Preparation and biological evaluation of antibody targeted metal-organic framework drug delivery system (TDDS) in Her2 receptor-positive cells.

In this study, we designed and prepared a trastuzumab-coupled drug delivery system with pH response characteristics using mesoporous zeolitic imidazolate framework-8 (ZIF-8) as the carrier, Trastuzumab@ZIF-8@DOX. As results, the targeted drug delivery system (TDDS) ultimately showed high drug loading and good biocompatibility. The cumulative curve of drug release indicated that the early leakage levels were low under neutral pH conditions. However, under acidic pH conditions, there was an effective enhancement in drug release, indicating the presence of an explicit pH-triggered drug release mechanism. The results indicate that the prepared nanoparticles have the potential to serve as drug delivery systems, as they can release the loaded drug in a controlled manner. The results of cellular uptake tests showed that the uptake of the nanoparticles was greatly enhanced by the internalization mediated by the HER2 antibody. This finding indicates that the prepared nanoparticles can selectively target cancer cells that overexpress HER2. When the doxorubicin dose was 5 µg/ml, the survival rate of SK-BR-3 cells (cancer cells) was 47.75 %, and the survival rate of HaCaT cells (healthy cells) was 75.25 % when co-cultured with both cells. The therapeutic efficacy of Trastuzumab@ZIF-8@DOX was assessed on BALB/c nude mice to validate its potential as an effective drug delivery system for tumor inhibition in vivo. In conclusion, these findings demonstrate the specificity-targeted and pH-responsive nature of this smart drug delivery system, highlighting its promising prospects for efficient and controllable cancer treatment applications.

Vitexnegheteroin M, a new phenolic glycoside from Vitex negundo var. heterophylla.

The investigation of chemical constituents from the leaves and seeds of Vitex negundo var. heterophylla resulted in the isolation of one new phenolic glycoside, vitexnegheteroin M (1), together with eleven known compounds (2-12). Their structures were elucidated through extensive spectroscopic analyses including 1D, 2D NMR, HR-ESI-MS, and by comparison with the literature. Among them, compound 3 was obtained from the Vitex genus for the first time, and compounds 4-8, and 10-12 were isolated from this plant for the first time. Their anti-inflammatory activities were investigated by measuring nitric oxide (NO) production in lipopolysaccharide (LPS)-induced murine microglial BV-2 cells. As the obtained results, compound 9 showed the strongest inhibitory activity against LPS-stimulated NO production in BV-2 cells with IC50 value ranging from 8.65 ± 0.67 µM.

[Rapid identification and evaluation of Chinese materia medica quality by near infrared spectroscopy].

In recent years, the research object of traditional Chinese medicine(TCM) analysis has not just been limited to the common analysis technology, but focused on the key relationship between chemical ingredients and traditional functions, including Chinese material medica (CMM) attributes, chemical substance and biological function. Near infrared spectroscopy (NIR) analysis technology, due to its unique advantages, has been developed rapidly in the field of pharmaceutical analysis, especially in the TCM analysis. NIRS can reflect the global chemical information comprehensively, and this holistic approach can be used for the identification and cluster analysis of CMM. On the other hand, inspiring by the concept of TCM quality markers (Q-markers), by means of the activity screening assay of the key components from the CMM, multiple bioactive components quantitation can be achieved by the NIRS combined with chemometrics. Taking the full advantage of the NIR technology, a simple and reliable method for the fast evaluation of the quality of TCMs can be provided. Therefore, the progress and trend of modern TCM quality evaluation by NIR are discussed and prospected in the present review.

Synthesis and in vitro antitumor activity of 4(3H)-quinazolinone derivatives with dithiocarbamate side chains.

A series of 4(3H)-quinazolinone derivatives with dithiocarbamate side chains were synthesized and tested for their in vitro antitumor activity against human myelogenous leukemia K562 cells. Among them, (3,4-dihydro-2-methyl-4-oxoquinazolin-6-yl)methyl 4-(4-fluorophenyl)piperazine-1-carbodithioate 8q exhibited significant inhibitory activity against K562 cells with IC(50) value of 0.5 microM.