Sesquiterpenoids from aged Artemisia argyi and their 3D-QSAR for anti-HBV activity.

Artemisia argyi Levl. Et Vant, commonly known as "Chinese Mugwort," has been utilized in traditional Chinese medicine and cuisine for centuries. Aged Chinese Mugwort has been uncovered to possess superior quality and safety, and its ethyl acetate extract has been found to exhibit anti-hepatitis B virus (HBV) activity. In this study, twenty-five sesquiterpenoids were isolated and characterized from three-year-aged A. argyi. Among them, 14 previously undescribed sesquiterpenoids (1-14), featuring double bond oxidation or ring opening. It is hypothesized that during the aging process, sesquiterpenes undergo oxidative transformation of their double bonds to form alcohols due to external factors and inherent properties. The anti-HBV activity and cytotoxicity of all compounds were assessed in vitro using HepG 2.2.15 cells, and their structure-activity relationships were analyzed through three-dimensional quantitative structure-activity relationship (3D-QASR) techniques. The α-methylene-γ-lactone sesquiterpenoid derivatives were discovered to have potent inhibitory activity against HBV. This research may broaden the potential applications of Chinese Mugwort and offer further guidance for its development and utilization as functional food or traditional Chinese medicine.

Surgical smoke: A hidden killer in the operating room.

Surgical smoke is a byproduct of aerosols containing several components produced by energy equipment. The characteristics of surgical smoke components produced by different types of tissues or using different kinds of energy devices vary. For example, the average diameter of smoke particles produced by electrocautery is smaller, and the possibility of viable cells and pathogens in surgical smoke produced by an ultrasonic knife is higher. According to the characteristics of its composition, surgical smoke may be an important risk factor affecting the health and safety of operating room staff and patients. The use of surgical masks, suction devices and portable smoke evacuation systems can reduce this risk to some extent. However, most operating room staff members do not implement corresponding measures to protect themselves. In this paper, the characteristics of surgical smoke and the research progress in protective measures are briefly reviewed.

The Effects of Smad3 on Adrenocorticotropic Hormone-Secreting Pituitary Adenoma Development, Cell Proliferation, Apoptosis, and Hormone Secretion.

OBJECTIVE: Down-regulation of mothers against decapentaplegic homolog 3 (Smad3) results in the formation of tumors both in vivo and in vitro. However, little is known about the effect of Smad3 on adrenocorticotropic hormone-secreting pituitary adenomas (ACTH-PAs). Our objective was to study the expression and effect of Smad3 in ACTH-PAs and its possible mechanisms. METHODS: Smad3, COOH-terminally phosphorylated mothers against decapentaplegic homolog 3 (pSmad3), and mothers against decapentaplegic homolog 2 proteins (Smad2) were detected in samples from 5 normal anterior pituitaries and 18 ACTH-PAs by Western blot and immunohistochemical analysis. Then, Smad3 expression was up-regulated by Smad3-CMV plasmid or down-regulated by small interfering RNA in ACTH tumor cells (AtT-20) in vitro. Cell proliferation, apoptosis, ACTH level, and pSmad3, B-cell lymphoma/lewkmia-2 (BCL-2), and pro-opiomelanocortin (POMC) protein expression in the AtT-20 cells were measured to investigate the antitumor effects of Smad3. RESULTS: Reduced expression of Smad3 and pSmad3 but unchanged Smad2 levels were found in ACTH-PAs compared with normal pituitaries. In vitro, the overexpression of Smad3 inhibited cell proliferation, promoted cell apoptosis, and decreased ACTH secretion; in contrast, Smad3 knockdown increased cell proliferation and decreased cell apoptosis but had no significant effect on ACTH secretion. At the same time, overexpression of Smad3 increased pSmad3 but inhibited BCL-2 and POMC protein expression. On the contrary, underexpression of Smad3 inhibited pSmad3 but promoted BCL-2 and POMC protein expression. CONCLUSIONS: Smad3 is underexpressed in ACTH-PAs. Reversing the expression of Smad3 in AtT-20 cells could suppress cell growth, promote tumor apoptosis, and decrease ACTH secretion. Tumor suppression was possibly mediated by the promotion of pSmad3 and the reduction of BCL-2 and POMC expression.

Optimization of PLGA nanoparticles formulation containing L-DOPA by applying the central composite design.

The aim of this work was to prepare L-DOPA loaded poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles by a modified water-in-oil-in-water (W(1)/O/W(2)) emulsification solvent evaporation method. A central composite design was applied for optimization of the formulation parameters and for studying the effects of three independent variables: PLGA concentration, polyvinyl alcohol (PVA) concentration and organic solvent removal rate on the particle size and the entrapment efficiency (response variables). Second-order models were obtained to adequately describe the influence of the independent variables on the selected responses. The analysis of variance showed that the three independent variables had significant effects (p < 0.05) on the responses. The experimental results were in perfect accordance with the predictions estimated by the models. Using the desirability approach and overlay contour plots, the optimal preparation area can be highlighted. It was found that the optimum values of the responses could be obtained at higher concentration of PLGA (5%, w/v) and PVA (6%, w/v); and faster organic solvent removal rate (700 rpm). The corresponding particle size was 256.2 nm and the entrapment efficiency was 62.19%. FTIR investigation confirmed that the L-DOPA and PLGA polymer maintained its backbone structure in the fabrication of nanoparticles. The scanning electron microscopic images of nanoparticles showed that all particles had spherical shape with porous outer skin. The results suggested that PLGA nanoparticles might represent a promising formulation for brain delivery of L-DOPA. The preparation of L-DOPA loaded PLGA nanoparticles can be optimized by the central composite design.

[Molecular cloning of two Rhipicephalus haemaphysaloides haemaphysaloides cathepsin L-like cysteine proteinase gene].

Ticks are obligate ectoparasites and vectors of arboviruses, vickettsiate, spirochetes and parasitil protozoa of humans and domestic animals. Immunological protection of mammalian hosts against tick infestation has been proposed as the most sustainable alternative tick control method to the current use of acaricides. The success of this method is dependent on the identification of key molecules for use as tick vaccine antigens. Proteolytic enzymes are involved in a wide range of cellular processes, thus they can be considered as good target antigens for a tick vaccine. In the present study, we used rapid amplification of cDNA ends protocol and primers that were designed based on the consensus amino acid motifs flanking present in all papain-like cysteine proteinases, to amplify, sequence and characterize two Rhipicephalus haemaphysaloides haemaphysaloides cathepsin L-like cysteine proteinases, named as cysA and cysB. The full length of cysA is 1168bp, encoding a 332 amino acid residue polypeptide with 36.33kD predicted molecular mass; the full length of cysB is 1153bp, encoding a 335 amino acid residue polypeptide with 37.56kD predicted molecular mass. The consensus amino acid motifs flanking presence in both deduced amino acid sequences. And both genes show high sequence homology to other tick cathepsin L-like cysteine proteinase, so they were identified as members of the cysteine proteinase gene family. Expression analysis by RT-PCR revealed that cysA and cysB were expressed differently in different periods of tick development.