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Abstract: 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 development of anticancer agents.

Aims: The aim of this study is to find the anticancer lead compounds or drug candidates from Chinese Traditional Plant Medicine of Ajuga decumbens Thunb. Background: Ajuga decumbens Thunb. has been used in clinical for a long time in China and was selected in “Chinses Pharmacopoeia” (part I in 1977) for its wide spectrum biological activities: such as anticancer, antioxidant, antifeedant, antibacterial, anti-inflammatory, antihyperlipidemic, anti-cholinesterase and cytotoxicity activities. However, there are relatively fewer studies of Ajuga decumbens Thunb. that have been carried out till now. For some years, our research group focused on the discovery of new anticancer agents, so we studied the chemical compositions of Ajuga decumbens Thunb., planted in Pingtan island of Fujian Province, to discover new anticancer lead compounds or candidates from this Chinese Traditional Plant Medicine. Methods: The dichloromethane (DCM) extract was obtained in this work, and then this extract was used for silica gel column chromatography to obtain different polar fractions. Several similar fractions were combined according to TLC or HPLC analysis. The combined fractions were isolated by preparative TLC or preparative HPLC to obtain the pure compounds and HPLC was used to detect the purity. All isolated compounds were determined by NMR (1HNMR, 13CNMR, DEPT, HMBC, HSQC, 1H-1H COSY and NOESY), HRESIMS and single crystal X-ray diffraction methods. The in vitro anticancer activity was evaluated using CCK8 method. Result: Seven compounds [three new compounds 1-3； and four known compounds (Ajugacumbins A, Ajugacumbin B, Ajugamarin A2 and Ajugamarin A1)] were isolated from Ajuga decumbens Thunb. in this work, and their structures were confirmed. The biological evaluation showed that 3 and Ajugamarin A1 exhibited potent in vitro anticancer activity both against A549 cell lines with IC50s=71.4 μM and 76.7 μM; and against Hela cell lines with IC50s=71.6 mM and 5.39×10-7 μM, respectively. Conclusion: Compounds (3 and Ajugamarin A1) can be regarded as the lead compounds for the development of anticancer agents.

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. 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. 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 148.3μM for 24hs and 35.94μM for 48hs, respectively; compound 1 displayed significant cytotoxic potential against MCF-7 cell lines with IC50 value of 38.5μM for 24hs; while compound 3 and 4 displayed potent cytotoxic effects against MCF-7 cell lines with IC50 values of 161.1μM and 243.7μM for 48hs, 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.

Lysimachia capillipes Hemsl. is an annual flowering plant, mainly distributed in some parts of Asia. In the early 1970s, it was discovered by the folk of Le'an county, Jiangxi province. Lysimachia capillipes Hemsl., contains many bioactive components (flavonoids, saponins, volatile oils, organic acids, etc.) and has a wide spectrum of pharmacological activities. This plant medicine was used in the treatment of cold cough, asthma, rheumatism, pain, irregular menstruation, neurasthenia, restoring deficiency, expelling roundworm, anti-tumor, etc. in Chinese folk. In this mini-review, the progress on the chemical constituents and biological activities of Lysimachia capillipes Hemsl., was comprehensively summarized by searching the CNKI, PubMed, Web of Science, Scopus, and Google Scholar databases using “Lysimachia capillipes Hemsl.” or “Manshanxiang” as the keywords. This article may provide a reference for researchers for further study of Lysimachia capillipes Hemsl.

Abstract: 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.

Cu2O is a p-type direct bandgap semiconductor with a band gap of 2~2.2 eV, which has excellent visible light absorption and utilization. However, slow charge transfer and poor stability hinder its practical application. In this paper, a facile electrodeposition approach successfully synthesized the heterostructure of p-Cu2O and n-Cu2O. The protective layer of n-Cu2O on the surface of p-Cu2O nanoparticles forms a p/n heterojunction. Due to the p/n heterojunction, the PEC performance of p/n-Cu2O is enhanced significantly. The charge separation efficiency of photogenerated electron/hole pairs in p/n-Cu2O is greatly improved. Therefore, p/n-Cu2O shows superior photoelectrochemical (PEC) CO2 reduction reaction (CO2RR) efficiency when used as a photocathode.

Psoriasis is an incurable autoimmune disease that affects 2-3% of the world's population. Limited understanding of its pathogenesis hinders the development of therapies for the disease. Herein, we reported that N-acylethanolamine acid amidase (NAAA), a cysteine enzyme that catalyzes the hydrolysis of fatty acid ethanolamides (FAEs), was upregulated in psoriasis patients and imiquimod (IMQ)-induced mouse model of psoriasis. The upregulated NAAA contributes to the progression of psoriasis via enhancing dendritic cell (DCs) maturation. Transgenic expression of NAAA in mice accelerated the development of psoriasis, whereas genetic ablation of NAAA or local administration of NAAA inhibitor F96 ameliorated psoriasis. NAAA expressed in dendritic cells (DCs), but not in macrophages, T cells, or keratinocytes plays a critical role in psoriasis development. In addition, the results showed that NAAA degrades palmitoylethanolamide (PEA) and reduces PEA-PPARα-mediated dissociation of NF-κB p65 from Sirtuin 1 (SIRT1), subsequently, repressing the acetylation of p65 and down-regulating IL10 production. The decreased IL10 then leads to the maturation of DCs, thus promoting the development of psoriasis. These results provide new insights into the pathophysiological mechanism of psoriasis and identify NAAA as a novel target for the treatment of psoriasis.

Aims: To develop new anticancer agents based on ferrocene core. Background: Cancer has become the major cause of human death globally. The death caused by cancer mainly focuses on lung cancer, breast cancer, liver cancer, carcinoma of the colon, and rectum. Some small molecular inhibitors have been authorized by FDA for the treatment of cancer and several candidates are in different phases of clinical trials. However, cancer chemotherapy is still highly inadequate. Thus, it is indispensable to develop novel anticancer agents. Objective: Based on the previous good results, twelve novel structures of ferrocene formates bearing isoxazole moiety (3a-3l) were synthesized in this work for the development of anticancer agents. Methods: The target compounds were synthesized using Ferrocenecarboxylic acid and 3-[(R)-substitutedphenyl]- isoxazole-5-methanol catalyzed by DCC and DMAP. The structures of target compounds were characterized by 1H NMR, 13C NMR, MS, HR-MS and XRD. Then, their preliminarily in vitro cytotoxicity against A549, HCT116, and MCF-7 cell lines was evaluated using the MTT method. Results: The results showed that most compounds exhibited moderate cytotoxicity against A549, HCT116, and MCF-7 cell lines compared with the positive control gefitinib. However, (3b, 3c, 3e, 3j, and 3k) simultaneously exhibited stronger inhibitory activity against A549, HCT116, and MCF-7 cell lines, which can be regarded as promising metal-based lead compounds for the development of anticancer agents. Conclusion: In this work, twelve new structures of ferrocene derivatives containing isozaole moiety were synthesized and their cytotoxicity against 549, HCT116, and MCF-7 cell lines was evaluated. (3b, 3c, 3e, 3j, and 3k) simultaneously exhibited stronger inhibitory activity towards A549, HCT116, and MCF-7 cell lines, which can be regarded as promising metal-based lead compounds for the development of anticancer agents.