Zhaoyou Deng

Objectives: Aspidopterys obcordata has been traditionally used by the Dai people in Xishuangbanna, China, for the prevention and treatment of renal calculi. This study aimed to investigate the inhibitory effect of A. tomentosa extracts on calcium oxalate stone formation. Methods: The extracts of A. tomentosa (EA) were obtained via 95% ethanol reflux extraction, followed by multi-polar solvent extraction and elution. The HK-2 cell injury model induced by calcium oxalate and the renal calculus mouse model established by intraperitoneal injection of glyoxylic acid were established to assess drug efficacy. EA intervention was performed to evaluate its effects on calcium oxalate crystal deposition, renal tubular injury, cell apoptosis, and serum creatinine (Scr) and blood urea nitrogen (BUN) levels. Furthermore, the potential mechanism underlying, particularly the regulation of PERK/ATF4/CHOP signaling pathway and endoplasmic reticulum stress-mediated apoptosis, was investigated. Results: EA treatment significantly reduced renal calcium oxalate crystal deposition, alleviated renal tubular injury, inhibited cell apoptosis, and decreased Scr and BUN levels. Mechanistically, the protective effects of EA were mediated by the downregulation of the PERK/ATF4/CHOP signaling pathway and the suppression of endoplasmic reticulum stress-mediated apoptosis. Conclusions: These findings provide experimental evidence supporting that A. tomentosa can be developed as a promising agent for the prevention of nephrolithiasis.

Postharvest processing plays an important role in improving the quality and storage stability of mature fresh Amomum villosum Lour. (A. villosum). We investigated the effects of seven common drying methods (electric baking drying (EBD), heat pump drying, sun drying after heat pump drying, shade drying, hot air drying, sun drying, and freeze drying) on the volatile components of Amomum villosum. To discriminate different samples and identify key markers, chemometric techniques, including principal component analysis (PCA) and orthogonal partial least squares discriminant analysis (OPLS-DA), were applied to Chromatography–Mass Spectrometer (GC-MS) data of 70 identified metabolites. As an unsupervised method, PCA was first utilized to observe the overall clustering tendency of 21 samples, showing clear dispersion among seven groups with a slight overlap in the samples from sun drying after heat pump drying and hot air drying. To improve discrimination accuracy, the OPLS-DA model was further established as a supervised method. Its reliability was verified by permutation tests and cross-validation, which confirmed the absence of overfitting (R² and Q² intercepts with the vertical axis were A. villosum, were determined by gas chromatography (GC) to identify the optimal drying method for fresh A. villosum. The results showed that the content of the quality markers in A. villosum obtained by the seven drying methods outclass the standards of the Chinese Pharmacopoeia.Comprehensively considering the experimental results and the convenience and operability of the drying process, EBD is the most suitable drying process of A. villosum for popularization and application. It is on account of the shortest drying time among the seven drying methods, which only took 21.63 h to complete the drying of fresh A. villosum. Besides that, the quality control parameters in the content of bornyl acetate, camphor, borneol and the essential oil of A. villosum obtained by EBD were far more than the standards stipulated in the pharmacopeia.

Cissampelos pareira is a medicinal plant with the potential effect of treating diabetes, commonly used by the Dai people in southern Yunnan Province. However, the wild resources of C. pareira are currently scarce. Endophytic fungi are a natural component of medicinal plants, while also serving as important repositories for discovering active natural products. In this study, we focused on 2-year-old C. pareira plants cultivated in potted and non-potted conditions. The community structure of endophytic fungi in the roots, stems, leaves, and flowers of two cultivation methods of C. pareira was investigated by using high-throughput sequencing (HTS) and traditional culture methods. Through HTS, we discover that the richness and diversity of endophytic fungi in C. pareira are associated with its growth environment and plant tissues. The endophytic fungi richness of C. pareira showed significant differences between the two habitats. And significant differences existed in the diversity of root endophytic fungi of C. pareira compared to those in the stems, leaves, and flowers. Additionally, the richness of endophytic fungi in the stems showed significant differences from that in the roots, leaves, and flowers. The results obtained using traditional culture methods revealed 69 endophytic fungi strains, classified into 2 phylum, 4 classes, 11 orders, 23 families, and 69 genera. The fermentation products of the obtained strains were evaluated for in vitro α-glucosidase inhibitory activity, and the results demonstrated that 11 endophytic fungi strains exhibited an inhibition rate exceeding 80%. The above-mentioned study can provide a theoretical basis for a comprehensive understanding of the community composition and diversity of endophytic fungi in C. pareira.

Liver injury caused by the irrational use of acetaminophen (APAP) represents a significant challenge in the field of public health. In clinical treatment, apart from N—acetylcysteine (NAC), the only approved antidote, there are extremely limited effective intervention measures for APAP-induced hepatotoxicity. Therefore, exploring novel liver-protecting drugs and elucidating their mechanisms of action is of great scientific significance and clinical value. Rosmarinic acid (RA), as a natural polyphenolic compound, has been proven to have significant antioxidant activity. Previous studies have shown that it has a protective effect against drug-induced liver injury. Nevertheless, the precise protective mechanism of RA in APAP-induced acute liver injury (AILI) has not been fully defined. This study was based on an AILI mouse model to systematically explore the liver-protecting effect of RA and its underlying molecular mechanisms. The research results showed that pretreatment with RA could notably mitigate liver pathological injury. It could decrease the activities of ALT and AST in the serum, suppress the liver inflammatory reaction, and reverse the decline in the levels of CAT, T-AOC, SOD, and GSH caused by APAP. Meanwhile, RA could enhance antioxidant defense capabilities by activating the Keap1/Nrf2/HO-1 signaling pathway, regulate the xCT/GPX4 axis to inhibit lipid peroxidation, and thus block the process of ferroptosis. In conclusion, this study confirmed that RA exerts a protective effect against AILI by regulating the Keap1/Nrf2/HO-1 axis to enhance antioxidant capacity and inhibit ferroptosis through the xCT/GPX4 pathway. Our research provides a theoretical basis for RA as a potential therapeutic agent for APAP-induced liver injury.

Drug-induced liver and kidney damage is an emergent clinical issue that should be addressed. Rosmarinic acid (RA) has obvious anti-inflammatory and antioxidant effects, so we evaluated the anti-inflammatory and antioxidant effects of RA pretreatment on serum and liver and kidney tissues of cisplatin (CP)-treated mice and explored the possible mechanisms. The results showed that RA pretreatment effectively downregulated the serum, liver, and kidney levels of ALT, AST, BUN, and CRE and the inflammatory factors IL-1β, IL-6, and TNF-α, and simultaneously enhanced the total antioxidant capacity of the liver and kidney. RA pretreatment significantly reduced the levels of MPO, MDA, and NO in liver and kidney tissue, inhibited the mRNA expression of IL-1β, IL-6, and TNF-α in liver and kidney tissue, activated the Nrf2 signaling pathway, and upregulated the mRNA expression of downstream target genes. Our findings show that RA could effectively prevent and alleviate acute liver and kidney injury caused by CP.

This study was designed to develop orally disintegrating/sustained-release praziquantel (PZQ) tablets using the hot-melt extrusion (HME) technique and direct compression, and subsequently evaluate their release in in vitro and in vivo pharmacokinetics. For the extrusion process, hypromellose acetate succinate (HPMCAS)-LG was the carrier of pure PZQ, with a standard screw configuration used at an extrusion temperature of 140 °C and a screw rotation speed of 100 rpm. Differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), powder X-ray diffraction (PXRD) and Fourier-transform infrared spectroscopy (FTIR) were performed to characterize the extrudate. Orally disintegrating/sustained-release praziquantel tablets (PZQ ODSRTs) were prepared by direct compression after appropriate excipients were blended with the extrudate. The release amount was 5.10% in pH 1.0 hydrochloric acid at 2 h and over 90% in phosphoric acid buffer at 45 min, indicating the enteric-coating character of PZQ ODSRTs. Compared with the pharmacokinetics of marketed PZQ tablets (Aipuruike^®) in dogs, the times to peak (T_max), elimination half-life (t_1/2λ) and mean residence time (MRT) were extended in PZQ ODSRTs, and the relative bioavailability of PZQ ODSRTs was up to 184.48% of that of Aipuruike^®. This study suggested that PZQ ODSRTs may have potential for the clinical treatment of parasitosis.