Shandong Mingren Freda Pharmaceutical Co. Ltd.

This study explored the efficacy of multielement analysis combined with element fingerprints and chemometrics to discriminate the geographical origins of asparagus (Asparagus officinalis L.). It investigated the potential health hazards of long-term intake of asparagus. 19 elements were set as variables, and the geographical origin discrimination analysis was conducted through element fingerprints and chemometrics. The principal component analysis (PCA) provided no clear regional delineations, while in orthogonal partial least square discriminant analysis (OPLS-DA) provided clear regional delineations. The final model has high predictive and cross-validation accuracies were maintained, underscoring the robustness and algorithm flexibility of elemental profiling for accurately identifying the geographical origins of asparagus. Health risk assessment based on the total target hazard quotient (THQ) value of heavy metals of Pb, Cd, As, Hg, Cu, Cr and cancer risk (CR) value of metals of Pb, Cd, As, Cr indicated that consumption of asparagus had certain risk to human health.

Two new stilbenoids, stemobenoids A (1) and B (2), together with three known compounds were obtained from the roots of Stemona tuberosa. The structures of the new compounds were established by extensive spectroscopic analysis, including HRMS, 1D and 2D NMR data. Compounds 1 and 2 displayed potent quinone reductase inducing activity in Hepa 1c1c7 cells.

Intra-articular injection of sinomenine (SN) is an effective treatment method for knee osteoarthritis (OA), however, SN could be eliminated quickly in vivo. To extend the residence time of SN in the joint cavity, the SN-hyaluronic acid (HA) conjugate was prepared previously. This study was performed to evaluate the pharmacokinetics and pharmacodynamics of SN-HA conjugate after intra-articular administration for the treatment of OA.

A high performance liquid chromatography-mass spectrometry (HPLC-MS/MS) method was established to determine the SN content in rat synovial fluid. One hundred and twenty rats were randomly divided into two groups, the SN-HA group and SN group. The concentration of SN in articular cavity washings was determined by HPLC-MS/MS. The protective effect on the cartilage was evaluated by histological evaluation in a model of papain induced rabbit knee osteoarthritis.

The method was validated with respect to sensitivity, specificity, linearity, precision, accuracy and especially the stability of analytes under various conditions, and was successfully applied in evaluating the pharmacokinetic profiles of SN in the joint cavity. Compared to the SN injection, the drug exposure in joint cavity was significantly increased following SN-HA injection administration, and AUC(0-12h) was 2.9 times of SN injection, mean residence time (MRT) was 1.88 times of SN injection. In the pharmacodynamic study, there was no significant difference between the SN-HA twice-treated group and SH/HA five-times mixture-treated group.

The local bioavailability of SN in joint cavity was improved significantly after conjugated with HA. The SN-HA conjugate showed good synergism effect of OA inhibition. The results indicated that the SN-HA conjugate seemed to be an effective therapeutic means for the treatment of OA.