraction are beneficial to extract effective constituents from fibrous roots more effectively. The present research was to optimize the enzymatic parameters by the central composite design and response surface method. Under the best conditions, the yields of total tanshinones and total salvianolic acids in the extracts of enzymatic pretreatment increased by 113.92% and 30.64%, comparing with the non-enzymatic extraction, respectively. TLC analysis also showed that the types of effective constituents in the two samples were not affected by enzymatic hydrolysis. Meanwhile, the complex correlation coefficients of the mathematical models were high, which provided a good prediction.
Diterpenes, Abietane ; Drugs, Chinese Herbal ; chemistry ; Phenanthrenes ; chemistry ; Plant Roots ; chemistry ; Salvia miltiorrhiza ; chemistry

Synthetic biology research methods which design and build a new artificial biological systems (medicinal plants or microorganisms system) with specific physiological functions through clarifying and simulating the basic law of the biosynthesis of active components of traditional Chinese medicine, is considered to be a potential method to produce an abundant resources of bioactive components. Tanshinones is a kind of diterpene quinone compounds with important pharmacological activities from traditional Chinese medicine Salvia miltiorrhiza. This article systematically introduced the research progress of the synthetic biology of S. miltiorrhiza, in order to provide references for studies on other terpenoid bioactive components of traditional Chinese medicines, and give new research strategies for the sustainable development of traditional Chinese medicine resources.
Diterpenes, Abietane ; biosynthesis ; Medicine, Chinese Traditional ; Salvia miltiorrhiza ; metabolism ; Synthetic Biology

OBJECTIVETo prepare the solid dispersion of tanshinone II A (TS II A) by the combined application of nano-silica and poloxamer 188 (F68), in order to observe its dissolution and stability.

METHODTanshinone II A solid dispersion was prepared by the solvent method with nano-silica and poloxamer 188 as binary vectors. Its physical characteristics, in vitro dissolution and stability were further assessed.

RESULTThe tanshinone II solid dispersion was prepared with the weight ratio of nano-silica and poloxamer 188 of 1: 3. The differential scanning calorimetry (DSC) demonstrated that Tanshinone II A existed in vectors as amorphous state. The in vitro dissolution of tanshinone II A solid dispersion is up to 90% at 60 min. Accelerating experiment showed that content and in vitro dissolution of tanshinone II A solid dispersion did not change after storage over 3 months.

CONCLUSIONSolid dispersion of binary vector of tanshinone II A can obviously improve the dissolution and stability of tanshinone II in practice.

Calorimetry, Differential Scanning ; Diterpenes, Abietane ; chemistry ; Drug Stability ; Drugs, Chinese Herbal ; chemistry ; Solubility

Porous silica was used as a carrier to prepare tanshinone solid dispersions (SDs). sThe effect of the spray drying method or the solvent method on the drug dissolution of SD was studied. The structure characteristics of SDs was analyzed by SEM, DSC,XPRD and FTIR. And in vitro dissolution was also investigated. The results showed that drugs were highly dispersed into SDs prepared by spray drying method and the solvent method in amorphous form. In addition, the results of the dissolution tested in vitro exhibited that the tanshinone I and tanshinone II A, accumulated dissolutions of SDs prepared using solvent achieved 80. 9% ,84. 6% and 86. 2% ,88. 7% within 45,60 min, respectively. And SDs prepared using spray-drying method were 92.7% ,95. 3% and 95. 8%, 97. 1% within 45,60 min, respectively. The tanshinone SDs were prepared successfully by spray drying method and solvent method. The SDs prepared by spray drying method was more conducive to improving the dissolution.
Calorimetry, Differential Scanning ; Diterpenes, Abietane ; chemistry ; isolation & purification ; Porosity ; Silicon Dioxide ; chemistry ; Spectroscopy, Fourier Transform Infrared