[Key quality attributes of benchmark samples of famous classical formula Kaixin Powder].

We prepared 15 batches of Kaixin Powder benchmark samples with the decoction pieces of different batches. Further, we established the specific chromatograms and index component content determination method of Kaixin Powder benchmark samples and analyzed the peaks and similarity of the chromatograms. With sibiricose A5, sibiricose A6, polygalaxanthone Ⅲ, 3,6'-disinapoyl sucrose, ginsenoside Rb_1, ß-asarone, α-asarone, and dehydropachymic acid as index components, the index component content determination method was established and 70%-130% of the mean content of each component was set as the range. The chromatograms of 15 batches of Kaixin Powder benchmark samples had a total of 22 characteristic peaks, among which 8 peaks were identified, which represented sibiricose A5, sibiricose A6, polygalaxanthone Ⅲ, 3,6'-disinapoyl sucrose, ginsenoside Rb_1, ß-asarone, α-asarone, and dehydropachymic acid, respectively. The chromatograms shared the similarity of 0.992-0.999. The 15 batches of benchmark samples had sibiricose A5 of 0.34-0.55 mg·g~(-1), sibiricose A6 of 0.43-0.57 mg·g~(-1), polygalaxanthone Ⅲ of 0.12-0.19 mg·g~(-1), 3,6'-disinapoyl sucrose of 1.08-1.78 mg·g~(-1), ginsenoside Rb_1 of 0.33-0.62 mg·g~(-1), ß-asarone of 2.34-3.72 mg·g~(-1), α-asarone of 0.11-0.22 mg·g~(-1), and dehydropachymic acid of 0.053-0.079 mg·g~(-1). This study established the specific chromatograms and index component content determination method of Kaixin Powder benchmark samples, and the method was simple, feasible, reproducible, and stable. This study provides a scientific basis for further research on the key chemical properties of the benchmark samples and preparations of Kaixin Powder.

Precise identification of Celosia argentea seed and its five adulterants by multiple morphological and chemical means.

Celosia argentea seed (CAS) has been used as a traditional Chinese medicine for the treatment of liver damage and eye diseases. CAS is easily falsely harvested and misused, five species from Amaranthaceae family have frequently found to be involved in the adulteration and misapplication, namely Celosia cristata seed (CCS), Amaranthus tricolor seed (ATS), Amaranthus retroflexus seed (ARS), Amaranthus cruentus seed (ACS), and Amaranthus spinosus seed (ASS). For the purpose of identification, multiple morphological means including stereomicroscopy, scanning electron microscopy, normal light and polarized light microscopy were comprehensively employed. As a result, micromorphological and microscopic characteristics were extracted and a diagnostic key to CAS and its five adulterants was proposed for the first time. With respect to the genetically closely related species, viz. CAS and CCS, chemical means were developed to achieve the goal of precise identification. Firstly, triterpenoid saponins in CAS and CCS were fully characterized by an HPLC-QTOF-MS/MS method, a total of 20 triterpenoid saponins including 9 novel members were identified. Secondly, the HPLC-ELSD specific chromatogram was established, in which 12 common peaks were assigned. Finally, after a careful comparison, the peak area ratio of two triterpenoid saponins was discovered as interspecies discriminant marker. In conclusion, CAS and its five adulterants can be precisely identified by multiple morphological and chemical means.

Recent advance in the discovery of tyrosinase inhibitors from natural sources via separation methods.

Tyrosinase (TYR) inhibitors are in great demand in the food, cosmetic and medical industrials due to their important roles. Therefore, the discovery of high-quality TYR inhibitors is always pursued. Natural products as one of the most important sources of bioactive compounds discovery have been increasingly used for TYR inhibitors screening. However, due to their complex compositions, it is still a great challenge to rapid screening and identification of biologically active components from them. In recent years, with the help of separation technologies and the affinity and intrinsic activity of target enzymes, two advanced approaches including affinity screening and inhibition profiling showed great promises for a successful screening of bioactive compounds from natural sources. This review summarises the recent progress of separation-based methods for TYR inhibitors screening, with an emphasis on the principle, application, advantage, and drawback of each method along with perspectives in the future development of these screening techniques and screened hit compounds.

Comprehensive identification of Vitex trifolia fruit and its five adulterants by comparison of micromorphological, microscopic characteristics, and chemical profiles.

Prevention against the adulteration of traditional Chinese medicine in an accurate way has been long exploring. Vitex trifolia fruit (VTF), as a widely used analgesic in East Asia, has frequently been found to be adulterated with five adulterants, namely Vitex cannabifolia fruit (VCF) (Fam. Verbenaceae), Vitex negundo fruit (VNF) (Fam. Verbenaceae), Piper cubeba fruit (PCF) (Fam. Lauraceae), Euphorbia lathyris seed (ELS) (Fam. Euphorbiaceae), and Vaccinium bracteatum fruit (VBF) (Fam. Ericaceae). In this study, the methods of micromorphological identification, microscopic identification, and chemical analysis were combined to distinguish VTF from its five adulterants comprehensively. As a result, the micromorphological features in terms of fruit or seed epidermis were photographed by stereomicroscopy firstly. Secondly, the microscopic characteristics of various herb powders were captured under light microscopy. Thirdly, 33 nonvolatile components and 124 volatile components in VTF were identified by ultra-performance liquid chromatography coupled with Orbitrap mass spectrometry (UPLC-Orbitrap-MS) and comprehensive two-dimensional gas chromatography hyphenated with mass spectrometry (GC × GC-MS), respectively. Furthermore, betulinic acid, persicogenin, and the volatile 4-(2,2,6-trimethyl-bicyclo[4.1.0]hept-1-yl)-butan-2-one were screened out to be the specific markers of VTF distinctive from the adulterants. Collectively, VTF and its five adulterants were distinguished successfully by the comparison of micromorphological, microscopic characteristics, and chemical profiles.

Innovative health risk assessment of heavy metals in Chinese herbal medicines based on extensive data.

In the present study, the concentrations of lead (Pb), cadmium (Cd), arsenic (As), mercury (Hg), and copper (Cu) in 2245 batches of Chinese herbal medicines (CHMs) were measured using inductively coupled plasma-mass spectroscopy (ICP-MS). We developed a risk assessment strategy that assessed the heavy metal-associated health risk of CHMs based on our large dataset. Using a combination of the mean and 95th percentile (P95) values of the chronic daily intake (CDI), hazard quotient (HQ), hazard index (HI), and lifetime cancer risk (CR), the health risks of the average exposure population and the high exposure population were estimated, respectively. To obtain a precise and realistic risk assessment, the exposure frequency and exposure duration were determined using questionnaire data from 20,917 randomly selected volunteers. Additionally, given the specific ingestion characteristics of CHMs, the safety factor and the transfer rates of heavy metals were highlighted as well. The concentrations of Pb, Cd, As, Hg, and Cu in 2245 batches of CHMs were 1.566, 0.299, 0.391, 0.074, and 8.386 mg/kg, respectively. The mean HI values indicated that consumption of most CHMs would not pose an unacceptable health risk to the average exposure population, except for argy wormwood leaf (1.326), morinda root (2.095), plantain herb (1.540), chrysanthemum flower (1.146), and Indian madder root (2.826). In addition, CR assessment for Pb and As revealed that, for the average exposure population, the risk of developing cancers was lower than the acceptable levels (1 × 10-4) in the clinic. However, the P95 of the HI and CR values indicated that more attention should be paid to the systemic effects of CHMs in terms of both non-carcinogenic and carcinogenic health risks for the high exposure population. Furthermore, in order to serve population health better, national and international guidelines have now been established. The risk assessment strategy developed in this study is the first of its kind, and contributed to the risk assessment, guidelines, and safety standards for heavy metals in CHMs.

Emodin Exerts an Antiapoptotic Effect on Human Chronic Myelocytic Leukemia K562 Cell Lines by Targeting the PTEN/PI3K-AKT Signaling Pathway and Deleting BCR-ABL.

The BCR-ABL kinase inhibitor, imatinib mesylate, is the front-line treatment for chronic myeloid leukemia, but the emergence of imatinib resistance has led to the search for alternative drug treatments. There is a pressing need, therefore, to develop and test novel drugs. Natural products including plants, microorganisms, and halobios provide rich resources for discovery of anticancer drugs. In this article, we demonstrate that emodin inhibited the growth of K562 cells harboring BCR-ABL in vitro and in vivo, and induced abundant apoptosis, which was correlated with the inhibition of PETN/PI3K/Akt level and deletion of BCR-ABL. These findings suggest that emodin is a promising agent to kill K562 cells harboring BCR-ABL.

[Research on quality standards of Aleuritopteris Herba].

This study aims to establish quality standards of Aleuritopteris Herba (AH), which could supply scientific evidence for the quality control of AH. The morphological and microscopic identification characters were reformulated. The tests of water content, total ash, acid-insoluble ash and ethanol-soluble extractives of AH were carried out according to the methods recorded in appendix of Chinese Pharmacopeia (2010 edition, volume 1). The TLC method was established by using aleuritopesis A [2,19-diol（2ß,4α）-16-enekaureniod] and reference herb as references. With preparation of aleuritopesis A[2,19-diol（2ß,4α）-16-enekaureniod] reference substance, the content of aleuritopesis A in AH was determined by HPLC. As a result, the macroscopic identification, microscopic features and TLC methods were specific and simple. The water content, total ash, acid-insoluble ash and ethanol-soluble extractive and the content of aleuritopesis A of all samples varied in the ranges of 8.8%-10.9%, 7.6%-11.4%, 2.5%-4.2%, 9.3%-10.2% and 0.56%-0.71%, respectively. The improved quality standard can be used to evaluate and guarantee the quality of AH comprehensively.

[Simultaneous determination of 5 kinds of alkaloids in Kechuanning tablets by SPE-UPLC under different UV-vis wavelength].

The paper is to establish a method for simultaneous determination of 5 kinds of alkaloids in ephedra and poppy which are in Kechuanning tablets. Solid-phase extraction (SPE) was adopted in pretreatment, and a UPLC method with 2 different wavelengths had been developed: 210 nm for the detection of morphine, codeine phosphate, ephedrine hydrochloride and pseudoephedrine hydrochloride, and 251 nm for papaverine hydrochloride. The column used was Acquity UPLC BEH C18 (100 mm x 2.1 mm ID, 1.7 microm) with linear gradient elution using acetonitrile and 0.1% phosphoric acid. The flow rate was 0.4 mL.min-1, and the column temperature was 30 degrees C. The linear response range was 0.375 0 - 12.50 microg.mL-1 for morphine, 0.064 32 - 2.144 microg.mL-1 for codeine phosphate, 0.030 06 - 1.002 microg.mL-1 for papaverine hydrochloride, 1.126 - 37.52 microg.mL-1 for ephedrine hydrochloride, 0.287 8 - 9.592 microg.mL-1 for pseudoephedrine hydrochloride (r = 0.999 7). The average recoveries of these compounds were 99.26%, 100.6%, 95.29%, 100.1% and 97.48%, respectively. This is a more reasonable and credible method of quality control for Kechuanning tablets.