Determination and effect of five alkaloids from extracts of Piper longum on rats with experimental myocardial ischemia induced by injection of pituitrin / 药学实践杂志

Objective To determine the content of five alkaloids from extracts of Piper longum and test the pharmacodynamic effect of them on rats with experimental myocardial ischemia induced by injection of pituitrin. Methods The content of five alkaloids was determined simultaneously by HPLC. The experimental myocardial ischemia in rats was induced by injection of pituitrin, and the absolute value of T wave change and change of heart rate before and after model establishment were chosen to be the observation index. The effects of large, medium and small dose groups were evaluated. Results Three batches of samples were analyzed, with the contents of piperine for 56.1%, 49.7%, 51.6%; N-isobutyl-(2E,4E)-octadecatrienamide for 4.5%, 4.2%, 4.3%; guineensine for 0.46%, 0.38%, 0.40%; piplartine for 1.73%, 1.67%, 1.70% and piperamide for 0.55%, 0.46%, 0.49%, respectively. All dose groups from extracts of piper longum had significantly reduced the absolute value of T wave and almost have no effect on the change of heart rate, except the high dose group showed the effect of reducing heart rate at some time . Conclusion The HPLC method was suitable for the simultaneous determination of five alkaloids from extracts of Piper longum. It was shown that extracts of Piper longum had good bioactivity in anti-myocardial ischemia.

Two new isoquinoline alkaloids from Corydalis hendersonii / 中国中药杂志

Corydalis hendersonii(CH) is a Tibetan folk medicine with the functions of clearing heat, detoxifying, cooling blood, checking diarrhea, and lowering blood pressure. It is often used to treat high altitude polycythemia, vasculitis, peptic ulcer, and diarrhea. Nine compounds were separated from the ethanol extract of CH by silica gel, ODS, Sephadex LH-20 chromatography and semi-preparative HPLC. Their structures were identified as hendersine H(1),hendersine I(2), dehydrocheilanthifoline(3), protopine(4), izmirine(5), 6,7-methylenedioxy-1(2H)-isoquinolinone(6), icariside D_2(7), ethyl 4-(β-D-glucopyranosyloxy)-3-methoxybenzoate(8), 3-hydroxy-4-methoxybenzoic acid(9), respectively, by the spectroscopic data analysis and comparison with those in the literature. Among them, compounds 1 and 2 are new isoquinoline alkaloids, and compounds 7-9 are reported the first time for Corydalis. The hypoglycemic model of H9c2 cardiomyocytes and the inflammatory model of H9c2 cardiomyocytes induced by conditional supernatant were employed to determine the activities of the above compounds. The results showed that 20 μmol·L~(-1) compound 1 had a protective effect on H9c2 cardiomyocytes and 10 μmol·L~(-1) compounds 4 and 5 inhibited H9c2 cardiomyocyte inflammation induced by conditional supernatant.

Virtual screening of components of safflower against myocardial ischemia based on molecular docking technology / 中国中药杂志

The screening of active components of traditional Chinese medicine has always been the focus and difficulty in modern research of Chinese medicine preparations. With the continuous development of life science, omics and computer technology, the virtual screening technology for active components of traditional Chinese medicine has gradually come into people's vision. Molecular docking technology is an important method for screening active components of traditional Chinese medicine. It not only has a short cycle and strong operability, but also avoids the disadvantage of poor stability in pharmacological experiments. Safflower extract can effectively alleviate the symptoms of myocardial ischemia, but its active components are not clear. In this study, with use of the molecular docking technology, the active components in safflower against myocardial ischemic were virtually screened based on the screening method of active components. Forty-six chemical components and 5 target proteins which showed high correlation with myocardial ischemia were obtained from the existing database and related literature reports. With the molecules of three commercially available drugs diltiazem, trimetazidine and verapamil as positive control molecules, the compomnents were docked with 5 target proteins. Active components were screened according to docking scores and interactions between molecules and targets, and then the active ingredients can be inferred. Fourteen chemical components were screened to have the most potential anti-myocardial ischemic activity, and all of them were flavonoids. Therefore, it can be inferred that the flavonoid components are the most potential anti-myocardial ischemic components in safflower. The screening of active anti-myocardial ischemia components in safflower was completed in this study, laying the foundation for subsequent researches.

Screening of active anti-myocardial ischemia components of Panax notoginseng based on molecular docking technology / 中国中药杂志

The molecular docking technology was used in this study to virtually screen the active anti-myocardial ischemic components in Panax notoginseng, clarify the compositions of the anti-myocardial ischemic component unit and the basis for pharmacological activity of P. notoginseng, and provide the basis for the acquisition of the component raw materials and the formulation design before the preparations. One hundred and nineteen compounds in P. notoginseng were collected by searching TCMSP to establish the ligand database, and TNF, IL1 B, NFKBIA, and NOS3 which were related with myocardial ischemia were selected to create the receptor database. Then Discovery Studio software LibDock module was used to dock the ligands and receptors, with the approved small-molecule drugs which were related to targets or the treatment of myocardial ischemia disease in the DrugBank as the reference, and the average scores of approved small-molecule drugs were set as the threshold. A total of 13 compounds with a score above the threshold and in the top ranking were virtually screened. The study showed that all the 13 components screened out were saponins, which constituted the main component unit of the anti-myocardial ischemic activity of P. notoginseng, namely the P. notoginseng saponin components. After the comparative analysis of the main active residues of the approved commercial drugs and P. notoginseng saponin components on each target, the similarity of their effects suggested that the P. notoginseng saponin components may have the same anti-myocardial ischemic efficacy as clinical drugs. The components of P. notoginseng which exerted anti-myocardial ischemic activity were mainly the saponin components. The preliminary screening of the active anti-myocardial ischemic components of P. notoginseng had been completed, which provided a certain reference for the development of anti-myocardial ischemic Chinese medicine component preparations.

Isolation and Elucidation of a Novel Isoquinoline Alkaloid from Corydalis hendersonii / 中国实验方剂学杂志

As part of systematic research of Corydalis hendersonii,a typical traditional Tibetan herbal medicine with clearing heat,relieving pain,and lowering blood pressure effects,a novel isoquinoline alkaloid,named hendersine G was isolated from the ethanol extract of the whole plant by various chromatographic techniques,including silica gel column,reverse phase column (ODS),Sephadex LH-20,and semi-preparative HPLC.Its structure was elucidated by MS,NMR and other spectroscopic data analysis.Hendersine G can be regarded as a condensation product of a tetrahydroberberine and a succinic acid,however,its absolute configuration has not been determined due to its structural complexity and less obtained amount.This present study provides an inspiration for further exploration of novel molecules from C.hendersonii.

Spectrum-activity relationship of trichosanthis fructus and trichosanthis fructus strip pieces for rat myocardial ischemia-reperfusion injury / 中国中药杂志

To investigate the spectrum-activity relationship of Trichosanthis Fructus and Trichosanthis Fructus strip pieces for rat myocardial ischemia-reperfusion injury. HPLC fingerprints of Trichosanthis Fructus and Trichosanthis Fructus strip pieces were established, and the values of creatinekinase-MB (CK-MB), myoglobin (MYO) and cardiac troponin-T (cTNT) in 3 dose groups (2.25, 13.5, 27.0 g·kg⁻¹, equivalent to the crude herb g·kg⁻¹) of Trichosanthis Fructus and Trichosanthis Fructus strip pieces with myocardial ischemia-reperfusion injury in rats were measured, and the grey relational analysis was used to study the spectrum-activity relationship of Trichosanthis Fructus and Trichosanthis Fructus strip pieces for rat myocardial ischemia-reperfusion injury. With the dosage increase from 2.25 g·kg⁻¹ to 27.0 g·kg⁻¹, the correlation degree of spectrum-activity relationship of Trichosanthis Fructus and Trichosanthis Fructus strip pieces was also enhanced, but the change trend was different between these two groups. According to the frequency of the top 10 peaks in the correlation degree, peak 17, 14, 16, 19, 32, 12, 26, 30, 4, 6 and 2 were the basic effective substances group of Trichosanthis Fructus, peak 6,14,12,32,30,4 and 6 were the basic effective substances group of Trichosanthis Fructus strip pieces. Peak 6, 14, 12, 32, 30, 4 and 26 in fingerprints of Trichosanthis Fructus and Trichosanthis Fructus strip pieces were the main common pharmacodynamic substance base, among them, peak 6 was 5-hydroxymethyl furfural, peak 14 was vanillic acid and the peak 28 was rutin, but the correlation degree with the efficacy was different. The effect of Trichosanthis Fructus and Trichosanthis Fructus strip pieces on rat myocardial ischemia-reperfusion injury was due to the synergistic effect of the effective substance groups related to the dosage. The essential pharmacodynamic substance groups of Trichosanthis Fructus and Trichosanthis Fructus strip pieces were different, but they shared a common active ingredient group.

Drug Quality Representation Analysis of Preparations of Aurea Helianthus based on Anti-myocardial Ischemia Effect / 世界科学技术-中医药现代化

This study was aimed to select the best preparation form of Aurea Helianthus in order to provide a scientific basis for research and development of anti-myocardial ischemia drugs.The content of effective index components of preparation of Aurea Helianthus was detected using HPLC-PDA.Acute myocardial ischemia rat model introduced by injecting pituitrin was used to investigate the effect of anti-myocardial ischemia.The quality of preparation from Aurea Helianthus was characterized based on pharmacy and efficacy.And the characterized results were given correlation analysis.The results showed that the HPLC method for quantitative determination was verified by methodology.The average recoveries were in the range of 97.04％-102.44％.All three preparations of Aurea Helianthus had the efficacy of anti-myocardial ischemia in varying degrees.The enrichment had the highest effect with lowest extraction rate and the lowest dosage,which was the best form in medicinal-preparation application of Aurea Helianthus.It was concluded that the content of related drug components was higher with unique proportion in enrichment of Aurea Helianthus which was prepared based on drug system proved a high quality medicine.Therefore,the key to the improvement of efficacy was to explore the fittest proportion and improve the content of related pharmaceutical ingredients pertinently according to drug system.

Effects of ento-i plastic on anti-anoxia and myocardial ischemia in mice: A preliminary study / 国际药学研究杂志

Objective To investigate the effects of Ento-I plastic on anoxia and myocardial ischemia. Methods The effect of Ento-I plastic on anoxia in mice was evaluated by testing mice’s anti-anoxia time under ordinary pressure, mice’s gasp time and the number of mouth breathing under ischemia-anoxia, and mice’s survival time after sodium nitrite poisoning. Animals were divided into normal saline(NS)group, matrix group, aspirin(ASP)group and Ento-I plastic(9.125, 18.25 and 37.5 mg/kg)groups. The effect of Ento-oon myocardial ischemia in mice was preliminarily evaluated using the animal model of acute myocardial ischemia induced by the subcutaneous injection of isoprenaline(the animals were divided into NS group, matrix group, compound danshen dropping pill(DSP)group and Ento-I plastic(5, 10 and 20 mg/kg)groups. In these experiments, NS group, ASP group and DSP group were administered intragastrically, while the matrix group and Ento-I plastic groups were administered by daubing on both sides of the temple. Results There was no significant difference in all indexes between the NS group and the matrix group in all four experiments. Compared with NS, the middle dosage of Ento-I plastic(18.25 mg/kg)could obviously prolong the anoxia tolerance time to (50.87±11.90)min under ordinary pressure, survival time to(14.15±4.61)min after sodium nitrite poisoning and the gasp time to (27.90±4.79)s after decapitation, with the statistically significant difference(P<0.01). In anti-myocardial ischemia experiment, both the myocardial superoxide dismutase(SOD)activity and malondialdehyde(MDA)content were significantly decreased in the high dosage Ento-I(20 mg/kg)and DSP groups than in the NS group(P<0.01). The pathological examination of the ischemic of myocardium itself showed that Ento-I plastic could significantly reduce ischemic myocardial injury and enhance the anti-ischemic effect of myocardium itself. Conclusion The Ento-I plastic could obviously strengthen the anti-anoxic and anti-ischemic ability of mice.

Research progress on C-glycosylflavones for protection of myocardial ischemia / 中草药

With the improvement of the public's recognition to the efficacy of total flavonoid extract from Chinese materia medica, wherein the C-glycosylflavones contained have been found by more and more researchers. The role of C-glycosylflavones to protect the cardiovascular disease is becoming more evident. The recent isolation and identification of C-glycosylflavones with the pharmacological activity about anti-oxidant and protecting myocardial ischemia injury and the possible mechanisms of anti-myocardial ischemia are reviewed in this article, so as to provide the information and evidence for the further research and development of C-glycosylflavones.

Active components of Polysaccharide of Ophiopogon Japonicus on acute myocardial ischemia / 中成药

AIM: To choose the anti myocardial ischemic ingredients from polysaccharide of Ophiopogon Japonicus(PO), then to confirm their effects. METHODS: According to molecular weight, PO was separated to three portions by using ultrafiltration technique. The effects of each separated portion on myocardial ischemia induced by isoproterenol were studied. Then the effects of PO active portions (POAP) on the convulsion of coronary artery induced by pituitrin and acute myocardial ischemia caused by the ligation of coronary artery were further studied in rats. RESULTS: POAP could resist the elevation of Tand S T phase induced by pituitrin in rats, remarkably decrease the elevated S T phase and contents of CK and LDH in serum caused by the ligation of rat coronary artery. POAP also exerted some inhibition effects on the reduction of SOD and increase of MDA caused by myocardial ischemia. CONCLUSION: POAP can protect myocardial cells, inhibit the generation of free radicals, and scavenge the oxygen free radicals generated from myocardial ischemia.