[Methods for traditional Chinese medicine syndrome-based efficacy evaluation: a review].

Traditional Chinese medicine(TCM) syndrome-based efficacy is an evaluation index which is unique to TCM and can reflect the advantages of TCM. The development of the methods and measurement tools for evaluating TCM syndrome-based efficacy can provide objective and quantitative evidence for the clinical efficacy evaluation of TCM and the development of new Chinese medicine preparations, being the exploration direction of innovative methods and technologies for evaluating TCM efficacy. The conventional evaluation methods are subjective and limited to the mitigation of symptoms and the improvement of physical signs, which make it difficult to form a unified evaluation standard. In addition, the evaluation methods lack unity, objectivity, and quantitative research. The scientific connotation, evaluation ideas and methods, and key technologies of the evaluation for the therapeutic effect on syndromes remain unclear, which leads to diverse evaluation modes, methods, and indexes. The syndrome-based efficacy scale provides a new idea for the objective quantification and standardization of TCM syndromes. This review systematically summarizes the methods and problems, introduces the research progress in the evaluation scales, and puts forward some thoughts on the characteristics of TCM syndrome-based efficacy evaluation, aiming to provide insights for the research in this field.

[Preparation and Evaluation of Intranasal in situ Gel of Bupleuri Radix Volatile Oil and Baicalin].

OBJECTIVE: To prepare and evaluate a new formulation of thermosensitive and ion-sensitive in situ gel for nasal administration, using the volatile oil of Bupleuri radix and baicalin, the effective component extracted from Scutellariae radix . METHODS: Formulation of in situ nasal gel of Bupleuri radix volatile oil and baicalin was prepared by using poloxamer 407 and deacetylated gellan gum as the gel base, 10% pharmasolve and 2% polysorbate 80 as the solubilizer, and 0.8% triethanolamine as the pH regulator. The physical appearance, phase transition temperature, and baicalin release performance of the prepared gel were examined. The pharmacodynamic evaluation was done with the rat fever model developed with dry yeast and the mouse auricle swelling inflammation model. RESULTS: The phase transition temperature of the gel was optimized to be 36 ℃. The release of baicalin from the gel showed obvious features of sustained release, which accorded well the zero-order kinetics equation. The results of experiments with the rat dry yeast fever model and the mouse xylene auricle swelling inflammation model showed that the gel had significant antipyretic and anti-inflammatory effects that were significantly better than those of the groups treated with the blank gel base and the Bupleuri radix and Scutellariae radix granule. Results from the cilia toxicity test showed that the gel did not have obvious toxic effect on toad palate mucosal cilia. CONCLUSION: The in situ nasal gel of Bupleuri radix volatile oil and baicalin prepared in the study had a rapid onset time, high efficiency, and prolonged release of active ingredients, thus showing promises for further applicational development.

Astragaloside IV inhibits adriamycin-induced cardiac ferroptosis by enhancing Nrf2 signaling.

Astragaloside IV (AsIV), an active ingredient isolated from traditional Chinese medicine astragalus membranaceus, is beneficial to cardiovascular health. This study aimed to characterize the functional role of AsIV against adriamycin (ADR)-induced cardiomyopathy. Here, healthy rats were treated with ADR and/or AsIV for 35 days. We found that AsIV protected the rats against ADR-induced cardiomyopathy characterized by myocardial fibrosis and cardiac dysfunction. Meanwhile, ADR increased type I and III collagens, TGF-ß, NOX2, and NOX4 expression and SMAD2/3 activity in the left ventricles of rats, while those effects were countered by AsIV through suppressing oxidative stress. Moreover, ADR was found to promote cardiac ferroptosis, whereas administration of AsIV attenuated the process via activating Nrf2 signaling pathway and the subsequent GPx4 expression increasing. These results suggest that AsIV might play a protective role against ADR-induced myocardial fibrosis, which may partly attribute to its anti-ferroptotic action by enhancing Nrf2 signaling.

Effectiveness and Safety of the Combination of the Traditional Chinese Medicine Prescription Jade Screen and Desloratadine in the Treatment of Chronic Urticaria: A Systematic Review and Meta-Analysis of Randomized Controlled Trials.

OBJECTIVE: The aim of this study is to systematically evaluate the clinical efficacy and safety of the traditional Chinese medicine prescription Jade Screen combined with desloratadine in the treatment of chronic urticaria. METHODS: Two researchers independently conducted literature searches. The extracted data were analyzed using Rev Man 5.2.3 software. The established retrieval time range of the various databases was up to 15 March, 2017. RESULTS: Sixteen randomized controlled trials were included in this study. The results of the meta-analysis showed that the total effective rate of using Jade Screen and desloratadine in combination to treat chronic urticaria was higher than that with desloratadine alone (P < 0.00001), while its recurrence rate (P < 0.00001) and symptom score (P = 0.006) were both significantly lower than the latter. The rate of adverse reaction in the combination group was lower than that when orally taking desloratadine alone (P = 0.74), and the serum level of total IgE in the combination group was lower than that when orally taking desloratadine alone (P = 0.82); however, the results of the rate of adverse reaction and the serum level of total IgE were insignificant. CONCLUSION: Using Jade Screen and desloratadine together to treat chronic urticaria gains a better clinical effect than using desloratadine alone.

[Effect of combination of gastrodia and uncaria on pharmacokinetics of gastrodin and rhynchophylline].

To investigate the effect of the combination of gastrodia and uncaria on the pharmacokinetics of gastrodin and rhynchophylline, and determine their pharmacokinetic parameters after administration of the combination of gastrodia and uncaria at the ratio of 12∶9. Compared with uncaria group or gastrodia group, Cmax and AUC of both gastrodin and rhynchophylline were significantly increased, and tmax was retroceded by 1.5 h for rhynchophylline and 0.25 h for gastrodin. The change of tmax resulted in a 1.25 h difference in the peak time between gastrodin and rhynchophylline , which was the same between them. Uncaria shows a more effect in suppressing hyperactive Yang, while gastrodia has a balancing effect by nourishing Yin and suppressing hyperactive Yang. As a result, gastrodia could exert the effect in nourishing Yin and suppressing effect of uncaria, which could avoid the deficiency of Yang affecting Yin due to mono-treatment of uncaria. On one hand, the enhanced AUC and Cmax of gastrodin could increase the average plasma drug concentration of gastrodin, and remedy the losing effect of uncaria at the early stage; On the other hand, the increased AUC and Cmax of rhynchophylline could make up the quick elimination of gastrodia in vivo at the late stage. Their combination could lead to an increased anti-hypertensive effect with the balance of Yin and Yang. They showed unique advantages compared with simple dosage increase of western medicines. The results were consistent with the principle of TCM treatment for the hypertension due to hyperactivity of the liver Yang. In short, this study gives a good pharmacokinetic explanation of the balance of Yin and Yang and TCM treatment for both symptoms and root cause.

Design, synthesis, antifungal, and antioxidant activities of (E)-6-((2-phenylhydrazono)methyl)quinoxaline derivatives.

Different substituted phenylhydrazone groups were linked to the quinoxaline scaffold to provide 26 compounds (6a-6z). Their structures were confirmed by (1)H and (13)C NMR, MS, elemental analysis, and X-ray single-crystal diffraction. The antifungal activities of these compounds against Rhizoctonia solani were evaluated in vitro. Compound 6p is the most promising one among all the tested compounds with an EC50 of 0.16 µg·mL(-1), more potent than the coassayed positive control fungicide carbendazim (EC50: 1.42 µg·mL(-1)). In addition, these compounds were subjected to antioxidant assay by employing diphenylpicrylhydrazyl (DPPH) and mice microsome lipid peroxidation (LPO) methods. Most of these compounds are potent antioxidants. The strongest compounds are 6e (EC50: 7.60 µg·mL(-1), DPPH) and 6a (EC50: 0.96 µg·mL(-1), LPO), comparative to or more potent than the positive control Trolox [EC50: 5.90 µg·mL(-1) (DPPH) and 18.23 µg·mL(-1) (LPO)]. The structure and activity relationships were also discussed.

Two new furostanol saponins from the fibrous root of Ophiopogon japonicus.

Two new furostanol saponins ophiopogonins J (1) and K (2) were isolated from the fibrous roots of Ophiopogon japonicus. The structures of 1 and 2 were established as (25R)-26-O-[(ß-D-glucopyranosyl-(1 --> 2)-ß-D-glucopyranosyl)]-14-hydroxy-furost-5,20(22)-diene 3-O-[α-L-rhamnopyranosyl-(1 --> 2)]-ß-D-glucopyranoside (1), and (25R)-26-O-[(ß-D-glucopyranosyl-(1 --> 2)-ß-D-glucopyranosyl)]-furost-5,20(22)-diene 3-O-α-L-rhamnopyranosyl-(1 --> 2)[(ß-D-xylopyranosyl-(1 --> 4)-ß-D-glucopyranoside)] (2) on the basis of spectroscopic means including HRESIMS, 1D, and 2D NMR experiments.

[Intestinal lymphatic transport of breviscapine orally administered in rat].

Double cannulation model of conscious rat allowing simultaneous collection of mesenteric lymph and jugular venous blood was established to investigate the intestinal lymphatic transport of breviscapine orally administered in rat. The concentrations of breviscapine in plasma and lymph were determined by HPLC. The pharmacokinetics of breviscapine after oral and intravenous administration was evaluated in the conscious rat model. It was observed that scutellarin distributed from blood circulation to lymphatic system after intravenous injection. The cumulative lymphatic transport amount within 12 h was (2.78 +/- 0.25) microg, equivalent to 0.0792% of intravenous dose. After oral administration of scutellarin to double-cannulation rats, the cumulative lymphatic transport amount within 12 h was (0.92 +/- 0.08) microg, equal to 0.0083% of oral dose. The absolute bioavailability of breviscapine orally administered to double-cannulation rats was 4.91%, indicating that scutellarin was mainly absorbed into the bloodstream through the portal vein. Lymphatic transport of scutellarin appears to reflect high affinity for the lymph lipoproteins to chylomicron. This study provided a biopharmaceutics basis for developing oral lipid delivery system for the promotion of intestinal lymphatic transport to improve oral bioavailability of breviscapine.

Bioavailability of salvianolic acid B and effect on blood viscosities after oral administration of salvianolic acids in beagle dogs.

Salvianolic acid B (SalB) is an active component isolated from Chinese herbal medicine Salvia miltiorrhiza. The aim of this study was to investigate the extent of absolute oral bioavailability (F) of SalB in beagle dogs and the effect on blood viscosity after intravenous and oral administration of Salvianolic acids (SAs). A gradient elution HPLC method was developed and validated to determine the concentration of SalB and its three possible metabolites in plasma. After SAs (180 mg/kg, p.o.; 9 mg/kg, i.v.) were given, the AUCs of SalB were 1680 +/- 670 and 7840 +/- 1140 ng/mL.h, respectively. The F of SalB in dogs was calculated to be only 1.07 +/- 0.43%. The blood viscosity was remarkably decreased after a single intravenous injection of SAs (9 mg/kg). However, no significant change of blood viscosity was observed after a single oral administration of SAs (180 mg/kg). The results suggested that the F of SalB was extremely low and single oral administrated SAs had no effect on ameliorating blood viscosity in beagle dogs.

Structure revision and synthesis of a novel labdane diterpenoid from Zingiber ottensii.

The structure of ottensinin, a recently reported constituent of the medicinal plant Zingiber ottensii, was revised by re-evaluation of available NMR data from alpha-ylidenebutenolide 1 to gamma-pyrone 2, whose rearranged labdane skeleton is unprecedented. Structure 2 was proven by synthesis from (+)-sclareolide (nine steps, 27% overall yield) and was further validated by X-ray diffraction analysis of our synthetic sample. A plausible biosynthesis of 2 is proposed.

[Optimal extraction of Dingxiang jiangqi granules].

OBJECTIVE: To screen and optimize the extraction of Dingxiangjiangqi granules. METHOD: The extraction route was screened by using pharmacodynamic experiment and the extraction conditions were optimized by orthogonal design and taking extract yield, content of naringin and tetrahydropalmatine as indexes. RESULT: The pharmacodynamic result showed that aqueous extract had the best effect to cure the esophagitis of rats and the optimized extraction technique was adding 12 times water, extracting 0. 5 hour for 3 times. CONCLUSION: The optimum extraction was simple, reasonable, stable and useful for further development.

[Studies on dissolution rate in vitro of silymarin dropping pill].

OBJECTIVE: To test the dissolution rate of silymarin dropping pill as well as to be compared with other three commercial products of the silymarin. METHOD: By UV spectrophotometry, we studied the dissolution conditions of silymarin dropping pill and compared its dissolution rate with Yiganling tablets (film-coating, sugar-coating) and Legalon capsule which are available in the market. RESULT: The dissolution parameters T50 and Td of silymarin dropping pill, Yiganling tablet (film-coating), Yiganling tablet (sugar-coating) and Legalon capsule are 6.78, 9.85 min, 51.01, 73.78 min, 74.35, 86.97 min and 53.10, 72.65 min. CONCLUSION: The dissolution rate of silymarin dropping pill is superior to that of two kinds of Yiganling tablets and Legalon capsule.

[Alumina-supported catalysts for the catalytic purification of lean-burn automobile exhaust].

Catalytic properties of Ag/Al2O3, In/Al2O3, Sn/Al2O3, Co/Al2O3, Pt/Al2O3 and a two-stage catalyst composed of Ag/Al2O3 and Pt/Al2O3 were investigated for the selective reduction of NO by C3H6 or C2H5OH in excess oxygen. The Ag/Al2O3 showed the highest NO reduction activity among the catalysts studied. A substantial amount of CO was formed over alumina-based transient metal oxides. HC and CO oxidations over Pt/Al2O3 occurred in relatively low temperatures, compared with the other catalysts. The sequential use of Ag/Al2O3 and Pt/Al2O3 was effective to broaden the temperature window for the reduction of NO, to improve oxidation of HC and CO and to inhibit the formation of N2O and CH3CHO.