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Cornus officinalis and Dioscorea opposita are two traditional Chinese medicines widely used in China for treating diabetes mellitus and its complications, such as diabetic cardiomyopathy. Morroniside (Mor) of Cornus officinalis and diosgenin (Dio) of Dioscorea opposita formed an innovative formula named M + D. The aims of the present study were to investigate myocardial protective effect of M + D on diabetic cardiomyopathy (DCM) through the inhibition of expression levels of caspase-3 protein, and identify the advantage of M + D compared with Mor, Dio, and the positive drug metformin (Met). We detected cell viability, cell apoptosis, intracellular reactive oxygen species (ROS) levels, and the expression levels of Bcl-2, Bax, and caspase-3 protein in rat cardiomyocytes. In result, Mor, Dio, and M + D increased cell viability, inhibited cell apoptosis and decreased ROS levels. Additionally, the expression of Bax and Bcl-2 protein was modulated and the expression levels of caspase-3 protein were markedly decreased. Among the treatment groups, M + D produced the most prominent effects. In conclusion, our data showed for the first time that Mor, Dio, and M + D prevented high glucose (HG)-induced myocardial injury by reducing oxidative stress and apoptosis in rat cardiomyocytes. Among all the groups, M + D produced the strongest effect, while Mor and Dio produced weaker effects.

As for traditional Chinese medicine (TCM) prescription, what puzzled researchers most was how to select proper chemical markers to represent the whole pharmacological action system. In this paper, an integrated metabolomic method was presented for a systematic discovery of potential active components in Fangji Huangqi Tang (FHT), a well-known TCM prescription for nephrotic syndrome treatment, based on “correlations between chemical and metabolic profiles.” Firstly, a metabolomics study was carried out to select representative biomarkers of nephrotic syndrome. Then, after drug administration, the dynamic process of serum composition was investigated by the ultra-high performance liquid chromatography coupled with electrospray ionization–quadrupole–time of flight–mass spectrometry (UHPLC-ESI-Q-TOF-MS) technique to detect the prototypes and related metabolites of relative components from FHT. Pearson correlation analysis was finally used to find out the correlations between the endogenous metabolic spectrums and the chemical serum spectrums. As a result, 17 biomarkers for nephrotic syndrome indication were identified, and the main metabolic pathways of their concern included linoleic acid metabolism; cyanoamino acid metabolism; alpha-linolenic acid metabolism; glycine, serine, and threonine metabolism; arachidonic acid metabolism; and glycerophospholipid metabolism. Meanwhile, active components in FHT for nephrotic syndrome treatment were screened out, including (+)-tetrandrine demethylation, fenfangjine G hydrogenation, tetrandrine, N -methylfangchinoline, tetrandrine demethylation, fangchinoline, glycyrrhetic acid, astragaloside II alcohol dehydration, atractylenolide III demethylation + hydrogenation, atractylenolide III demethylation + hydrogenation, and licoricone- N -acetylcysteine conjugation. This study demonstrated a promising way to elucidate the active chemical material basis of TCM prescription.

Brucine was encapsulated into stealth liposomes using the ammonium sulfate gradient method to improve therapeutic index. Four brucine stealth liposomal formulations were prepared, which were made from different phosphatidylcholines (PCs) with different phase transition temperatures (T(m)). The PCs used were soy phosphatidylcholine (SPC), dipalmitoyl phosphatidylcholine (DPPC), hydrogenated soy phosphatidylcholine (HSPC), and distearoyl phosphatidylcholine (DSPC). The stabilities, pharmacokinetics, and toxicities of these liposomal formulations were evaluated and compared. Size, zeta potential, and entrapment efficiency of brucine-loaded stealth liposomes (BSL) were not influenced by PC composition. In vitro release studies revealed that drug release rate increased with decreased T(m) of PCs, especially with the presence of rat plasma. After intravenous administration, the area under the curve (AUC) values of BSL-SPC, BSL-DPPC, BSL-HSPC, and BSL-DSPC in plasma were 7.71, 9.24, 53.83, and 56.83-fold as large as that of free brucine, respectively. The LD(50) values of brucine solution, BSL-SPC, BSL-DPPC, BSL-HSPC, and BSL-DSPC following intravenous injection were 13.17, 37.30, 37.69, 51.18, and 52.86 mg/kg, respectively. It was found in calcein retention experiments that the order of calcein retention in rat plasma was SPC < DPPC << HSPC < DSPC stealth liposomes. PC composition could exert significant influence on the stabilities, pharmacokinetics, and toxicities of brucine-loaded stealth liposomes. DSPC or HSPC with T(m) above 50°C should be used to prepare the stealth liposomal formulation for the intravenous delivery of brucine. However, it was found in the present paper that the pharmacokinetics and toxicity of BSL were not influenced by the PC composition when the T(m) of the PC was in the range of -20°C to 41°C.

Flos Lonicerae Japonicae (FLJ) is a popular herb used for many centuries in Traditional Chinese Medicine as a treatment of fever and inflammation. Non-fumigated processing of FLJ has been the traditional approach used in post-harvest preparation of the commodity for commercial use. However, in recent years, natural drying processing of FLJ has been replaced by sulfur-fumigation for efficiency and pest control. Sulfur-fumigation can induce changes in the volatile compounds of the herb, altering its medicinal properties. A comprehensive two-dimensional gas chromatography time-of-flight mass spectrometry (GC×GC-TOF/MS) method was established for the resolution and determination of volatile components in non-fumigated and sulfur-fumigated FLJ. In this paper, analysis of the volatile oils in non-fumigated and sulfur-fumigated (including lab-prepared sulfur- fumigated and industrial sulfur-fumigated) FLJ was performed using GC×GC-TOF/MS. Seventy-three representative volatile components were identified, including furans, alkalies, acids, aldehydes, ketones, alcohols, terpenes, esters, and others, as the main components of FLJ volatile oils. The proposed method was successfully applied for rapid and accurate quality evaluation of FLJ and its related medicinal materials and preparations.

Aim： To investigate the mechanisms underlying the intestinal absorption of the major bioactive component forsythoside A （FTA） extracted from Forsythiae fructus. Methods： An in vitro Caco-2 cell model and a single-pass intestinal perfusion in situ model in SD rats were used. Results： In the in vitro Caco-2 cell model, the mean apparent permeability value （Papp-value） was 4.15x10-7 cm/s in the apical-to- basolateral （AP-BL） direction. At the concentrations of 2.6-10.4 pg/mL, the efflux ratio of FTA in the bi-directional transport experi- ments was approximately 1.00. After the transport, 〉96% of the apically loaded FTA was retained on the apical side, while 〉97% of the basolaterally loaded FTA was retained on the basolateral side. The Papp-values of FTA were inversely correlated with the transepithelial electrical resistance. The paracellular permeability enhancers sodium caprate and EDTA, the P-gp inhibitor verapamil and the multi-drug resistance related protein （MRP） inhibitors cyclosporine and MK571 could concentration-dependently increase the Papp-values, while the uptake （OATP） transporter inhibitors diclofenac sodium and indomethacin could concentration-dependently decrease the Papp-values. The intake transporter SGLT1 inhibitor mannitol did not cause significant change in the Papp-values. In the in situ intestinal perfusion model, both the absorption rate constant （Ka） and the effective permeability （Pefcvalues） following perfusion of FTA 2.6, 5.2, and 10.4 pg/mL via the duodenum, jejunum and ileum had no significant difference, although the values were slightly higher for the duodenum as compared to those in the jejunum and ileum. The low, medium and high concentrations of verapamil caused the largest increase in the Pefcvalues for duodenum, jejunum and ileum, respectively. Sodium caprate, EDTA and cyclosporine resulted in concen-tration-dependent increase in the Pefrvalues. Diclofenac sodium and indomethacin caused concentration-dependent decrease in the Peff-values. Mannitol did not cause significant change in the Papp-values for the duodenum, jejunum or ileum. Conclusion： The results suggest that the intestinal absorption of FTA may occur through passive diffusion, and the predominant absorp-tion site may be in the upper part of small intestine. Paracellular transport route is also involved. P-gp, MRPs and OATP may partici-pate in the absorption of FTA in the intestine. The low permeability of FTA contributes to its low oral bioavailability.

ObjectivesTo explore the protective effects of Tongmai Yizhi Decoction (通脉益智汤, TYD), a Chinese herb complex prescription against the impairment of cognitive functions and memory loss in amyloid beta 1–40 (Aβ1-40) peptide and ibotenic (IBO)-induced Alzheimer's disease (AD) model rats.MethodsThe in vivo model was established by injecting Aβ1-40 and IBO into left hippocampal CA1 area of Sprague-Dawley (SD) rat to mimic AD. Totally 32 SD rats were divided into 4 groups, including sham operation group, AD model group, TYD group [AD rats treated with TYD at the dosage of 19.44 g/(kg•d) for 4 weeks] and huperzine A group [AD rats treated with huperzine A at the dosage of 40.5 μg/(kg•d) for 4 weeks]. Spatial learning and memory level was detected by Morris Water Maze test. Histological morphology in the hippocampus was tested by hematoxylin-eosin (HE) staining. Cyclin-dependent kinase-5 (Cdk5) protein and gene expression level were investigated by Western blot analysis and real-time quantitative polymerase chain reaction (RT-qPCR), respectively.ResultsAβ1-40 and IBO treatment induced longer escape latency of rats, compared with sham operation group from day 25 (P<0.01). However, TYD and huperzine A obviously shortened the escape latency from day 26 (P<0.01). Moreover, the effect of TYD was similar to huperzine A (P>0.05). Furthermore, HE staining also showed that TYD and huperzine A reversed the neuropathological changes in the hippocampus triggered by Aβ1-40 and IBO. TYD and huperzine A effectively reduced the expression levels of Cdk5 protein and gene located in rat hippocampus, compared with the AD model group (P<0.01).ConclusionTYD could be a promising neuroprotective agent for protecting neuron from AD injury through inhibiting Cdk5 expression.

An accurate and reliable method of high-performance liquid chromatographic fingerprint combining with multi-ingredient determination was developed and validated to evaluate the influence of sulfur-fumigated Paeoniae Radix Alba on the quality and chemical constituents of Si Wu Tang. Multivariate data analysis including hierarchical cluster analysis and principal component analysis, which integrated with high-performance liquid chromatographic fingerprint and multi-ingredient determination, was employed to evaluate Si Wu Tang in a more objective and scientific way. Interestingly, in this paper, a total of 37 and 36 peaks were marked as common peaks in ten batches of Si Wu Tang containing sun-dried Paeoniae Radix Alba and ten batches of Si Wu Tang containing sulfur-fumigated Paeoniae Radix Alba, respectively, which indicated the changed fingerprint profile of Si Wu Tang when containing sulfur-fumigated herb. Furthermore, the results of simultaneous determination for multiple ingredients showed that the contents of albiflorin and paeoniflorin decreased significantly ( P < 0.01 ) and the contents of gallic acid and Z-ligustilide decreased to some extent at the same time when Si Wu Tang contained sulfur-fumigated Paeoniae Radix Alba. Therefore, sulfur-fumigation processing may have great influence on the quality of Chinese herbal prescription.

Asthma is one of the most common chronic airway inflammatory diseases. The clinical hallmarks of asthma include elevated serum levels of immunoglobulin E (IgE), eosinophilic inflammation and airway hyper-responsiveness (AHR). Arsenic trioxide (As 2 O 3 ) is considered a carcinogen; however, it has also been used to treat diseases, such as syphilis, in traditional Chinese and Western medicine. Today, As 2 O 3 is used as one of the standard therapies for acute promyelocytic leukemia (APL). Previous studies have indicated that As 2 O 3 can induce apoptosis in eosinophils. However, the effect of As 2 O 3 on asthma has not been investigated. We used ovalbumin (OVA)-immunized mice as a model for asthma and treated mice with As 2 O 3 at doses of 2.5 and 5 mg/kg. The mice were then monitored for OVA-specific IgE production, airway inflammatory cell infiltration and AHR. We found that administration of As 2 O 3 in OVA-immunized mice abrogated airway eosinophil recruitment by downregulating eotaxin expression but did not alter serum IgE or IL-5 levels in bronchoalveolar lavage fluid (BALF). Furthermore, the development of AHR and cellular infiltration into the airway were reduced by treating mice with As 2 O 3 . In vitro data suggested that low concentrations of As 2 O 3 could induce only a small degree of apoptosis in primary pulmonary cells but could significantly inhibit the secretion of eotaxin by these cells. These results indicate that the administration of As 2 O 3 to OVA-immunized mice can suppress lung allergic inflammatory responses. As 2 O 3 might therefore have therapeutic potential in treating allergic airway inflammatory diseases.

建立RP-HPLC法同時測定五味子（Schisandra chinensis）中11種具生物活性之木酚素，包括schisandrin、gomisin J、schisandrol B、angeloylgomisin H、gomisin G、schisantherin A、schisantherin B、deoxyschisandrin、γ-schisandrin、schisandrin B及schisandrin C。層析柱為Elite ODS C18 (250 mm × 4.6 mm，5 μm)，移動相為乙腈－水。11種木酚素在以下濃度範圍內線性關係良好(r ≥ 0.9995)：25.02 - 150.12 μg/mL (schisandrin)；5.20 - 31.20 μg/mL (gomisin J)；10.99 - 65.94 μg/mL (schisandrol B)；14.10 - 84.60 μg/mL (angeloylgomisin H)；2.55 - 15.30 μg/mL (gomisin G)；3.79 - 22.74 μg/mL (schisantherin A)；8.32 - 49.92 μg/mL (schisantherin B)；5.16 - 30.96 μg/mL (deoxyschisandrin)；9.10 - 54.60 μg/mL (γ-schisandrin)；20.70 - 124.20 μg/mL (schisandrin B)；4.56 - 27.36 μg/mL (schisandrin C)。平均回收率為97.74 - 102.71%。本方法經精密性、再現性及準確性確效，應用於五味子生品及炮製品檢驗，可同時測定五味子中11種木酚素含量。結果顯示，醋五味子與酒五味子中11種木酚素含量較生品高，證實五味子生品與炮製品功效有別，各成分含量百分比為五味子品種挑選和臨床應用提供科學依據。

Cimicifugae rhizoma was a Ranunculaceae herb belonging to the composite family, and the roots of C. rhizoma have been widely used in tradition Chinese medicine. Ultrasound-assisted extraction (UAE) of phenolic compounds from C. rhizoma. Caffeic acid (CA), isoferulic acid (IA), ferulic acid (FA), and total phenols were quantified by high-performance liquid chromatography-diode array detection and ultraviolet-visible spectrophotometer. Effects of several experimental parameters, such as ultrasonic power (W), extraction temperature (°C), and ethanol concentration (%) on extraction efficiencies of phenolic compounds from C. rhizoma were evaluated. The results showed that the optimal UAE condition was obtained with ultrasonic power of 377.35 W, extraction temperature of 70°C, and ethanol concentration of 58.37% for total phenols, and ultrasonic power of 318.28 W, extraction temperature of 59.65°C, and ethanol concentration of 64.43% for combination of CA, IA, FA. The experimental values under optimal conditions were in good consistent with the predicted values, which suggested UAE is more efficient for the extraction of phenolic compounds from plant materials.