Mesoporous Oxidized Mn-Ca Nanoparticles as Potential Antimicrobial Agents for Wound Healing.

Managing chronic non-healing wounds presents a significant clinical challenge due to their frequent bacterial infections. Mesoporous silica-based materials possess robust wound-healing capabilities attributed to their renowned antimicrobial properties. The current study details the advancement of mesoporous silicon-loaded MnO and CaO molecules (HMn-Ca) against bacterial infections and chronic non-healing wounds. HMn-Ca was synthesized by reducing manganese chloride and calcium chloride by urotropine solution with mesoporous silicon as the template, thereby transforming the manganese and calcium ions on the framework of mesoporous silicon. The developed HMn-Ca was investigated using scanning electron microscopy (SEM), transmission electron microscope (TEM), ultraviolet-visible (UV-visible), and visible spectrophotometry, followed by the determination of Zeta potential. The production of reactive oxygen species (ROS) was determined by using the 3,3,5,5-tetramethylbenzidine (TMB) oxidation reaction. The wound healing effectiveness of the synthesized HMn-Ca is evaluated in a bacterial-infected mouse model. The loading of MnO and CaO inside mesoporous silicon enhanced the generation of ROS and the capacity of bacterial capture, subsequently decomposing the bacterial membrane, leading to the puncturing of the bacterial membrane, followed by cellular demise. As a result, treatment with HMn-Ca could improve the healing of the bacterial-infected wound, illustrating a straightforward yet potent method for engineering nanozymes tailored for antibacterial therapy.

Four New Unusual Pentacyclic Triterpenoids from the Roots of Jasminum sambac (L.) Ait.

Four new unusual pentacyclic triterpenoids (1-4) were isolated from the roots of Jasminum sambac (L.) Ait. Their structures were elucidated by 1D and 2D NMR analysis, single-crystal X-ray diffraction and HRESIMS.

Chemical Constituents from the Roots of Jasminum sambac (L.) Ait. and their Cytotoxicity to the Cancer Cell Lines.

BACKGROUND: The roots of J. sambac is the Traditional Chinese Medicine (TCM) with analgesic and anesthetic effects. However, relatively fewer studies on the chemical compositions and the biological activities of the roots of J. sambac have been carried out till now. We studied the chemical compositions of the roots of J. sambac planted in Fujian Province to discover new compounds from this TCM to develop new drugs or drug candidates. AIM: This work aims to find the new compounds from the roots of Jasminum sambac (L.) Ait. (J. sambac) for the development of new drugs or drug candidates. METHODS: The dichloromethane (DCM) extract was selected to isolate over silica gel column chromatography to obtain different polar fractions. Several similar fractions were combined according to Thin Layer Chemotherapy (TLC) or High-Performance Liquid Chromatography (HPLC) analysis. The combined fractions were reisolated by silica gel column chromatography, preparative TLC or HPLC to obtain nine pure compounds (1-9). The purity of the isolated compounds was detected by HPLC, and their structures were determined by 1D, 2D NMR, and HRESIMS analysis. The in vitro anticancer activity was evaluated using Cell Counting Kit-8 (CCK8) method. RESULTS: Nine compounds were isolated in this work. Compounds (1-3) are new compounds, while compounds (4-9) were isolated for the first time from the roots of J. sambac. Their structures were elucidated by 1D, 2D NMR, and HRESIMS analysis. The biological evaluation showed that compound 7 exhibited potent cytotoxic efficacy against MCF-7 cell lines with IC50 values of 148.3 µM for 24 hs and 35.94 µM for 48 hs, respectively; compound 1 displayed significant cytotoxic potential against MCF-7 cell lines with IC50 value of 38.5 µM for 24 hs; while compound 3 and 4 displayed potent cytotoxic effects against MCF-7 cell lines with IC50 values of 161.1 µM and 243.7 µM for 48 hs, respectively. CONCLUSION: We discovered new compounds from the roots of J. sambac. and several compounds exhibited potent cytotoxity to MCF-7 cell lines. This work encourages us to further study the chemical constituents and their biological activities from the roots of J. sambac.

Isolation, Structural Elucidation of a New Triterpenoid from the Roots of Jasminum sambac (L.) Ait. with Potent Cytotoxicity against MCF-7 Cell Lines.

A new triterpenoid was isolated from the roots of Jasminum sambac (L.) Ait. Its structure was elucidated by 1D and 2D NMR analysis, single crystal X-ray diffraction, and HRESIMS. This compound exhibited potent in vitro anticancer efficacy against MCF-7 cell lines with IC50's of 193.5 µM for 24 h and 154.6 µM for 48 h.

A Review on Shikonin and Its Derivatives as Potent Anticancer Agents Targeted against Topoisomerases.

The topoisomerases (TOPO) play indispensable roles in DNA metabolism, by regulating the topological state of DNA. Topoisomerase I and II are the well-established drug-targets for the development of anticancer agents and antibiotics. These drugs-targeting enzymes have been used to establish the relationship between drug-stimulated DNA cleavable complex formation and cytotoxicity. Some anticancer drugs (such as camptothecin, anthracyclines, mitoxantrone) are also widely used as Topo I and Topo II inhibitors, but the poor water solubility, myeloma suppression, dose-dependent cardiotoxicity, and multidrug resistance (MDR) limited their prolong use as therapeutics. Also, most of these agents displayed selective inhibition only against Topo I or II. In recent years, researchers focus on the design and synthesis of the dual Topo I and II inhibitors, or the discovery of the dual Topo I and II inhibitors from natural products. Shikonin (a natural compound with anthraquinone skeleton, isolated from the roots of Lithospermum erythrorhizon) has drawn much attention due to its wide spectrum of anticancer activities, especially due to its dual Topo inhibitive performance, and without the adverse side effects, and different kinds of shikonin derivatives have been synthesized as TOPO inhibitors for the development of anticancer agents. In this review, the progress of the shikonin and its derivatives together with their anticancer activities, anticancer mechanism, and their structure-activity relationship (SAR) was comprehensively summarized by searching the CNKI, PubMed, Web of Science, Scopus, and Google Scholar databases.

An Overview of Dihydroartemisinin as a Promising Lead Compound for Development of Anticancer Agents.

Dihydroartemisinin (DHA) is a derivative of artemisinin, which firstly showed higher antimalarial activity. Over the years, DHA has also been discovered to exhibit higher anticancer efficacy without adverse side effects. Although some shortcomings have been discovered during biological evaluation (such as poor aqueous solubility, short half-life, and initial burst release effect), several attempts have been developed to overcome these shortcomings. For example, appropriate delivery techniques were used to improve its anticancer efficacy. In this minireview, we focused on summarizing the anticancer mechanisms, anticancer efficacy of free DHA and in combination therapies, hybrids, and nanoparticle formulations, which will provide adequate insights for its clinical use as anticancer agents, and on the design and synthesis of DHA derivatives for the development of anticancer agents.

Isolation, structural elucidation of new phytoecdysteroids from Ajuga decumbens Thunb.

Five new phytoecdysteroids (1, 2, 3, 4, and 5) were isolated from Ajuga decumbens Thunb. planted at Pingtan island of Fujian Province. Their structures were elucidated by NMR(1H NMR, 13C NMR, DEPT, HMBC, HSQC, 1H-1H COSY, ROESY), and HRESIMS. Especially, compound 2 is the epimer of Cyasterone, which was directly confirmed using single crystal X-ray diffraction analysis.

The Progress of the Anticancer Agents Related to the Microtubules Target.

Anticancer drugs based on the microtubules target are potent mitotic spindle poison agents, which interact directly with the microtubules, and were classified as microtubule-stabilizing agents and microtubule-destabilizing agents. Researchers have worked tremendously towards the improvements of anticancer drugs, in terms of improving the efficacy, solubility and reducing the side effects, which brought about advancement in chemotherapy. In this review, we focused on describing the discovery, structures and functions of the microtubules as well as the progress of anticancer agents related to the microtubules, which will provide adequate references for researchers.