Traditional Chinese medicinal materials (TCMMs) are the material basis of the traditional Chinese medicines (TCM) in the treatment of disease, and the inherent quality of the TCMMs are of crucial importance for the efficacy and safety of TCM. Most of the TCMMs are originated from the plants with complex chemical compositions, and the chemical diversity is inevitable. How to clarify the relationship between the chemical identity and the biological activity is the key point for quality control of TCMMs in the establishment of the quality standards. The components with great impact on the biological activities should be used as index compounds in the quality evaluation. In this study, based on the results in our previous studies, a research idea on the evaluation of quality difference of TCMMs is proposed. Its application and existing problems are also discussed.

The aim of the experiments is to screen human single-chain variable fragment (scFv) targeting glypican 3 from phage display library, and analyze its biological activity. After several rounds of panning, the binders with high affinity were obtained through phage ELISA and IMGT analysis. The desired scFv gene was then ligated with pET-22b vector yielding recombinant plasmids, which was then introduced into E. coli Rosetta (DE3). Soluble scFv protein was expressed and further purified using Ni²⁺ affinity chromatography. The purified proteins were identified by SDS-PAGE and Western blot. Subsequently, the affinity and cell based binding activity were measured using Surface Plasmon Resonance (SPR) and flow cytometry assay, separately. Four enriched sequences with relatively high binding affinity were found (1F7, 1D7, 1D4 and 1B10). We also found that 1F7 scFv showed better targeting ability and higher affinity. The scFv could pave the way for new immunotherapies, such as bispecific anitbody, antibody-drug conjugate and chimeric antigen receptor T-cell immunotherapy cell, etc.

Photo-sensitive reactive oxygen species (ROS) responsive liposomes loaded with 1, 4, 8, 11, 15, 18, 22, 25-octabutoxypalladium phthalocyanine[PdPC(OBu)₈] and doxorubicin hydrochloride (DOX) (LPD) were prepared by (NH4)₂SO₄-gradient method. LPD was characterized with transmission electron microscopy (TEM), dynamic light scattering particle size, zeta potentials, photo-sensitive ROS-responsive DOX release behaviors and the serum stability in vitro. LPD cytotoxicity, DOX uptake and singlet oxygen production in MCF-7 cells were evaluated. The results showed that the particle size of LPD was (169.3 ±1.2) nm, PDI of LPD was 0.198 ±0.003 and zeta potentials of LPD was (-39.8 ±0.8) mV. The accumulated release of DOX reached 95.5% in 5 min under 730 nm laser irradiation (300 mW·cm^-2). The DOX uptake of liposome was increased and ¹O₂ was generated. The half inhibition concentration (IC₅₀) of DOX in LPD with irradiation group was decreased by 85.7% and no irradiation group was decreased by 67.9% compared with free DOX group in MCF-7 cells. Therefore, photo-sensitive ROS-responsive liposomes would be a promising drug delivery system for tumor therapy.

Nimodipine is a selective calcium channel antagonist of cerebral vessels smooth muscle and also has polymorphs. It hasn't been reported that different crystal forms influence the metabolism process in huge animals like rhesus monkeys in vivo. This article may provide reference in the control of the quality of nimodipine and quality consistency evaluation. The powder X-ray diffraction (PXRD) method was used to identify different crystal forms and the dissolution test in vitro was used to detect the dissolution. The LC-MS method of assay nimodipine in rhesus monkey plasm was established to determine pharmacokinetics characters of different tablets from different crystal forms in rhesus monkey in vivo. As a result, the tablets inherit difference crystal forms and the dissolution of reference tablets is 1.3% higher than crystal tablets. However, the maximal blood concentration (C_max) of crystal tablet was 37.3% higher than reference tablet and AUC of crystal tablet was 29.8% higher than reference tablet. After administrated 2.5 mg·kg^-1 orally, calculated pharmacokinetics characters were observed as following:C_max was 381.4 ±327.3 and 178.0 ±214.8 μg·L^-1; AUC_0-t was 853.1 ±500.7 and 646.5 ±430.3 μg·L^-1·h respectively. The serum concentration result of different nimodipine tablets in rhesus monkeys in vivo suggests that polymorphs has a significantly distinction, which points out that controlling the crystal forms of nimodipine is essential to ensure the therapeutic efficacy. It is essential to execute quality consistency evaluation.

Jasmonic acid (JA) is an important signal molecule involved in plant resistance, and allene oxide synthase (AOS) is a key enzyme in the biosynthesis of jasmonates. In this study, a full-length cDNA of AsAOS1 gene was cloned from Aquilaria sinensis. Meanwhile, the sequence analysis, prokaryotic expression, purification, tissue-specific expression analysis and expression analysis under different abiotic stresses and hormone treatments were performed. The open reading frame (ORF) of AsAOS1 gene was 1 575 bp, encoding a protein of 524 amino acid residues, with a predicted molecular mass of 58.70 kDa. AsAOS1 protein possessed the conserved sequences of cytochrome P450 (CYP450). The phylogenetic analysis indicated that AsAOS1 protein had the highest level of homology with AOS protein of Citrus sinensis. The recombinant AsAOS1 protein was successfully expressed in Escherichia coli BL21(DE3) cells using the prokaryotic expression vector pET28a-AsAOS1 and the recombinant AsAOS1 was purified by Ni²⁺ affinity chromatography. Expression analysis results in different tissues showed that AsAOS1 was primarily observed in stems, and then roots, followed by leaves. AsAOS1 transcript level was significantly induced after 12 h treatment of NaCl, cold temperature and CdCl₂. Furthermore, AsAOS1 expression level was enhanced upon methyl jasmonate (MeJA), salicylic acid (SA) and abscisic acid (ABA) treatment. However, mannitol and gibberellin (GA₃) treatments had little influence on the expression level of AsAOS1. These results provides valuable insights into the role of JA in the mechanism of agarwood formation and plant resistance.

Ferroptosis is a novel type of cell death which induced by iron-dependent lipid peroxidation accumulation. This type of cell death is significantly different from other cell death in terms of morphology, genetics and biochemistry. It has been reported that ferroptosis is involved in a variety of human diseases, particularly in liver diseases. Therefore, screening and studying of inhibitors or activators of ferroptosis may provide novel strategies for prevention and treatment of liver diseases. This review provides the biological characteristics and regulatory signaling pathways of ferroptosis, as well as the relationship between ferroptosis and liver diseases, which will contribute to new insight into the pathogenesis of liver diseases.

A droplet microfluidic chip system was developed for drug screening against Candida albicans. The microfluidic chip was designed and prepared for the formation of droplets. Alamar blue was selected as an indicator for its characteristic of fluorescence mission in live cells. Four antifungal drugs (amphotericin B, caspofungin, 5-fluorocytosine, terbinafine) and a new drug (iodiconazole) were selected as model drugs to test the microfluidic chip approach. At the same time, 96-well microplate method was performed to verify the applicability of the chip method. The results showed that the developed droplet microfluidic chip platform was able to complete the antifungal susceptibility test within 2 h. In comparison with the 96-well microplate method, the microfluidic chip method showed a consistence of 100% with regard to the minimum inhibition concentrations and less reagent consumption. The new droplet microfluidic chip method is simple, rapid and suitable for rapid screening of antifungal drugs.

Interleukin-6 (IL-6)/signal transducers and activators of transcription (STAT) signaling pathway is closely related to the development and progression of atherosclerosis (AS). Taking Chinese natural product berberine (BBR) as the leading compound, a series of novel BBR analogues defined on different types of substituents on position 3 or/and 9 were designed, synthesized and evaluated for their inhibitory activities on phosphorylation of STAT-1 and STAT-3 induced by IL-6. The structure-activity relationship indicated that introduction of rigid fragment on position 3 or 9 was beneficial for enhancing their activities. Among them, compounds 2b and 9 exhibited the most satisfactory potency. The study revealed that the compounds 2b and 9 exhibit anti-inflammatory potencies via activating AMPK, and down-regulation of phosphorylation of STAT1 and STAT3 induced by IL-6 in HUVEC cells. These results suggest that BBR derivatives may inhibit the inflammatory response mediated by the IL-6/STAT signaling pathway through regulation of AMPK, which provides useful insight into the development of BBR derivatives for treatment of atherosclerosis.

Integrin is a class of important cell surface molecules involved in cell proliferation, differentiation, adhesion and migration processes, which play an important role in a variety of pathological processes. In recent years, with the research in integrin regulation and the treatment of tumor, tissue fibrosis, and other fields, integrin has gradually become a new target in the diagnosis and treatment of diseases. In this article, we provide a summary on the advances of the regulation of integrin gene expression.

The aim of this study was to investigate the regulatory effect of the total glycoside extracted from leaves of Rehmannia (TLR) and Dihuangye total glycoside capsule (DTG) on intestinal microflora in diabetic nephropathy rats. Forty-eight rats were randomly divided into the control group (C), model group (M), Huangkui capsule group (0.75 g·kg^-1·d^-1, HK), irbesartan group (27 mg·kg^-1·d^-1, YX), TLR low dose group (4.3 g·kg^-1·d^-1, DHYL), TLR high dose group (7.2 g·kg^-1·d^-1, DHYH), DTG low dose group (216 mg·kg^-1·d^-1, JNL), DTG high dose group (360 mg·kg^-1·d^-1, JNH). Rat model of diabetic nephropathy was induced by intraperitoneal injection of small dose of streptozotocin (45 mg·kg^-1, STZ) and feeding high-fat diet and 5% glucose drinking water. After oral administration for two weeks, the 16S rDNA sequencing method was used to study the effects of the TLR and DTG on intestinal flora in diabetic nephropathy rats. The results showed that compared with the control group, the intestinal flora of diabetic nephropathy rats had changed from phylum units to the genus units. Moreover, the proportion of lactobacilli in the intestinal bacteria of the model group was significantly decreased, and the proportion of lactobacilli in the administration group was increased, especially the YX group, TLR low dose group and DTG low dose group. The data suggest that the total glycosides of Rehmannia glutinosa improved the disorder of intestinal flora in STZ-induced diabetic nephropathy rats.