Toxicity of Five Herbs in Aconitum L. on Tetrahymena thermophila Based on Spectrum-effect Relationship / 中草药·英文版

Objective: To explore the active components with toxic effects in five Aconitum L. herbal medicines on Tetrahymena thermophila. Methods: The fingerprints of five Aconitum L. herbal medicines were established by ultra-high performance liquid chromatography (UPLC) and the toxicity was evaluated by using a TAM Air Isothermal Calorimeter on Tetrahymena thermophila SB110. Results: By analyzing the spectrum-effect relationships between UPLC fingerprints and toxic effects, the active components which had the toxic effects were obtained. Conclusion: This work provides a general model of the combination of UPLC and microcalorimetry to study the spectrum-effect relationships of the five Aconitum L. herbal medicines, which could be used to evaluate the toxic effects and analyze the principal toxic components of the five Aconitum L. herbal medicines. On the whole, this result provides the experimental basis for the safe use of the five Aconitum L. herbal medicines in clinic. © 2014 Tianjin Press of Chinese Herbal Medicines.

Comparison of anti-bacterial activity of three types of di-O-caffeoylquinic acids in Lonicera japonica flowers based on microcalorimetry / 中国天然药物

The anti-bacterial activities of three types of di-O-caffeoylquinic acids (diCQAs) in Lonicera japonica flowers, a traditional Chinese medicine (TCM), on Bacillus shigae growth were investigated and compared by microcalorimetry. The three types of diCQAs were 3, 4-di-O-caffeoylquinic acid (3, 4-diCQA), 3, 5-di-O-caffeoylquinic acid (3, 5-diCQA), and 4, 5-di-O-caffeoylquinic acid (4, 5-diCQA). Some qualitative and quantitative information of the effects of the three diCQAs on metabolic power-time curves, growth rate constant k, maximum heat-output power Pm, and the generation time tG, total heat output Qt, and growth inhibitory ratio I of B. shigae were calculated. In accordance with a thermo-kinetic model, the corresponding quantitative relationships of k, Pm, Qt, I and c were established. Also, the half-inhibitory concentrations of the drugs (IC50) were obtained by quantitative analysis. Based on the quantity-activity relationships and the IC50 values, the sequence of inhibitory activity was 3, 5-diCQA > 4, 5-diCQA > 3, 4-diCQA. The results illustrate the possibility that the caffeoyl ester group at C-5 is the principal group that has a higher affinity for the bacterial cell, and that the intramolecular distance of the two caffeoyl ester groups also has an important influence on the anti-bacterial activities of the diCQAs.

Effects of Two Curcuminoids on Candida albicans / 中草药·英文版

Objective To investigate and compare the action of curcuminoids on the causal pathogens of Candida albicans growth.Methods The effects of curcumin (CUR) and demethoxycurcumin (DMC) on C.albicans growth were first investigated and compared by microcalorimetry coupled with multiple analytical methods.The quantitative thermo-kinetic parameters obtained from these curves were analyzed to show difference of the actions.Results By analyzing the main parameters screened from principal component analysis together with 50％ inhibiting concentration values,it was demonstrated that both CUR and DMC showed good antifungal activities and CUR was stronger.It was further concluded from structure-activity relationship that the existence of methoxy group might enhance lipophilicity of the mother nucleus,which made it easier for the molecular to enter into the cell membrane of fungi to inhibit its growth.Conclusion This study provides a new method for screening new antifungal agents with high efficacy and low toxicity.Meanwhile,it contributes to the application of curcuminoids as food additive,colorant,and drug.Microcalorimetry is real-time,online,and dynamic,and it could be used to characterize the subtle difference among the effects of synthetic and natural products on the vital process of fungi.

Biothermo-kinetic comparative study on Taohua anti-diarrhea decoction prepared by two different ways / 第二军医大学学报

Objective: To compare the bioactivities of Taohua anti-diarrhea granula prepared by two different methods based on biothermo-kinetics study. Methods: The coarse and fine powder preparations of Taohua decoction were prepared. Microcalorimetry was used to obtain the metabolic curves and biothermo-kinetic parameters of Escherichia coli (E. coli) growth after treated by the two preparations to evaluate their bioactivities. Results: The values of growth rate constant k and maximum heat-out power Pm declined with the concentration increase of the 2 preparations; meanwhile, the values of peak time of the highest peak tm and growth inhibitory ratio I increased with the concentration increase of the two preparations. The results showed that the growth of E. coli was inhibited and the inhibitory effect was strengthened with the concentration increase of the two preparations. The IC50 was 35.9 mg/ ml for the coarse powder preparation and 31.4 mg/ml for the fine powder preparation. Aggregate analysis of the metabolic curves and biothermo-kinetic parameters of E. coli indicated that the fine powder preparation of Toohua decoction had stronger inhibitory action against E. coli growth than the traditional coarse powder preparation. Conclusion: Microcalorimetry can be used to examine the bioactivity differences of the fine and coarse preparations of Taohua decoction. Superfine comminution may increase the inhibitory action of Taohua decoction.

Determination of optimal glucose concentration for microcalorimetric metabolic evaluation of equine spermatozoa

The heat conduction microcalorimeter can be used to evaluate the metabolic rates of the sperm cell. Two ejaculates of four stallions were cooled to +5ºC and checked for sperm motility (bright field microscopy), viability (eosin 3 percent), functional membrane integrity (hyposmotic swelling test), and heat production (microcalorimetry). Glucose and sperm cell concentrations were determined in order to measure the heat outputs resulting from sperm metabolism. Sperm viability, membrane integrity and sperm motility did not differ among the different glucose concentrations tested. Nevertheless, the highest heat output detected by the microcalorimeter was obtained with 6 mM glucose and 10(8) spermatozoa/mL. Since conduction microcalorimetry offered additional information on equine sperm metabolism, it could be used as a method to study equine semen preservation.

O microcalorímetro de condução pode ser usado para avaliar as taxas metabólicas do espermatozóide eqüino. Dois ejaculados de quatro garanhões foram avaliados quanto à motilidade progressiva pela microscopia, viabilidade espermática (eosina 3 por cento), integridade funcional da membrana (teste hiposmótico) e produção de calor (microcalorimetria). Concentrações ótimas de glicose e de células espermáticas foram determinadas, para mensurar o calor liberado resultante do metabolismo espermático em relação à capacidade de detecção do calor pelo microcalorímetro. Não foi observada diferença da motilidade, viabilidade e integridade funcional de membrana espermática quando adicionada glicose nas três concentrações estudadas. No entanto a avaliação por microcalorimetria ressaltou um maior fluxo de calor a uma concentração de 6 mM de glicose e uma concentração espermática de 10(8) espermatozóides/mL. Portanto, a técnica de microcalorimetria oferece informações adicionais sobre o metabolismo tornando-se uma ferramenta importante no estudo do processo de preservação do sêmen eqüino.

Biothermo-kinetic comparative study on Taohua anti-diarrhea decoction prepared by two different ways / 第二军医大学学报

Objective:To compare the bioactivities of Taohua anti-diarrhea granula prepared by two different methods based on biothermo-kinetics study.Methods:The coarse and fine powder preparations of Taohua decoction were prepared.Microcalorimetry was used to obtain the metabolic curves and biothermo-kinetic parameters of Escherichia coli(E.coli)growth after treated by the two preparations to evaluate their bioactivities.Results:The values of growth rate constant k and maximum heat-out power Pm declined with the concentration increase of the 2 preparations;meanwhile,the values of peak time of the highest peak tm and growth inhibitory ratio I increased with the concentration increase of the two preparations.The results showed that the growth of E.coli was inhibited and the inhibitory effect was strengthened with the concentration increase of the two preparations.The IC50 was 35.9 mg/ml for the coarse powder preparation and 31.4 mg/ml for the fine powder preparation.Aggregate analysis of the metabolic curves and biothermo-kinetic parameters of E.coli indicated that the fine powder preparation of Taohua decoction had stronger inhibitory action against E.coli growth than the traditional coarse powder preparation.Conclusion:Microcalorimetry can be used to examine the bioactivity differences of the fine and coarse preparations of Taohua decoction.Superfine comminution may increase the inhibitory action of Taohua decoction.

Biothermodynamic study on four therapeutic features of TCM Ⅱ Comparison of therapeutic features of Folium ginseng and Flos ginseng by microcalorimetry / 中草药

Object To demonstrate the naked truth of four therapeutic features of TCM (cold, hot, warm and cool) from biophysical and biochemical point of view. Methods Growth thermogenesis curves of Escherichia coli were determined under different conditions by microcalorimetry to give biothermodynamic parameters, such as multiplication constant (k), median inhibitory concentration (IC 50 ), and enthalpy (?H). Differences between folia ginseng and flos ginseng were comprehensively compared with reference to classical Chinese literatures on material medica. Results The bacteriostatic curve of both drugs were basically similar. With increasing concentration of decoctions of both drugs, the lag phase was delayed and the peaks shifted to the right. While the difference of ?H was stable, which decreases with the increasing concentration of Folium ginseng, but increases with increasing concentration of Flos ginseng. Conclusion Microcalorimetry is not only a new effective method to describe the therapeutic features of TCM, but also could be used as a tool for the screening of active TCM.

Microcalorimetric studies of drug property differences during combination of Rhizoma Coptidis with Fructus Evodiae after separated decoction / 中草药

Transzuojin Pill.Conclusion Microcalorimetry can be used to investigate the drug property differences during combination of Rhizoma Coptidis with Fructus Evodiae after separated decoction.

Biothermodynamic characteristics of Radix Isatis by microcalorimetry / 中草药

Objective To establish the characteristic biothermokinetic methods in different extract fractions of Radix Isatis using Escherichia coli as model bacteria under biothermodynamics. MethodsMicrocalorimetry was used to obtain the characteristic metabolic growth power-time curves and biothermodynamic parameters of bacteria affected by different extract fractions of Radix Isatis, and evaluate the differences among the different extract fractions of Radix Isatis. Results Different extracting fractions of Radix Isatis could inhibit or promote the growth and metabolism of E. coli in different levels. Water-extract fractions and residues could promote its growth while organic solvent extract fractions did the opposite. Furthermore, with the decline of the solvent polarity, the inhibiting rate of organic solvent extract fraction was decreased and the generation time of bacteria was prolonged. There were steady and distinct differences among the different extract fractions in the characteristic metabolic growth power-time curves, such as the maximum power value's decrease and peak time's delay of water-extract fraction and residue, the specific power enhancement in later stage of organic solvent extract fraction. ConclusionMicrocalorimetry is a new and useful mean for the study on the biothermodynamic parameters and characteristics of Radix Isatis which can be helpful to investigate the other models using microcalorimetry.

Quality evaluation of Rhizoma Coptidis in different growing years by microcalorimetry / 中草药

Objective To establish a set of methods of Chinese materia medica quality evaluation based on biothermodynamics.Methods Using microcalorimetry,the thermal power of Escherichia coli meta-bolism affected by Rhizoma Coptidis in different growing years was measured.According to the thermokinetic model,the relationship of the thermokinetic parameters,caloric bioactivity and chemical constituent was analyzed.Results There were obvious difference in the caloric active fingerprints of E.coli metabolism affected by Rhizoma Coptidis in different growing years,which presented significant finger character.Compared with the normal groups,the metabolism of E.coli was inhibited in different levels by Rhizoma Coptidis in different growing periods,the multiplication rate constants and heat output were decreased,and the generation time was prolonged.Especially,Rhizoma Coptidis under four years' growing period with the highest content of total alkaloids showed a significant inhibitory effect on E.coli.Conclusion There are evident correlation among the thermokinetic parameters of E.coli metabolism affected by Rhizoma Coptidis in different growing years,the caloric bioactivity,and chemical composition.The thermokinetic parameters can indirectly reflect caloric bioactivity of Rhizoma Coptidis.As the method of biothermodynamics is on line,microamount,high throughout screening,and universality.The microcalorimetry is considered to be a useful mean for Chinese materia medica quality evaluation.

Biothermokinetic studies on four properties of traditional Chinese materia medica——Comparison of different preparation properties of Coptidis Rhizoma by microcalorimetry / 中草药

Object To probe into the objectivity and authenticity of four properties (cold, heat, warm, and cool) of raw Coptidis Rhizoma (RCR) and their preparations from biophysics and biochemistry. Methods Microcalorimetry was used to obtain the metabolic growth power-time curve of bacteria affected by the total alkaloid in different preparations of RCR and biothermokinetic parameters. Combined with the records of ancient herbal literatures, the influence of properties by different preparations to RCR were synthetically evaluated. Results All the effective total alkaloid in different preparations of RCR can restrain the Escherichia coli growth and metabolism in different level. Drugs, such as Coptidis Rhizoma Stir-fried with ginger juice (CRGJ), Coptidis Rhizoma stir-fried with wine (CRW), and Coptidis Rhizoma stir-fried with Fructus Evodiae (CRFE), with a little Warm Property can decrease the multiplication rate constants of E. coli index and increase heat output in growth metablism remarkably, while the drugs, such as RCR, Coptidis Rhizoma stir-fried with vinegar (CRV), and Coptidis Rhizoma stir-fried with gallbladder juice (CRGBJ), with a little Cold Property can decrease the multiplication rate constants and increase heat output a little. There was a stable difference between them. Conclusion Microcalorimetry is a new and useful mean for the study of the properties of tradition Chinese medicine.