Synthesis, isolation, characterization of C3-C11 bridge-bond isomer of paclitaxel and its antitumor effect via inducing A549 cells pyroptosis.

During the chemical manufacturing control processing of new paclitaxel formulations, a photodegradation impurity called C3-C11 bridge-bond isomer appeared. Our work describes the synthesis, isolation, purification, and structural characterization methods using four spectroscopies: FT-IR, UV, NMR (1H and 13 C), and LC-MS. In addition, we discovered that the C3-C11 bridge-bond isomer can promote A549 cells pyroptosis, and increase pyroptosis-related proteins, including cleaved-caspase 3, cleaved-PARP, GSDME-N, and lactate dehydrogenase, thus making it anti-tumor effects. The study offered data suggesting that the C3-C11 bridge bond isomer may be used as an anti-tumour drug in the future.

Puerarin: A review of its mechanisms of action and clinical studies in ophthalmology.

BACKGROUND: Pueraria is the common name of the dried root of either Pueraria montana var. lobata (Willd.) Maesen & S.M.Almeida ex Sanjappa & Predeep (syn. Pueraria lobata (Willd.) Ohwi) or Pueraria montana var. thomsonii (Benth.) M.R.Almeida (syn. Pueraria thomsonii Benth.). Puerarin is a C-glucoside of the isoflavone daidzein extracted from Pueraria. It has been widely investigated to explore its therapeutic role in eye diseases and the molecular mechanisms. PURPOSE: To collect the available literature from 2000 to 2022 on puerarin in the treatment of ocular diseases and suggest the future required directions to improve its medicinal value. METHOD: The content of this review was obtained from databases such as Web of Science, PubMed, Google Scholar, China National Knowledge Infrastructure (CNKI), and the Wanfang Database. RESULTS: The search yielded 428 articles, of which 159 articles were included after excluding duplicate articles and articles related to puerarin but less relevant to the topic of the review. In eleven articles, the bioavailability of puerarin was discussed. Despite puerarin possesses diverse biological activities, its bioavailability on its own is poor. There are 95 articles in which the therapeutic mechanisms of puerarin in ocular diseases was reported. Of these, 54 articles discussed the various signalling pathways related to occular diseases affected by puerarin. The other 41 articles discussed specific biological activities of puerarin. It plays a therapeutic role in ophthalmopathy via regulating nuclear factor kappa-B (NF-ĸB), mitogen-activated protein kinases (MAPKs), PI3K/AKT, JAK/STAT, protein kinase C (PKC) and other related pathways, affecting the expression of tumour necrosis factor α (TNF-α), interleukin-1ß (IL-1ß), intercellular adhesion molecule-1 (ICAM-1), monocyte chemoattractant protein-1 (MCP-1), superoxide dismutase (SOD), B-cell lymphoma-2 (Bcl-2) and other cytokines resulting in anti-inflammatory, antioxidant and anti-apoptotic effects. The clinical applications of puerarin in ophthalmology were discussed in 25 articles. Eleven articles discussed the toxicity of puerarin. The literature suggests that puerarin has a good curative effect and can be used safely in clinical practice. CONCLUSION: This review has illustrated the diverse applications of puerarin acting on ocular diseases and suggested that puerarin can be used for treating diabetic retinopathy, retinal vascular occlusion, glaucoma and other ocular diseases in the clinic. Some ocular diseases are the result of the combined action of multiple factors, and the effect of puerarin on different factors needs to be further studied to improve a more complete mechanism of action of puerarin. In addition, it is necessary to increase the number of subjects in clinical trials and conduct clinical trials for other ocular diseases. The information presented here will guide future research studies.

The physiological functions and pharmaceutical applications of inulin: A review.

Inulin (IN), a fructan-type plant polysaccharide, is widely found in nature. The major plant sources of IN include chicory, Jerusalem artichoke, dahlia etc. Studies have found that IN possessed a wide array of biological activities, e.g. as a prebiotic to improve the intestinal microbe environment, regulating blood sugar, regulating blood lipids, antioxidant, anticancer, immune regulation and so on. Currently, IN is widely used in the food and pharmaceutical industries. IN can be used as thickener, fat replacer, sweetener and water retaining agent in the food industry. IN also can be applied in the pharmaceutics as stabilizer, drug carrier, and auxiliary therapeutic agent for certain diseases such as constipation and diabetes. This paper reviews the physiological functions of IN and its applications in the field of pharmaceutics, analyzes its present research status and future research direction. This review will serve as a one-in-all resource for the researchers who are interested to work on IN.

GGP modified daunorubicin plus dioscin liposomes inhibit breast cancer by suppressing epithelial-mesenchymal transition.

Tumor invasion and metastasis are the nodus of anti-tumor. Epithelial cell-mesenchymal transition is widely regarded as one of the key steps in the invasion and metastasis of breast cancer. In this study, GGP modified daunorubicin plus dioscin liposomes are constructed and characterized. GGP modified daunorubicin plus dioscin liposome has suitable particle size, narrow PDI, zeta potential of about -5 mV, long cycle effect, and enhanced cell uptake due to surface modification of GGP making the liposome could enter the inside of the tumor to fully exert its anti-tumor effect. The results of in vitro experiments show that the liposome has superior killing effect on tumor cells and invasion. In vivo results indicate that the liposome prolongs the drug's prolonged time in the body and accumulates at the tumor site with little systemic toxicity. In short, the targeted liposome can effectively inhibit tumor invasion and may provide a new strategy for the treatment of invasive breast cancer.

Development and characterization of octreotide-modified curcumin plus docetaxel micelles for potential treatment of non-small-cell lung cancer.

We prepared octreotide (OCT)-modified curcumin plus docetaxel micelles to enhance active targeting and inhibit tumor metastasis by destroying vasculogenic mimicry (VM) channels. Soluplus was applied as an amphiphilic material to form micelles via film dispersion. The cytotoxic effects, active cellular targeting, and inhibitory effects on metastasis were systematically evaluated in vitro using A549 cells, and in vivo antitumor effects were evaluated using xenograft tumor-bearing mice. In vitro assays indicated that the OCT-modified curcumin plus docetaxel micelles showed robust cytotoxicity on A549 cells and effectively inhibited VM channels and tumor metastasis. Studying the mechanism of action indicated that OCT-modified curcumin plus docetaxel micelles downregulated MMP-2 and HIF-1α. In vivo assays indicated that OCT-modified curcumin plus docetaxel micelles increased drug accumulation at tumor sites and showed obvious antitumor efficacy. The developed OCT-modified curcumin plus docetaxel micelles may offer a promising treatment strategy for non-small-cell lung cancer.