benzofurans and isoborneol

Fufang Danshen preparation (FDP) is consisted of Salviae Miltiorrhizar Radix et Rhizoma (Danshen), Notoginseng Radix et Rhizoma (Sanqi) and Borneolum Syntheticum (borneol). FDP is usually used to treat myocardial ischemia hypoxia, cerebral ischemia and alzheimer's disease, etc. In the treatment of cerebrovascular diseases, borneol is usually used to promote the absorption and distribution of the bioactive components to proper organs, especially to the brain. The purpose of this study is investigating the effects of borneol on the pharmacokinetics and brain distribution of tanshinone IIA (TS IIA), salvianolic acid B (SAB) and ginsenoside Rg1 in FDP. Male healthy Sprague-Dawley (SD) rats were given Danshen extracts, Sanqi extracts (Panax notoginsengsaponins) or simultaneously administered Danshenextracts, Sanqi extracts and borneol. Plasma and brain samples were collected at different points in time. The concentration of TS IIA, SAB and Rg1 was determined by UPLC-MS/MS method. The main pharmacokinetics parameters of plasma and brain tissue were calculated by using Phoenix WinNolin 6.1 software. In comparison with Danshen and Sanqi alone, there were significant differences in pharmacokinetic parameters of TS IIA, SAB and Rg1, and the brain distribution of SAB and TS IIA when Danshen, Sanqi and borneol were administrated together. Borneol statistically significant shortened t

Topics: Abietanes; Animals; Benzofurans; Brain; Camphanes; Chromatography, Liquid; Drugs, Chinese Herbal; Ginsenosides; Male; Rats; Rats, Sprague-Dawley; Tandem Mass Spectrometry

Salviae miltiorrliza-borneol Jun-Shi coupled-herbs have been widely used for treatment of ischemia stroke. Salvianolic acid B was the most abundant and bioactive compound of Salviae miltiorrliza and used for prevention and treatment of cerebrovascular diseases. However, the scientific intension and compatible mechanism of Salvianolic acid B - borneol combination were still unknown. A metabolomics study approach based on ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-Q/TOF-MS) combined with a pathological study has been applied to study the metabolic disturbances of cerebral ischemia and evaluate the efficacies of Sal B and Sal B/borneol against cerebral ischemia in middle cerebral artery occlusion (MCAO) rats. The neuroprotection of Sal B and Sal B/borneol was reversed through the evaluation of neurological deficits, infarct volume, and neuronal apoptosis in MCAO model. The metabonomic analysis revealed that the MCAO-induced cerebral ischemia could be ameliorated by Sal B through improving the energy metabolism, lipids metabolism, inflammatory responses, and oxidant stress. Borneol could enhance the neuroprotective effects, was associated with the increased concentration of Sal B, and attenuate the function of sphingolipid metabolism pathway in cerebral ischemia rats. These findings perhaps clarify the mechanism of neuroprotective effects of treating ischemia stroke by Sal B or Sal B/borneol preliminarily through metabolomics and push the quality promotion and the composition of borneol/Sal B in secondary development of prescription.

Topics: Animals; Benzofurans; Brain Ischemia; Camphanes; Chromatography, High Pressure Liquid; Male; Malondialdehyde; Mass Spectrometry; Metabolic Networks and Pathways; Metabolome; Metabolomics; Multivariate Analysis; Neuroprotection; Oxidative Stress; Principal Component Analysis; Rats, Sprague-Dawley

To determine the contents of salvianolic acid B and borneol in compound Danshen tablet (composed of Salviae Miltiorrhizae Radix et Rhizome, Notoginseng Radix et Rhizome and Borneolum Syntheticum) by near-infrared spectroscopy (NIR) and to establish a dependency model for rapid quantitative analysis. NIR data of 74 batches of compound Danshen tablet from different companies were collected; the contents of salvianolic acid B and borneol were determined by using high performanceliquid chromatography (HPLC) and gas chromatography (GC) respectively to establish the dependency model for salvianolic acid B and borneol. The results showed that the best waveband for salvianolic acid B was 10 846.2-10 013, 9 195.3-8 362.2, 6 719.1-4 242.8 cm⁻¹; root-mean-squares error of cross-validation (RMSECV), coefficient of determination

Topics: Benzofurans; Camphanes; Salvia miltiorrhiza; Spectroscopy, Near-Infrared; Tablets

The main purpose of this study was to illustrate the effect of borneol on pharmacokinetics of salvianolic acid B (SalB) in rats after oral administration of SalB with different doses of borneol. The concentrations of SalB in rat plasma were determined by an established and validated LC-MS/MS method. Our data showed that when 20, 40, and 80 mg kg⁻¹ of borneol were orally administrated with SalB at 50 mg kg⁻¹, C (max) of SalB was increased by 18.4%, 55.8%, and 103.2% compared with that of SalB alone. And AUC(0-t) of SalB in plasma was increased by 14.4%, 48.5%, and 123.3%, respectively. The results indicated that borneol is able to enhance the intestinal absorption and relative bioavailability of SalB, with a positive dose-dependent relationship. The described herb-drug interactions might prove the scientific rationality of the compatible ratio of traditional Chinese medicines.

Topics: Administration, Oral; Animals; Benzofurans; Camphanes; Dose-Response Relationship, Drug; Male; Medicine, Chinese Traditional; Rats

Salviae miltiorrhizae is one of the most commonly used herbal plants in the treatment of numerous ailments including cardiovascular diseases for hundreds of years. According to the theory of traditional Chinese herbal medicine, S. miltiorrhizae is always used in combination with borneol to obtain better pharmacological effects. The purpose of this study was to investigate the effects of borneol on the pharmacokinetic and bioavailability of S. miltiorrhizae. The pharmacokinetics studying on rosmarinic acid, salvianolic acid A and salvianolic acid B which are the main active compounds of S. miltiorrhizae in rat plasma, was achieved using a optimal high-performance liquid chromatographic technique coupled with liquid-liquid extraction method. After administration of either single salvianolic acids or salvianolic acids in combination with borneol, plasma concentrations of rosmarinic acid, salvianolic acid A and salvianolic acid B of male Sprague-Dawley rats were determined at different time points (5, 10, 20, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min). In comparison with salvianolic acid extract alone, there were statistically significant differences in pharmacokinetic parameters of rosmarinic acid, salvianolic acid B and salvianolic acid A, and the bioavailability of the three salvianolic acids increased by different degrees when the salvianolic acid extract and borneol were administered together. These results indicated that borneol could enhance the intestinal absorption, decrease the distribution and inhibit the metabolism of salvianolic acids.

Topics: Animals; Benzofurans; Biological Availability; Caffeic Acids; Camphanes; Cinnamates; Depsides; Drugs, Chinese Herbal; Lactates; Male; Random Allocation; Rats; Rats, Sprague-Dawley; Reproducibility of Results; Rosmarinic Acid; Salvia miltiorrhiza; Sensitivity and Specificity

This study aimed to investigate the effects of concentration, intestinal section and borneol on the intestinal absorption of salvianolic acids. The experiment not only studied the intestinal absorption properties of three concentrations of rosmarinic acid, salvianolic acid B and salvianolic acid A at duodenum, jejunum and ileum, but also of salvianolic acids compatible with borneol at different concentrations using single-pass intestinal perfusion model in rat with phenol red as the marker. The results showed that salvianolic acids was stable under weak-acid condition and affected by metabolism enzyme; The Peff and Ka significantly different among three concentrations of rosmarinic acid and salvianolic acid B, whose intestinal absorption were saturated in high concentration, suggesting that the transport mechanisms of rosmarinic acid and salvianolic acid B were similar to active transport or facilitated diffusion; However, there was inconspicuousness in the Peff and Ka of salvianolic acid A at different concentrations, whose absorption was not saturated in high concentration, indicating that the transport mechanisms of salvianolic acid A was passive diffusion; The Peff and Ka in the ileum obviously higher than those in the duodenum and jejunum, namely the ileum was the best absorption section; When concentration of borneol increased, the enhancing effect of intestinal absorption of salvianolic acids increased, but significantly decreased when borneol increased to some degree. The enhancing effect of medium borneol concentration was the optimum. This implied that borneol can enhance the intestinal absorption of salvianolic acids, and the capacity of enhancing effect was influenced by the concentration of borneol.

Topics: Animals; Benzofurans; Caffeic Acids; Camphanes; Cinnamates; Depsides; Dose-Response Relationship, Drug; Duodenum; Ileum; Intestinal Absorption; Jejunum; Lactates; Male; Perfusion; Plants, Medicinal; Rats; Rats, Sprague-Dawley; Rosmarinic Acid; Salvia miltiorrhiza