Polar auxin transport gene PIN (PIN-FORMED) determines the concentration gradient of auxin and plays an important role in development and secondary metabolism of plants. This study was designed to analyze the bioinformatics and expression of the PIN genes in Panax ginseng to explore a novel way of breeding ginseng varieties. Heatmap and cluster analysis of PIN2, PIN3, PIN6 was performed in four-year-old Jilin ginseng. Sequence homology alignment, RT-PCR amplification, sequencing and bioinformatics analysis were used to identify three PIN family genes PgPIN2, PgPIN3 and PgPIN6 in P. ginseng. PIN expression in ginseng adventitious root and culture seedling was analyzed with qRT-PCR technique. Results suggested that in ginseng adventitious root tip, PgPIN3 and PgPIN6 exhibited a high level of expression; in ginseng culture seedling root, PgPIN2 showed a high level of expression; in four-year-old Jilin ginseng at the fruit ripening stage, PgPIN2 and PgPIN6 were highly expressed in root and rhizome, while PgPIN3 had a high level in ginseng leaf, fruit and root. Tissue specific expression profile showed that PgPIN2 and PgPIN6 probably were involved in the development and tropism growth in ginseng roots, while PIN3 might be in relation to the growth and development of the aerial part of plants.

A rapid fluorescence polarization immunoassay (FPIA) has been developed for the determi-nation of aflatoxins in samples of naturally-contaminated herbal teas. The tracers were synthesized by chemical method and determined by thin layer chromatography (TLC) and mass spectroscopy (MS). Fluorescence polarization was evaluated by the detection of polarized light. The results showed that the limit of detection (LOD) of FPIA for aflatoxins was 20 ng·mL^-1, the IC₅₀ was 371.80 ng·mL^-1, and the linear range of the developed FPIA was 92.76-252.32 ng·mL^-1. Compared with conventional HPLC methods, the FPIA developed in this study has the advantages of short analysis time and low cost. This method may be suitable for high-throughput screening of aflatoxins in herbal teas.

Eighteen novel levofloxacin-thiadiazole HDACi conjugates were designed and synthesized from levofloxacin. The chemical structures of all conjugates were confirmed by ¹H NMR, ¹³C NMR and HR-MS spectra. The inhibitory activities of new conjugates were evaluated in an assay with a HDACs reagent kit, and their anti-tumor activities were tested in CCK-8 assay. The results showed that these new conjugates displayed potent inhibitory activity against HDACs, and the hydroxamate conjugates exhibited more potent activity than carboxylic acid and benzamide derivatives. Specifically, conjugate 5d exhibited the most potent anti-HDAC1 (IC₅₀=0.031±0.011 μmol·L^-1) and HDAC6 (IC₅₀=0.019±0.006 μmol·L^-1) activities, which was more potent than SAHA. Molecular docking studies suggest that the hydroxamate group of conjugate 5d was deeply inserted into the active site to interact with the residues in coordination with the zinc ion. Additionally, the thiadiazole group of conjugate 5d also engaged in hydrogen bonding with F679 in HDAC6, which had been linked to the selectivity of the HDAC isoforms. Moreover, these conjugates displayed significant antiproliferative effects on SW620, MGC-803, PC-3, NCIH460, MCF-7 and HepG2 cells, in particular, conjugate 5d showed the greatest potency against MGC-803 (IC₅₀=0.7±0.05 μmol·L^-1), NCIH460 (IC₅₀=2.3±0.421 μmol·L^-1), MCF-7 (IC₅₀=1.6±0.56 μmol·L^-1) and HepG2 (IC₅₀=3.9±0.26 μmol·L^-1), which was >3-fold more potent than SAHA. Additionally, all conjugates were nontoxic to health GES-1 cells, while SAHA showed some toxicity.

Parthenolide is a sesquiterpene lactone derived from the plant feverfew (Tanacetum parthenium) that possesses multiple anti-inflammatory and anti-cancer properties. A specific, sensitive, accurate and precise LC-MS/MS method was developed and validated in the quantitative analysis of parthenolide in rat plasma. A liquid-liquid extraction method was used to separate the analyte and the internal standard (IS, costunolide) from plasma. A water-methanol mobile phase system was utilized in the gradient chromatographic separation. The calibration curve with good linearity (r² > 0.99) was established between 2 and 128 ng·mL^-1 with accuracy and precision within acceptable limits at different QC levels. High extraction recovery was achieved for both parthenolide (89.55%-95.79%) and IS (96.87%). Based on this LC-MS/MS method, the plasma stability and pharmacokinetics of parthenolide were assessed in rats. Parthenolide was proved to be very unstable in rat plasma, and was distributed and eliminated quickly in vivo, with a half-life less than 90 min. A high dose of parthenolide (80 mg·kg^-1) resulted in a very low initial concentration (138.86±21.07 ng·mL^-1). The systemic exposure of parthenolide (area under the curve) increased disproportionally from 40 mg·kg^-1 dose group to 80 mg·kg^-1 dose group. The present study may provide helpful information for the development of parthenolide as a drug candidate.

Persicae semen has been used for years as a traditional Chinese medicine to treat diseases. Because of their similar morphologies, Persicae semen was commonly inadvertently mixed with Armeniacae semen amarum (a toxic herbal seed). Development of a reliable method for discriminating Persicae semen from its adulterant is necessary to reduce confusion for the drug safety in clinical practices. This study evaluates the efficiency of high-resolution melting (HRM) combined with internal transcribed spacer 2 (ITS2) to analyze Persicae semen. Our findings show that HRM allows not only the identification of adulteration but also the quantification of the most common admixture. HRM sensitivity in adulterant detection was assessed through the analysis of mixing samples with different proportions of Prunus persica and Prunus armeniaca control. The results are presented as a linear regression with r of 0.96 and imply the capability of the method to detect adulteration. In particular, HRM detected seeds of Prunus persica in Prunus armeniaca at concentrations as low as 1%, and commercial products labeled as 'Persicae semen' were purchased from markets and could rapid authenticated by HRM analyses. This study is significant in the verification of the authenticity in the quality control of herbal medicine. In the near future, it is promising to be the main trend for identifying traditional Chinese medicinal materials.

In this study, we developed a qualitative analytical method based on liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry (UHPLC-Q-TOF-MS/MS) for identification of multi-constituents of raw Fructus Arctii (RFA) and processed Fructus Arctii (PFA). We established a UHPLC-UV analytical method for simultaneously determining 6 major compounds in Fructus Arctii. UHPLC-Q-TOF-MS/MS qualitative analysis was performed under negative and positive ion modes and a total of 23 chemical compounds were identified. The analysis data were subjected to a principle component analysis with a t-test. Ten peaks were found to be the main difference (P < 0.05) between RFA and PFA. HPLC-UV quantitative method result showed the contents of 6 constituents were different between RFA and PFA. The results indicated that there was less arctiin, chlorogenic acid, isochlorogenic acid A in PFA than in RFA. However, there were higher levels of arctigenin, isochlorogenic acid B, isochlorogenic acid C in the PFA than RFA, which may be the main reason for different clinical efficacy of RFA and PFA.

Diabetic neuropathic pain (DNP) is the most common chronic complication of diabetes mellitus, significantly affecting people's quality of life. Studies have indicated that ion channels play a very important role in the occurrence of DNP. This review provides a summary in the role of ion channels in diabetic neuropathic pain and treatment strategies for diabetic neuropathy targeting ion channels.

Transglutaminase (TG) posttranslational modification of antibody permits more precisely conjugating. Based on the amino acid sequence of an anti-CD24 antibody (cG7), this article is aimed to generate a deglycosylated cG7 mutant (cG7Q). Firstly, we introduced additional glutamines at position 297 (N297Q) by site-directed mutagenesis, and then transfected the recombinant plasmids into CHO-s cells via electroporation method and screened by Dot blot assay. Subsequently, cG7Q was expressed and purified through Protein A affinity chromatography, further identified by SDS-PAGE electrophoresis and Western blot. Its affinity was detected with surface plasmon resonance and flow cytometry assay, and ADCC effect was determined by lactate dehydrogenase (LDH) release. Eventually, a cG7 mutant, cG7Q was successfully expressed with sequence-specific conjugation sites for further study.

The pharmacological activities of natural glycosides are closely related to the polyfunctional sugar moieties. Modification of active natural products by glycosylation can change the stereochemical configuration, improve the solubility, tune up the activities and change pharmacokinetic properties for higher efficacy and better selectivity. Compared with the common D-glucose, D-allose, a C-3 epimer of D-glucose rarely exists in nature, but it plays an important role in food, health, medicine, and so on. It is not easily metabolized in the living organisms, but can be used as a safe and low-calorie sweetener. The natural allopyranosides are absolute conjugation forms which are same as other glucopyranosides and rhamno-pyranosides with a broad array of biological activities. This article summarizes the major progresses made in phytochemistry and biological activity studies of these compounds. Structure-activity relationship analyses of partial anti-tumor and anti-diabetic allopyranosides were performed regarding the data reported in the literatures. These insights may provide a theoretical and experimental reference for the discovery of new drug and drug design based on allopyranosides.

This study was conducted to test the effects of schizandrin B (Sch B) on clozapine (CLZ) induced chronic liver injury in mice and the mechanism of action, and this may provide a new approach for clinical prevention of CLZ-induced side effects. The CLZ was given to mice for three weeks alone or co-administration with Sch B. The changes of alanine aminotransferase (ALT), aspartate transaminase (AST), alkaline phosphatase (ALP) and antioxidation indexes superoxide dismutase (SOD), malonic dialdehyde (MDA), glutathione (GSH) and liver histological evaluation were determined. Expression of Nrf2 was assayed in hepatic cells by immunohistochemical staining and Western blotting. The changes of relative gene expression of NAD (P) H:quinone oxidoreductase l (NQO1) and heme oxygenase 1 (HO-1) were assayed by real-time Q-PCR. The results showed that pretreatment with a lower dosage of Sch B (25, 50 mg·kg^-1) prevented CLZ-induced liver injury as indicated by the reduced levels of ALT, AST and ALP, and the preserved activities of SOD, GSH and inhibiting MDA. It was shown that Sch B could up-regulate Nrf2 expression leading to nuclear accumulation of Nrf2 to induce oxidative response genes such as NQO1 and HO-1. These results suggest that Sch B could protect against liver injury induced by CLZ via the activation of the Nrf2/ARE signal pathway in a dose-dependent manner.