[Changes in fingerprint and chromaticity values of Mori Cortex during stir-frying process].

This study aims to reveal the dynamics of the HPLC fingerprint, chromaticity values, and main chemical components of Mori Cortex during the stir-frying process. The fingerprints of raw and processed products of Mori Cortex were established. The content of mulberroside A, oxyresveratrol, kuwanon G, and kuwanon H in the samples and the chromaticity values of the samples were determined. Furthermore, the similarity evaluation of fingerprints and the correlation analysis between fingerprints and chromaticity values were carried out. The results showed that the fingerprints of raw and processed products of Mori Cortex had high similarity, and the overall changes in the content of the main chemical components in the stir-frying process were similar. According to the experience, when the stir-frying is moderate, the total chromaticity value difference |ΔE~*_(ab)| is above 1.5. With the extension of stir-frying time, the L~* and E~*_(ab) values keep decreasing, and the a~* value keeps increasing. The results of the correlation analysis between fingerprints and chromaticity values showed that peaks 1(5-hydroxy maltol), 2(mulberroside A), 3, 4, 6, 7, 11(oxyresveratrol), 14, 17(kuwanon G), and 18(kuwanon H) had significant correlations with the chromaticity values. Quantitative analysis of the four components with higher content showed that the content of the four components decreased to varying degrees when the stir-frying was excessive. In addition, 5-hydroxy maltol was produced after stir-frying of Mori Cortex, and the fingerprint and chromaticity values showed regular changes during the stir-frying process. The chromaticity can be included in the evaluation of the stir-frying process of Mori Cortex, which provides a reference for standardizing the quality of stir-fried Mori Cortex.

[Comparison of HPLC fingerprints and determination of main components of Viticis Fructus from different species].

In order to comprehensively evaluate the quality of Viticis Fructus, this study established HPLC fingerprints and evaluated the quality of 24 batches of Viticis Fructus samples from different species by similarity evaluation and multivariate statistical analysis(PCA, HCA, PLS-DA). On this basis, an HPLC method was established to compare the content differences of the main components, including casticin, agnuside, homoorientin, and p-hydroxybenzoic acid. The analysis was performed on the chromatographic column(Waters Symmetry C_(18)) with a gradient mobile phase of acetonitrile(A)-0.05% phosphoric acid solution(B) at the flow rate of 1 mL·min~(-1) and detection wavelength of 258 nm. The column temperature was 30 ℃ and the injection volume was 10 µL. The HPLC fingerprint of 24 batches of Viticis Fructus samples was established with 21 common peaks, and nine peaks were identified. Similarity analysis was carried out based on chromatographic data of 24 batches of chromatographic data of Viticis Fructus, and the results showed that except for DYMJ-16, the similarity of Vitex trifolia var. simplicifolia was ≥0.900, while that of V. trifolia was ≤0.864. In addition, the similarity analysis of two different species showed that the similarity of 16 batches of V. trifolia var. simplicifolia was 0.894-0.997 and that of the eight batches of V. trifolia was between 0.990 and 0.997. The results showed that the similarity of fingerprints of these two species was different, but the similarity between the same species was good. The results of the three multivariate statistical analyses were consistent, which could distinguish the two different species. The VIP analysis results of PLS-DA showed that casticin and agnuside contributed the most to the distinction. The content determination results showed that there was no significant difference in the content of homoorientin and p-hydroxybenzoic acid in Viticis Fructus from different species, but the content of casticin and agnuside was significantly different in different species(P<0.01). The content of casticin was higher in V. trifolia var. simplicifolia, while agnuside was higher in V. trifolia. The findings of this study show that there are differences in fingerprint similarity and component content of Viticis Fructus from different species, which can provide references for the in-depth study of the quality and clinical application of Viticis Fructus.

[Complanatoside A and complanatoside B in rats administered with raw and salt-processed Astragali Complanati Semen: a pharmacokinetics study].

An UPLC-MS/MS method was developed to simultaneously determine complanatoside A and complanatoside B in rat plasma with rutin as the internal standard and applied to examine the effect of salt-processing on pharmacokinetics of these two flavonoid glycosides. The pharmacokinetic parameters were estimated using DAS 3.2.6 and subjected to independent sample t-test with SPSS 23.0. No significant difference in T_(max) of complanatoside B was observed between the raw and processed groups; however, in the processed group, C_(max) and AUC_(0-12 h) of complanatoside B increased obviously(P<0.05), while MRT_(0-12 h) decreased from(3.34±0.44) h to(1.81±0.36) h(P<0.05). C_(max) [(14.72±11.13) µg·L~(-1)] and MRT_(0-24) [(3.93±0.26) h] of complanatoside A in the raw group were statistically different from those [(35.64±21.99) µg·L~(-1),(1.43±0.24) h] in the processed group(P<0.05). As a result, salt-processing can facilitate the in vivo adsorption and accelerate the excretion of complanatoside A and complanatoside B.

A new homo-aro-cholestane glycoside from the rhizome of Paris polyphylla var. chinensis.

A new homo-aro-cholestane glycoside parispolyside H, along with nine known compounds, were isolated from 75% ethanolic extract of the rhizome of Paris polyphylla var. chinensis. Their chemical structures were elucidated on the basic of analysis of detailed spectroscopic and physicochemical properties. In addition, the isolated compounds (1, 6-9) were evaluated for their cytotoxic activity against HepG2 human liver cancer cell lines. Among them, four known compounds (6-9) showed cytotoxicity with IC50 values ranging from 0.41 to 3.6 µM.

[Effects of processing on pharmacokinetics of Descurainiae Semen's constituents in rats].

An UPLC-MS/MS method simultaneously determining contents of quercetin-3-O-ß-D-glucose-7-O-ß-D-gentiobioside and sinapic acid in rats' plasma was firstly established and applied to study the effects of processing on pharmacokinetics of Descurainiae Semen's active constituents. Complantatoside A as internal standard,methanol used for protein precipitation,the method was validated according to the instructions of CFDA. Rats' plasma was collected after being oral administrated equal dosage of 60% ethanal extract of raw or processed Descurainiae Semen at different point of time,then the concentrations were determined to calculate pharmacokinetic parameters using DAS 3. 2. 6. And the parameters were analyzed using SPSS 23. 0,meantime the concentration-time curve was drawn.The results showed that processing had no effects on the pharmacokinetics of QGG,but could improve the absorption of sinapic acid and slow down the excretion.

Chemical constituents from the seeds of Cassia obtusefolia and their in vitro α-glucosidase inhibitory and antioxidant activities.

Basing on chromatographic separation techniques, fifteen aglycones (1-15), including two new anthraquinone aglycones (1, 2) and thirteen known compounds (3-15), were isolated from the small polar fraction of Cassia obtusefolia (petroleum ether extract). Structural elucidations were performed by 1D/2D NMR spectroscopy and mass spectrometry. The in vitro antioxidant and α-glucosidase inhibitory activities of these fifteen compounds were determined. Except compounds 12 (IC50 3.03 ±â€¯0.31 µg/mL, stronger than ascorbic acid, which IC50 was 6.48 ±â€¯2.30 µg/mL) and 13 (IC50 78.40 ±â€¯2.39 µg/mL), the free radical scavenging capacities of other compounds were weak. Compounds 4, 5, 6 and 13 exhibited inhibitory activities on α-glucosidase with IC50 values of 50.60 ±â€¯1.10, 22.57 ±â€¯0.07, 60.09 ±â€¯1.40, and 80.01 ±â€¯2.66 µg/mL separately, however, all the α-glucosidase inhibitory activities were weaker than positive control (acarbose).

[Chemical study on Cassiae Semen processing procedure].

References and our previous experiment showed that the contents of glycosides were significantly decreased，while the contents of aglycones were significantly increased after processing of Cassiae Semen.It may be related to its glycosidases or the heating process. In order to investigate the reasons, high performance liquid chromatographic (HPLC) was used to study the effects of these two factors on contents of Cassiae Semen's main chemical components in processing. The results showed that glycoside hydrolases was present in Cassiae Semen and could rapidly hydrolyze glycosides from Cassiae Semen into aglycones in suitable temperature with sufficient water.However，it didn't show effect on contents change of main constituents in the procedure of Cassiae Semen processing.The reason for content decrease of glycosides and content increase of aglycones in processed Cassiae Semen was glycoside bond cracking to produce corresponding aglycone at high temperature.This study further provides basis for further revealing of the processing mechanism of Cassiae Semen.

[Chemical constituents from seeds of Astragali complanati].

A new flavonoid glycoside, named complanatoside C (1), and 19 known compounds (2-20) were isolated from an 95% ethanol extract of Astragali Semen by various chromatographic methods. Their structures were identified on the basis of UV, IR, NMR, MS spectroscopic data analysis, and comparison with those in literature, including fifteen flavonoid glycoside (1-15), and six other constituents (16-20), among which compounds 16-19 were isolated from this plant for the first time.

A Chinese Herbal Decoction, Shaoyao-Gancao Tang, Exerts Analgesic Effect by Down-Regulating the TRPV1 Channel in a Rat Model of Arthritic Pain.

Shaoyao-Gancao Tang (SGT) is one of the most frequently used compound formulas in the treatment of pain-related diseases in the medical practice of traditional Chinese medicine (TCM). To investigate the anti-inflammatory and antinociceptive effects, as well as to uncover the molecular mechanism of SGT, the rat pain model of arthritis was experimentally induced by single unilateral injection of rats' left hind paw with Freund's complete adjuvant (FCA). SGT was orally administered to the rats daily at three doses individually for a period of 16 days post-model induction. Swollen degrees and pain thresholds of the rats in different groups were measured for evaluation of the anti-inflammatory and anti-nociceptive effects of SGT. Furthermore, the mRNA and protein expression levels of transient receptor potential ion channel protein vanilloid receptor 1 (TRPV1) channel as well as its calcium-mediating function in the isolated DRG neurons were further detected to provide indexes for exploration of the molecular mechanisms mediating anti-arthritic activities of SGT. As a result, FCA injection induced significant allodynia, inflammation and edema, accompanied by a significant increase in both expression and calcium-mediating function of the TRPV1 channel. Pharmacologically, oral administration of SGT at a high or middle dose demonstrated a significant relief from the above-mentioned pathological conditions in a dose-dependent manner. Simultaneously the mRNA and protein expressional levels of TRPV1 channel, as well as its calcium-mediating function, were down-regulated greatly. These findings suggest that SGT possesses a significant analgesic and anti-inflammatory effect on arthritis rats; its therapeutic activities might be achieved through reversing the elevated expression and function of TRPV1 channel evoked by FCA.

Synthesis of biscoumarin and dihydropyran derivatives with promising antitumor and antibacterial activities.

Two series of biscoumarin (1-3) and dihydropyran (4-12) derivatives were successfully synthesized as new antitumor and antibacterial agents. The molecular structures of four representative compounds 2, 4, 7 and 10 were confirmed by single crystal X-ray diffraction study. The synthesized compounds (1-12) were evaluated for their antitumor activities against human intestinal epithelial adenocarcinoma cell line (HuTu80), mammary adenocarcinoma cell line (4T1) and pancreatic cancer cell line (PANC1) and antibacterial activities against one drug-sensitive Staphylococcus aureus (S. aureus ATCC 29213) strain and three MRSA strains (MRSA XJ 75302, Mu50, USA 300 LAC). The further mechanism study demonstrated that the most potent compound 1 could obviously inhibit the proliferation of cancer cells via the mechanism to induce apoptosis.

Antibacterial and Antitumor Activities of Biscoumarin and Dihydropyran Derivatives.

A novel series of biscoumarin (1-4) and dihydropyran (5-13) derivatives were synthesized via a one-pot multicomponent condensation reaction and evaluated for antibacterial and antitumor activity in vitro. The X-ray crystal structure analysis of four representative compounds, 3, 7, 9 and 11, confirmed the structures of these compounds. Compounds 1-4 showed the most potent antitumor activity among the total 13 derivatives; especially for compounds 1 and 2, they also emerged as promising antibacterial members with better antibacterial activity. In addition, the results of density functional theory (DFT) showed that compared with compounds 3 and 4, biscoumarins 1 and 2 had lower intramolecular hydrogen bonds (HB) energy in their structures.

[Discrimination of Descurainiae Semen and Pantagirus Semen by HPLC fingerprints].

OBJECTIVE: To discriminate Descurainiae Semen and Pantagirus Semen. METHOD: A high-performance liquid chromatographic method was developed to establish the fingerprint of Descurainiae Semen, and hierarchical cluster analysis (HCA) and partial least squares discriminant analysis (PLS-DA) were applied to study HPLC fingerprinting and chemical recognition. RESULT: There exists large difference of chromatographic peaks and its relative peak area of HPLC fingerprints between Descurainiae Semen and Pantagirus Semen, and after conducting statistical analysis, the result demonstrated that all samples were classified into three categories: Descurainiae Semen, Pantagirus Semen and their mixtures. CONCLUSION: The developed HPLC fingerprint combined with chemometrics can be utilized to discriminate between Descurainiae Semen and Pantagirus Semen, which was quick, simple, accurate and reliable an can provide the basis for the characterization and quality assess of Descurainiae Semen and Pantagirus Semen.

Five new anthraquinones from the seed of Cassia obtusifolia.

A phytochemical investigation on the seeds of Cassia obtusifolia led to the isolation of five new anthraquinones, including one aglycon and four glycosides. The structures were elucidated by analysis of extensive spectroscopic data and the results of acid hydrolysis. All these isolates were evaluated for their inhibitory effects against α-glucosidase, and 1 showed potent activity with IC50 value of 185 ± 15 µM.

[Advances on Lepidii Semen and Descurainiae Semen].

"Tinglizi", the ripe seed of Descurainia sophia and Lepidium apetalum, is a member of Brassicaceae (Cruciferae). Traditionally, the former is called "Nantinglizi" (Descurainiae Semen) while the latter is called "Beitinglizi" (Lepidii Semen). In the theory of traditional Chinese medicine, it has the power to purge lung-fire, relieve dyspnea, promote diuresis and reduce edema, and it is mainly indicated in a case with phlegm-fluid accumulation, cough with excessive sputum, dyspnea with being unable to lie, and general swelling. In view of its wide-spread application in clinic, a comprehensive review of Lepidii Semen and Descurainiae Semen was conducted from the following aspects: herbalogical study, variety identification, historical evolution of processing, chemical constituents, pharmacological effects, quantitative determination and toxicity which could provide reference for further research and development of "Tinglizi".

[Determination of five primary chemical constituents in Cassia angustifolia by HPLC].

OBJECTIVE: To establish a method for determining the content of primary chemical constituents in the leaves of Cassia angustifolia. METHOD: The HPLC with Diamonsil C18 (4.6 mm x 250 mm, 5 microm) column was used , acetonitrile-1% acetic acid (10:90-15: 85-18: 82-20: 80-25: 75) in a gradient manner was used as a mobile phase, with flow rate of 1 mL x min(-1), column temperature at 40 degrees C and detection wavelength at 270 nm. RESULT: The results showed that 5 effective components all separated well and showed good linearity. CONCLUSION: The method was proved to be rapid, sensitive, accurate, credible and repeatable. It can be applied to quality control of Folium Sennae.

[Determination of rubrofusarin gentiobioside in Cassia obtusifolia by HPLC].

OBJECTIVE: To establish a method for determining the content of rubrofusarin gentiobioside in Cassia obtusifolia. METHOD: The HPLC with Diamonsil C18 (4.6 mm x 250 mm, 5 microm) column was used, acetonitrile-THF-1% acetic acid (18: 3:79) was used as a mobile phase, with flow rate of 1 mL x min(-1), column temperature at 40 degrees 2 and detection wavelength at 278 nm. RESULT: A good linearity was obtained from 0.1-0.5 microg with r = 0.999 9 for rubrofusarin gentiobioside. The average recovery was 101.1%, and RSD was 2.23% (n = 5). CONCLUSION: The method was proved to be simple, rapid, sensitive, precise, reliable and repeatable. It can be applied to the quality control of Semen Cassia.

[Quantititive study for chromatographic fingerprints of processed products of Paeonia lactiflora].

OBJECTIVE: To explore the utility of Principal Factor Analysis (PFA) in chromatographic data for quality control. METHOD: Chromatographic fingerprints of processed root pieces of Paeonia lactiflora were determined by HPLC, the PFA was used for data processing. RESULT: The quantitative differences among different growing areas and different processing batches were found with the method. CONCLUSION: The method could be used in quality control for monitoring between-batch products of traditional Chinese pharmaceutical process.

[Clustering analysis of HPLC chromatographic fingerprints of Paeonia suffruticosa].

OBJECTIVE: To explore the utility of chromatographic data for quality control of Paeonia suffruticosa, a Chinese herbal medicine. METHOD: Chromatographic fingerprints of Paeonia suffruticosa were determined by HPLC, the clustering analysis was used for data processing. RESULT: The quantitative differences among different growing areas were found and could be used to classify herbals from different growing areas, while there seemed to be no quantitative differences for processing factor. CONCLUSION: The method could be used in quality control for monitoring herbal quality control, and the result also suggested that different growing areas may greatly affected the herbal qualities.

[Chemical constituents from the leaves of Cassia angustifolia].

OBJECTIVE: To study the chemical constituents from the leaves of Cassia angustifolia. METHODS: Compounds were isolated and repeatedly purified by chromatographic techniques on silica gel column. Their structures were elucidated by chemical and spectral methods. RESULTS: eight compounds were isolated from the leaves of Cassia angustifolia, and identified as tinnevellin glycoside(I), isorhamnetin-3-O-beta-gentiobioside(II), apigenin-6,8-di-C-glycoside(III), emodin-8-O-beta-D-glucopyranoside(IV), kaempferol(V), aloe emodin(VI), D-3-O-methylinositol(VII), sucrose(VIII). CONCLUSION: Compounds III, VII and VIII are isolated from the plant for the first time.

[Study on quality control of Paeonia lactiflora].

OBJECTIVE: To provide the experimental data for the quality control of Paeonia lactiflora a prepared Chinese medicinal herb. METHOD: The contents paeoniflorin among different growing areas and different processing methods methods were assayed by HPLC. RESULT: The quantitative differences of paeoniflorin content among different growing areas and different processing methods wereanalyzed quantitatively. CONCLUSION: The quantitative differences among different growing areas were not significant and the quantitative differences among different processing methods within 10%.