Anoectochilus roxburghii (Wall.) Lindl. is a medicinal species belonging to the Orchidaceae, whose whole plant can be used as a medicinal herb, known as "JinXianLian". It has antidiabetic, liver-protecting, anti-inflammatory, etc. A. roxburghii has long been used as food and medicine in Guangdong and Fujian provinces. With the wide recognition of the concept of "medicine and food homology" and the surge of market demand, wild A. roxburghii has been far from meeting the supply. It is important to establish an artificial propagation system. Resource characteristics are the key basis for optimizing germplasm and propagation systems. Therefore, this paper summarizes the germplasm resource characteristics and propagation technologies of A. roxburghii in China to provide a reference for sustainable development and subsequent mechanistic research.

Increasingly researches suggested that intermittent fasting (IF) can be part of a healthy lifestyle, which can improve risk factors associated with obesity and diabetes. Based on LC-MS metabolomics technology, this study preliminarily discussed the effect of IF on the metabolism of mice under normal physiological conditions by detecting the fecal metabolites. All experiments were approved by the Animal Research Committee of Shanghai University of Traditional Chinese Medicine. Animal welfare and the animal experimental protocols were strictly consistent with related ethics regulations of Shanghai University of Traditional Chinese Medicine. The mice were subjected to intermittent fasting for 10 weeks by fasting for 24 hours on alternate days, and their feces at 5 and 10 weeks were collected. The results show that the weight, food and water intake was not significant altered in mice with IF, but fasting blood glucose level was decreased. We found that fecal metabolites change was present at 5-week, being more prominent in 10-week. Relative to the control mice, we detected 17 and 108 metabolites in two time points, respectively. These metabolites were mainly enriched in the pathways of linoleic acid metabolism and bile acid biosynthesis. We further found that 10 metabolites may be a close correlation with IF, which had the same change trend at two time points. In conclusion, the present study provides a new approach to study the metabolism mechanism in IF treatment of related diseases.

Local drug delivery is a new strategy to prevent postoperative recurrence of cancer, thermosensitive gel is a typical topical drug delivery system. In this study, a novel paclitaxel thermosensitive gel (PTG) was prepared to prevent recurrence after chemotherapy for cancer, the effects of drug particle size on release and absorption rate in vivo were investigated. Paclitaxel suspensions with different particle sizes were prepared by medium grinding, high pressure homogenization, air crushing and screening. Using poloxamer as the gel matrix and carbomer as the biological adhesive, Box-Behnen was used to optimize the formulation of PTG. The morphology, viscosity, rheological properties and biological adhesion of thermosensitive gel were characterized. The relationship between dissolution and release of thermosensitive gel was investigated by weight loss method, pharmacokinetics was studied in rats. The paclitaxel suspensions with the particle sizes of 350 nm, 800 nm, 3 μm and 9 μm were prepared, 19% poloxamer 407, 4% poloxamer 188 and 0.1% carbomer were used to prepare PTG. The phase transition temperature of thermosensitive gel was 30 to 35 ℃, there was a good linear relationship between in vitro release and gel dissolution. In the pharmacokinetic study, area under the curve (AUC_0-t) increased with the decrease of particle size. In general, the PTG prepared in this study can rapidly change into gel under human body temperature, provided with good adhesion. The release rate in vitro is closely related to the particle size, the release rate increased with the decrease of particle size. This study provides data support for preventing postoperative recurrence of cancer. The animal welfare and experimental process in this paper follow the regulations of the Animal Ethics Committee of the Academy of Military Medical Sciences.

The quality control and evaluation methods of Schizonepeta tenuifolia were established by HPLC fingerprint, multi index component content determination and chemical pattern recognition to provide basis for the quality control of medicinal materials. The chemical components of 25 batches of Schizonepeta tenuifolia panicle medicinal materials and decoction pieces collected were analyzed by high performance liquid chromatography, and the common pattern of fingerprint was established. A total of 22 common chromatographic peaks were calibrated, and their similarity was more than 0.9. The samples were divided into three categories according to different producing areas by cluster analysis. The results of principal component analysis and cluster analysis were consistent. Finally, five differential markers of different batches of Schizonepeta tenuifolia were selected by orthogonal partial least squares discriminant analysis. Through the identification of the reference substance, it was determined that peak 9 was hesperidin, peak 10 was rosmarinic acid, peak 13 was tilianin, peak 14 was quercetin, and peak 20 was pulegone. The quality evaluation method established in this study is stable and reliable, and is suitable for the quality control of Schizonepeta tenuifolia.

This study is to establish and validation in vivo models of moxifloxacin based on the theory of physiologically based pharmacokinetics (PBPK), and then to predict the distribution of moxifloxacin in human venous return and organ such as lung, spleen and so on. The efficacy of moxifloxacin and its pharmaceutical preparations were quantified by comparing the pharmacokinetic parameters with the minimum inhibitory concentration of related pathogenic bacterium. The results showed that the anti-infection efficacy of pharmaceutical moxifloxacin preparation in the corresponding organs was basically the same. The PBPK model of moxifloxacin preparations can be more accurately described the pharmacokinetic of anti-infective drugs in human, it is suitable for the efficacy evaluation of anti-infective drugs and provides a strong basis for the corresponding scientific research and scientific supervision.

This study evaluated the regulatory effect of curcumin on memory follicular T cells (mTf) in obese mice with ulcerative colitis on the basis of determining its effective treatment of ulcerative colitis in obese mice. Forty male leptin mutant (ob/ob) mice were randomly divided into control group, control + curcumin group, dextran sodium sulfate (DSS) group and DSS + curcumin group, with 10 mice in each group. Mice in the DSS group and the DSS + curcumin group were induced by DSS to establish chronic ulcerative colitis model, and mice in the control + curcumin group and the DSS + curcumin group were given curcumin (200 mg·kg^-1·d^-1) by intragastric administration. Mice were sacrificed under anesthesia, and colon mass index, colon length and other conditions were observed in each group. Pathological injury of colonic was performed after HE staining. The levels of memory follicular helper T cells (mTfh) and memory follicular regulatory T cells (mTfr) in spleen of mice were detected by flow cytometry. The expression levels of interleukin-10 (IL-10) and interleukin-17A (IL-17A) in colon tissue were detected by ELISA. The results showed that curcumin significantly increased the body weight and colon length of obese mice with colitis, and decreased the colon weight, colon mass index and pathological score (P < 0.05). Curcumin significantly reduced the levels of central memory follicular T cells (cmTf), mTfh1, mTfh17 cells and the content of pro-inflammatory cytokine IL-17A (P < 0.01). The levels of effector memory follicular T cells (emTf) and mTfr and the content of anti-inflammatory cytokine IL-10 were increased (P < 0.05, P < 0.01). Therefore, curcumin may treat colitis in obese mice by regulating the balance of mTf cell subsets.

A randomized, open, fasting, single dose, two sequence, two cycle and double cross administration trial design was adopted. Took the test or reference efavirenz tablets of 200 mg orally in a single time. The plasma concentration of efavirenz in healthy subjects was determined by LC-MS/MS. WinNonLin8.1 software was used to calculate the main pharmacokinetic parameters of efavirenz and to evaluate the bioequivalence. The main pharmacokinetic parameters within 72 h: t_max were 2.574 ± 0.871 and 2.808 ± 0.912 h; C_max were 1 586.732 ± 424.538 and 1 549.518 ± 366.086 ng·mL^-1; AUC_{0-72 h} were 28 464.672 ± 5 682.518 and 27 828.826 ± 5 082.487 h·ng·mL^-1; t_1/2 were 63.524 ± 26.037 and 58.748 ± 20.950 h; λ_z were 0.013 ± 0.006 and 0.013 ± 0.005 h^-1. The main bioequivalence indicators were as follows: The 90% confidence interval of C_max was 95.62%-107.15%, and the geometric mean ratio was 101.22%; The 90% confidence interval of AUC_{0-72 h} was 100.43%-104.38%, and the geometric mean ratio was 102.38%. The results showed that the main pharmacokinetic parameters of the test drug and the reference drug were similar, and the two preparations had bioequivalence. This human bioequivalence clinical study was approved by the drug clinical trials ethics committee of the Second Hospital of Anhui Medical University (ethics approval No.: YW2021-110).

Coronavirus (CoVs) is a widespread pathogen that can infect humans and animals to cause serious acute and chronic respiratory diseases. Among them, SARS-CoV broke out in 2003, MERS-CoV was discovered and spread widely in 2012, and SARS-CoV-2 emerged at the end of 2019. They all belong to β-coronavirus. Peptidomimetic inhibitors targeting coronavirus main proteases (M^pro, 3CL^pro) have attracted much attention because of their broad spectrum and strong antiviral efficacy. In this review, peptidomimetic inhibitors of coronavirus main protease were classified and summarized according to the different "warheads" in design strategy. And also, the molecular structures, biological activity and design ideas of the inhibitors were analyzed and discussed, which is aimed to provide useful reference for further design and development of coronavirus inhibitors.

Peptide drugs exhibit an irreplaceable role in clinics due to their high specificity, efficiency and low toxicity. At present, more than 80 peptide drugs have been approved for marketing with global sales exceeding $50 billion in 2019. However, with large molecular weights, high hydrophilicity and instability in digestive tract, oral peptide drugs encounter substantial physiological barriers leading to low oral bioavailability. Therefore, peptide drugs are mostly administered by parenteral routes. Although parenteral delivery of peptide drugs achieves high bioavailability, this is associated with inconvenience and discomfort, even causing severe side effects compared with the oral route possessing a high degree of patient compliance. Therefore, numerous studies concentrate on novel strategies to improve the oral bioavailability of peptide drugs. Some delivery technologies such as Eligen™ and Axcess™ have been successfully applied to the oral dosage form of therapeutic peptides and have accelerated relevant oral formulations for Food and Drug Administration (FDA) approval and clinical treatment. In this review, we focus on the oral peptide delivery, mainly summarizing the progress of recent strategies used to overcome oral barriers and the commercialization applications of related patents, which could facilitate the research and development (R & D) of clinical applications of oral delivery techniques for peptide drugs.

This study is to explore the mechanism of Xueshuantong improving cerebral microcirculation disorder through the combination of network pharmacology and experimental validation in vivo. Structural formulas of main Panax notoginseng saponins, including notoginsenoside R1, and ginsenoside Rg1, Re, Rb1 and Rd were obtained from Pubchem website and their potential targets were predicted by Swiss Target Prediction database. Potential molecular targets of brain microcirculation disorder were acquired from OMIM and GeneCards database. The overlapped molecular targets between the drug and disease were analyzed. Protein interaction analysis and topology maps were constructed through the STRING online analysis platform and Cytoscape software. Core action targets were selected. GO function and KEGG pathway were analyzed by DAVID database. Immunohistochemical method was used to examine the expression of platelet endothelial cell adhesion molecule-1 (CD31) in the ischemic cortex of middle cerebral artery occlusion and reperfusion (MCAO/R) rats. The levels of mRNA and protein expressions of core action targets in MCAO/R model rats′ brain microvessels were verified by RT-qPCR and Western blot. Based on network pharmacology, 242 targets of Xueshuantong, 425 targets of brain microcirculation disorder, and 35 overlapped targets were obtained. The potential key targets of Xueshuantong, protein kinase B (AKT1), vascular endothelial growth factor A (VEGFA), caspase 3 (CASP3), matrix metallopeptidase 9 (MMP-9), phosphatidylinositol-4, 5-bisphosphate 3-kinase catalytic subunit alpha (PIK3CA), signal transducer and activator of transcription 3 (STAT3) involved in the alleviation of cerebral microcirculation disorder were obtained by setting degree and betweenness centrality as screening parameters. Xueshuantong at the dose of 48 mg·kg^-1 was shown to significantly improve the injury of neurological behaviors, as well as the density and morphology of microvessels of MCAO/R model rats. Xueshuantong could down-regulate the mRNA levels of AKT1, MMP-9, and STAT3, increase the protein expression levels of CD31, phosphorylated AKT and phosphatidylinositol-4, 5-bisphosphate 3-kinase (PI3K), and the ratio of B-cell lymphoma 2/Bcl-2-associated X (Bcl-2/Bax), but decrease the protein expression levels of MMP-9, cleaved caspase-3 and phosphorylated STAT3. In summary, Xueshuantong could improve ischemic cerebral microcirculation disorder and thereby reduce nerve damage in ischemia-reperfusion rats by regulating signaling pathways related with PI3K, AKT, MMP-9, STAT3 and caspase-3 in microvessels. The study strictly adhered to all ethical protocols that experimental animals should follow in the course of medical research.