Amiodarone (AD) is a benzofuran derivative that has been used for the treatment of recurrent arrhythmia and as a coronary vasodilator in Europe since 1964. AD-related hyperpigmentation develops after an average of 20 months of continuous AD treatment and with a minimal total dose of 160 g AD in less than 10% of the patients. A 49-year-old man presented with asymptomatic blue-gray patches that had slowly developed on the face over the previous 3 months. He had been taken amiodarone continuously for 39 months (cumulative dose: 974 g). A skin lesion biopsy from the face showed many dermal melanophages containing brown granules. The AD was discontinued and he begin using sunscreen and is courrently being followed-up. The skin discoloration was still evident, but slightly diminished at five month's follow up.
Amiodarone ; Arrhythmias, Cardiac ; Benzofurans ; Biopsy ; Europe ; Follow-Up Studies ; Humans ; Hyperpigmentation ; Middle Aged ; Pigmentation ; Skin

No abstract available.
Benzofurans ; Depsides ; Diabetic Nephropathies

Usnic acid and its derivatives, a group of organic molecules with great importance, are characteristic to lichens, possessing pharmacological activities such as anti-virus, anti-bacteria, anti-humor, anti-inflammatory, analgesic, and anaesthetic effects. Many of them have been widely used as medicine, but also bring side effects such as dermatitis and liver damages. In the past decades, great efforts by isolation, organic synthesis, and structure modification methods were put on discovery of UA derivatives with higher biological activities or less side effects. This paper describes herein the most progress on natural sources, isolation and structure elucidation, structural characteristics, synthesis and modification results, pharmacological activities and toxicities of UA and its derivatives, hopefully to provide valuable reference for further research.
Benzofurans ; chemistry ; pharmacology ; Biological Products ; Lichens ; chemistry

Salvianolic acid B(Sal B) is the main water-soluble component of Salvia miltiorrhiza Bunge. Studies have found that Sal B has a good protective effect on blood vessels. Sal B can protect endothelial cells by anti-oxidative stress, inducing autophagy, inhibiting endoplasmic reticulum stress(ERS), inhibiting endothelial inflammation and adhesion molecule expression, inhibiting endothelial cell permeability, anti-thrombosis, and other ways. In addition, Sal B can alleviate endothelial cell damage caused by high glucose(HG). For vascular smooth muscle cell(VSMC), Sal B can reduce the synthesis and secretion of inflammatory factors by inhibiting cyclooxygenase. It can also play a vasodilatory role by inhibiting Ca~(2+) influx. In addition, Sal B can inhibit VSMC proliferation and migration, thereby alleviating vascular stenosis. Sal B also inhibits lipid deposition in the subendothelium, inhibits macrophage conversion to foam cells, and reduces macrophage apoptosis, thereby reducing the volume of subendothelial lipid plaques. For some atherosclerosis(AS) complications, such as peripheral artery disease(PAD), Sal B can promote angiogenesis, thereby improving ischemia. It should be pointed out that the conclusions obtained from different experiments are not completely consistent, which needs further research. In addition, previous pharmacokinetics showed that Sal B was poorly absorbed by oral administration, and it was unstable in the stomach, with a large first-pass effect in the liver. Sal B had fast distribution and metabolism in vivo and short drug action time. These affect the bioavailability and biological effects of Sal B, and the development of clinically valuable Sal B non-injectable delivery systems remains a great challenge.
Endothelial Cells ; Oxidative Stress ; Benzofurans/pharmacology* ; Lipids

OBJECTIVEThis study investigated the effects of salvianolic acid B (Sal B), a major bioactive component of the Chinese medicine salvia miltiorrhiza, on osteogenic differentiation of human periodontal ligament cells (hPDLCs).

METHODSThird passage PDLCs were used in this experiment. Methyl thiazolyl tetrazolium (MTT) method was employed to observe the effects of different Sal B concentrations on proliferation activity of hPDLCs. Alkaline phosphatase (ALP) activity and mineralization capability were measured, and mRNA expression of osteocalcin (OCN) was detected to investigate the effects of Sal B on osteogenesis of hPDLCs.

RESULTSSal B did not influence the viability of hPDLCs. The ALP activity and OCN mRNA expression levels of hPDLCs were both significantly improved (P<0.05) under treatment with different Sal B concentrations (0.5, 1, and 5 μmol·L⁻¹) compared with those in OIM group. Moreover, the number of mineralized nodules formed by hPDLCs were considerably higher under treatment with different Sal B concentrations (0.5, 1, and 5 μmol·L⁻¹) than that in the OIM group.

CONCLUSIONSAppropriate Sal B concentration can improve the osteogenic differentiation of hPDLCs.

Benzofurans ; Cell Differentiation ; Cells, Cultured ; Humans ; Osteocalcin ; Osteogenesis ; Periodontal Ligament

OBJECTIVEThis study aimed to investigate the effects of different light quality on the growth, accumulation of active ingredients and enzymes activities of Salvia miltiorrhiza.

METHODThe seedlings of S. miltiorrhiza were treated by different light quality, and relative parameters were measured. The data was statistically processed.

RESULTPlant height was significantly decreased with supplemental blue light (WB), and the root length, root diameter, root fresh weight and root dry weight were significantly increased with supplemental red light (WR). Salvianolic acid B concentration in S. miltiorrhiza was highly increased by supplemental blue and red light, but tanshinone IIA concentration was not significantly affected by supplemental blue and red light. Enzymes activities of SOD, POD, PAL, TAT and PPO in S. miltiorrhiza were significant increased by supplemental blue light, and enzymes activities of POD, TAT and PPO were significant increased by supplemental red light.

CONCLUSIONThe root growth of S. miltiorrhiza was greatly promoted by supplemental red light (WR). Salvianolic acid B concentration in S. miltiorrhiza was highly increased by supplemental blue and red light. Enzymes activities of TAT and PPO in S. miltiorrhiza were significant increased by supplemental blue light and red light.

Benzofurans ; analysis ; Light ; Salvia miltiorrhiza ; chemistry ; enzymology ; growth & development

OBJECTIVE: To determine whether salvianolic acid B (Sal B) exerts protective effects on diabetic peripheral neuropathy by attenuating apoptosis and pyroptosis. METHODS: RSC96 cells were primarily cultured with DMEM (5.6 mmol/L glucose), hyperglycemia (HG, 125 mmol/L glucose) and Sal B (0.1, 1, and 10 µ mol/L). Cells proliferation was measured by 3-(4, 5-cimethylthiazol-2-yl)-2, 5-dilphenyltetrazolium bromide assay. Reactive oxygen species (ROS) generation and apoptosis rate were detected by flow cytometry analysis. Western blot was performed to analyze the expressions of poly ADP-ribose polymerase (PARP), cleaved-caspase 3, cleaved-caspase 9, Bcl-2, Bax, NLRP3, ASC, and interleukin (IL)-1β. RESULTS: Treatment with HG at a concentration of 125 mmol/L attenuated cellular proliferation, while Sal B alleviated this injury (P<0.05). In addition, Sal B inhibited HG-induced ROS production and apoptosis rate (P<0.05). Furthermore, treatment with Sal B down-regulated HG-induced PARP, cleaved-caspase 3, cleaved-caspase 9, Bax, NLRP3, ASC, and IL-1β expression, but mitigated HG-mediated down-regulation of Bcl-2 expression (P<0.05). CONCLUSION Sal B may protect RSC96 cells against HG-induced cellular injury via the inhibition of apoptosis and pyroptosis activated by ROS.
Apoptosis ; Benzofurans/pharmacology* ; Oxidative Stress ; Pyroptosis ; Reactive Oxygen Species/metabolism*

OBJECTIVETo study the chemical changes of salvianolic acid B and lithospermic acid of Salvia miltiorrhiza under the conditions of high temperature and high pressure and explore the reaction mechanism.

METHODS. miltiorrhiza extracts, salvianolic acid B and lithospermic acid were put in the reactor under the conditions of high temperature and high pressure (120 degrees C, 0.2 MPa), and the chemical changes and stability was studied.

RESULTSalvianolic acid A was the primary product in salvianolic acid B and lithospermic acid's conversion process, and lithospermic acid was an intermediate in the conversion process of salvianolic acid B. Compared with salvianolic acid B, lithospermic acid could convert into more salvianolic acid A and fewer other products in the same conditions. Salvianolic acid A was not stable under the conditions of high temperature and high pressure, and could sequentially convert into other small molecules.

CONCLUSIONReferring to the chemical conversion of salvianolic acid B and lithospermic acid, a method of large-scale preparation of salvianolic acid A can be developed.

Benzofurans ; analysis ; Caffeic Acids ; analysis ; Depsides ; analysis ; Hot Temperature ; Lactates ; analysis ; Pressure ; Salvia miltiorrhiza ; chemistry

OBJECTIVETo establish a new quality evaluation method for traditional Chinese medicine preparations, using one chemical reference substance to calcutate multi-components simultaneously.

METHODEmployed puerarin as the maker component, puerarin relative correction factors (RCF) of salvianolic acid B to puerarin and paidzein to puerarin were calcatated in the chromatographic conditions for determination of the three components in Guanmaikang capsules. The contents of Puerarin were determined by external standard method, and those of salvianolic acid B and paidzein were calculated by puerarin and their RCF. The accuracy of the new method was evaluated by comparing the calculated contents with the determined.

RESULTThe analysis methods were established, and it has been no significant difference between the calculated contents and determined contents.

CONCLUSIONSThe method can control the components without providing salvianolic acid B and paidzein reference. It is to be a suitable quality evaluation pattern for TCM Preparation.

Benzofurans ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Isoflavones ; chemistry ; Medicine, Chinese Traditional ; methods ; Reference Standards

Benzofurans ; analysis ; chemistry ; Dibenzofurans, Polychlorinated ; Dioxins ; analysis ; chemistry ; Humans ; Occupational Exposure ; prevention & control