benzofurans and tetramethylpyrazine

Cerebral ischemia is also known as ischemic stroke. In recent years, research on neuroprotection after ischemia has became a hot spot as stroke can result in symptoms of nerve damages such as hemiplegia, learning and memory disorders. The key factors that cause the death of cells include excitotoxicity, oxidative damage, nitrosative stress and inflammation. However, there is no effective preparation for the treatment of post-ischemic nerve defects at present, so it is urgent to find and develop effective drugs for the treatment of nerve damages after ischemia. Traditional Chinese medicine has advantages and potentials in the treatment of neurological diseases. Many scholars have carried out related researches on the active ingredients of traditional Chinese medicine and achieved some good results. In this context, the researches on the neuroprotective effects of traditional Chinese medicines such as tetramethylpyrazine, butylphthalide and total saponins of Panax notoginseng were reviewed. The author found that the neuroprotective researches of traditional Chinese medicine mostly focused on anti-apoptosis, anti-inflammatory and anti-oxidative stress, but those effects were not sounique to the nervous system. Furthermore, most ingredients of traditional Chinese medicine showed a poor water-soluble property. In view of the research status and existing problems of traditional Chinese medicine in nerve injury, the suggestions for the research and development of the potent neuroprotective agents were proposed in this study from the perspective of pharmacological mechanism research and preparation theory.

Topics: Benzofurans; Brain Ischemia; Cerebral Infarction; Drugs, Chinese Herbal; Humans; Medicine, Chinese Traditional; Neuroprotective Agents; Panax notoginseng; Pyrazines; Saponins

To investigate the effect of tetramethylpyrazine hydrochloride combined with butylphthalide on serum S100B, CRP, Hcy and NIHSS score in patients with acute cerebral infarction. 80 patients with acute cerebral infarction treated in our hospital from February 2019 to February 2021 were selected for retrospective analysis, and according to different treatment methods, the patients were equally divided into control group (conventional treatment) and experimental group (tetramethylpyrazine hydrochloride and butylphthalide). After treatment, the total effective rate of patients in the experimental group was significantly higher than that in the control group (P<0.05); the levels of serum S100B, CRP and Hcy, and NHISS scores in the two groups decreased, and the experimental group was significantly lower than the control group (P<0.05); the ADL scores of the two groups increased and the experimental group witnessed higher score (P<0.05); the number of patients in the experimental group with scores of 0-2 and 5 were significantly larger than that in the control group (P<0.05). The combination of tetramethylpyrazine hydrochloride and butylphthalide emanates a promising result in the treatment of patients with ACI. It reduces serum S100B, CRP and Hcy levels, protects nerve tissue, and improves nerve function, and thus merits clinical application.

Topics: Acute Disease; Benzofurans; Brain Ischemia; Cerebral Infarction; Humans; Pyrazines; Retrospective Studies; S100 Calcium Binding Protein beta Subunit; Stroke

It was previously reported that cytokines and neurotoxins released from activated inflammatory cells induced the loss of projecting dopaminergic neurons in the substantia nigra, which triggered the pathogenesis of PD. The present study investigated the effect of treatment with tetramethylpyrazine (TMP) on the central cytokine synthesis, striatal dopamine content and glutamatergic transmission, and behavioral performance in the rotarod task in mice injected with 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). Treatment with TMP significantly improved the behavioral performance in the rotarod task in mice injected with MPTP. It also decreased the upregulation of cytokines (tumor necrosis factor-α and interleukin-1β) in the substantia nigra and striatum in these modeled mice. Furthermore, treatment with TMP significantly improved the dopamine deficits and attenuated the upregulation of striatal basal glutamatergic strength in the striatum of mice injected with MPTP. These results indicated that TMP might serve as a novel approach for the treatment of patients with PD.

Topics: Analysis of Variance; Animals; Benzofurans; Corpus Striatum; Cytokines; Disease Models, Animal; Dopamine; Dose-Response Relationship, Drug; Excitatory Postsynaptic Potentials; In Vitro Techniques; Male; Mice; Neurons; Parkinsonian Disorders; Patch-Clamp Techniques; Postural Balance; Psychomotor Performance; Pyrazines; Quinolines; Vasodilator Agents

To develop a RP-HPLC method for the simultaneous determination of five components including ligustrazine, ferulic acid, butylphthalide, ligustilide and butene-NBP in Rhizoma Chuanxiong, a Chinese herbal medicine.. The chromatographic analysis was carried out by using a grace smart RP C18 column with the mobile phase consisted of acetonitrile and 0.1% phosphoric acid (volume fraction), which was in gradient elution. A DAD detector was used to detect the components. The peak area was chosen under their maximum absorption wavelength for different components, and quantitated by using the external standard method.. The calibration curves were linear within the range of 0.008 35-0.668, 0.020 6-1.648, 0.012 2-0.976 , 0.050 75-4.06, 0.015 7-1.256 microg for ligustrazine, ferulic acid, butylphthalide, ligustilide and butene-NBP, respectively. The average recoveries of the five components were 101.98%, 99.91%, 96.94%, 100.85% and 99.04%, respectively.. This method is simple, quick, reproducible, with high recovery, and has been successfully applied to the simultaneous determination of the five components in Rhizoma Chuanxiong. This method can be used to control the quality of Rhizoma Chuanxiong and its preparations.

Topics: 4-Butyrolactone; Benzofurans; Calibration; Chromatography, High Pressure Liquid; Coumaric Acids; Drugs, Chinese Herbal; Pyrazines

Apoptosis induced by high shear stress has been reported for the dysfunction of various vascular endothelial cells. We investigated the protective effects of tetramethylpyrazine (TMP) and salvianolic acid B (SAB) from Chinese medicine on the shear-induced early and late stages of apoptosis in cultured rat cerebral microvascular endothelial cells (rCMECs) under pathological high shear stress. Near-confluent cultures of rCMECs were pretreated with TMP or SAB and their combinational dosages, and exposed to high shear stress generated by a rheometer. Apoptotic death rate of rCMECs was assessed by immunofluorescence microscopy of Annexin V-FITC and propidium iodide (PI). We found that early and late stage apoptosis occurred at 3.0 Pa for a short duration of 450 sec but did not occur at 1.5 Pa. SAB inhibited the cells from apoptosis at concentrations from 10 microM to 20 microM in a dose-dependent manner, while effect of TMP at 0.37 mM and 0.73 mM did not significantly differ. Moreover, the combined use of TMP and SAB had synergistic anti-apoptotic effects (P<0.01). The results indicate that the anti-apoptotic effect of TMP and SAB on rheologically induced endothelial injury is likely involved in their efficacy.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Apoptosis; Benzofurans; Cells, Cultured; Cerebrovascular Circulation; Drugs, Chinese Herbal; Endothelium, Vascular; Hemorheology; Male; Microcirculation; Pyrazines; Rats; Rats, Sprague-Dawley; Stress, Mechanical

Tetramethylpyrazine (TMP) and salvianolic acid B (SAB) are effective ingredients of Rhizoma Ligustici chuanxiong Hort. and Radix Salviae miltiorrhizae Bge., accordingly. The inhibitive effects of TMP, SAB and their combination on shear-induced platelet aggregation (SIPA) were investigated in the present study. SD rats were used as blood donors to collect anticoagulated blood, the concentration of platelet-rich-plasma (PRP) was adjusted to 5 x 10(5) microl. HAAKE rheometer RS 600 with sensor C60/0.5 degrees was used as shear generator. Different doses of TMP and SAB and their combinations were added to the PRP. After constant shear of 15 Pa at 37 degrees C for 360 seconds, PRP was transferred to a platelet aggregometer and SIPA was determined by turbidity. SIPA was inhibited by TMP and SAB in a dose-dependent manner. SIPA was decreased from 48.6 +/- 4.6% of the control to 12.5 +/- 2.1% in the presence of TMP (1.46 mM) and SAB (10 microM) (P < 0.0001). In conclusion, TMP and SAB have additive effects on inhibiting platelet aggregation induced by high shear stress.

Topics: Animals; Benzofurans; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Drug Synergism; Drugs, Chinese Herbal; Hemorheology; Nephelometry and Turbidimetry; Platelet Aggregation; Platelet Aggregation Inhibitors; Pyrazines; Rats; Stress, Mechanical

Topics: Albuminuria; Animals; Benzofurans; beta 2-Microglobulin; Cyclosporine; Diabetes Mellitus, Experimental; Diabetic Nephropathies; Enzyme Inhibitors; Immunosuppressive Agents; Kidney; Organ Size; Pancreas Transplantation; Pyrazines; Rats; Rats, Wistar; Thromboxane A2; Thromboxane-A Synthase; Transplantation, Isogeneic