Developing a Hetero-Trinuclear Erbium(III)-Copper(II) Complex Based on Apoferritin: Targeted Photoacoustic Imaging and Multimodality Therapy of Tumor.

For the integration of targeted diagnosis and treatment of tumor, we innovatively designed and synthesized a single-molecule hetero-multinuclear Er(III)-Cu(II) complex () and then constructed an @apoferritin (AFt) nanoparticle (NP) delivery system. and @AFt NPs not only provided an evident photoacoustic imaging (PAI) signal of the tumor but also effectively inhibited tumor growth by integrating photothermal therapy, chemotherapy, and immunotherapy. @AFt NPs improved the targeting ability and decreased the systemic toxicity of .

Developing a Ruthenium(III) Complex to Trigger Gasdermin E-Mediated Pyroptosis and an Immune Response Based on Decitabine and Liposomes: Targeting Inhibition of Gastric Tumor Growth and Metastasis.

To develop next-generation metal drugs with high efficiency and low toxicity for targeting inhibition of gastric tumor growth and metastasis, we not only optimized a series of ruthenium (Ru, III) 2-hydroxy-1-naphthaldehyde thiosemicarbazone complexes to obtain a Ru(III) complex () with remarkable cytotoxicity but also constructed a -decitabine (DCT)/liposome (Lip) delivery system (-DCT-Lip). The results showed that -DCT-Lip not only had a stronger capacity to inhibit gastric tumor growth and metastasis than -DCT but also addressed the co-delivery problems of -DCT and improved their targeting ability. Furthermore, we confirmed the mechanism of -DCT/-DCT-Lip inhibiting the growth and metastasis of a gastric tumor.

Developing a Gadolinium(III) Compound Based on Apoferritin for Targeted Magnetic Resonance Imaging and Dual-Modal Therapy of Cancer.

To integrate targeted diagnosis and treatment of cancer, we proposed to develop a gadolinium (Gd) agent based on the properties of apoferritin (AFt). To this end, we not only optimized a series of Gd(III) 8-hydroxyquinoline-2-carboxaldehyde-thiosemicarbazone compounds to obtain a Gd(III) compound (C4) with remarkable -weighted magnetic resonance imaging (MRI) performance and cytotoxicity to cancer cells but also constructed an AFt-C4 nanoparticle (NP) delivery system. Importantly, AFt-C4 NPs improved the targeting ability of C4 and showed enhanced MRI performance and tumor growth inhibition ratio relative to C4 alone.

Developing an Anticancer Platinum(II) Compound Based on the Uniqueness of Human Serum Albumin.

To develop the next-generation Pt drug with remarkable activity and low toxicity to maximally inhibit tumor growth, we optimized a Pt(II) thiosemicarbazone compound (C4) with remarkable cytotoxicity to SK-N-MC cells and then constructed a new human serum albumin-C4 (HSA-C4) complex delivery system. The results showed that C4 and the HSA-C4 complex have remarkable therapeutic efficiency and almost no toxicity; they induced apoptosis and inhibited tumor angiogenesis. This system showed potential as a practical Pt drug.

Developing a Gallium(III) Agent Based on the Properties of the Tumor Microenvironment and Lactoferrin: Achieving Two-Agent Co-delivery and Multi-targeted Combination Therapy of Cancer.

To develop a next-generation anticancer metal-based drug, realize the multi-targeted combination therapy of protein drug and metal-based drug for cancer, solve their co-delivery challenges, and improve their in vivo targeting ability, we proposed to develop a multi-targeted anticancer metal-based agent exploiting the properties of the tumor microenvironment (TME) and of lactoferrin (LF). To this end, we optimized a series of gallium (Ga, III) isopropyl-2-pyridyl-ketone thiosemicarbazone compounds to obtain a Ga compound (C4) with remarkable cytotoxicity and then constructed a new LF-C4 nanoparticle (LF-C4 NP) delivery system. In vivo studies showed that LF-C4 NPs not only had a greater capacity for inhibiting tumor growth than LF or C4 alone but also solved the co-delivery problems of LF and C4 and improved their targeting ability.

Current status of iridium-based complexes against lung cancer.

Lung cancer is one of the most common malignant tumors, with the highest mortality rate in the world, and its incidence is second only to breast cancer. It has posed a serious threat to human health. Cisplatin, a metal-based drug, is one of the most widely used chemotherapeutic agents for the treatment of various cancers.

Developing a Novel Indium(III) Agent Based on Human Serum Albumin Nanoparticles: Integrating Bioimaging and Therapy.

To effectively integrate diagnosis and therapy for tumors, we proposed to develop an indium (In) agent based on the unique property of human serum albumin (HSA) nanoparticles (NPs). A novel In(III) quinoline-2-formaldehyde thiosemicarbazone compound (C5) was optimized with remarkable cytotoxicity and fluorescence to cancer cells . An HSA-C5 complex NP delivery system was then successfully constructed.

Design of a novel Pt(II) complex to reverse cisplatin-induced resistance in lung cancer a multi-mechanism.

In order to develop a novel platinum (Pt) complex aiming to overcome cisplatin resistance, we synthesised a series of novel Pt complexes (C1-C6). These Pt complexes displayed potent cytotoxicity activity against resistant lung cancer cells (A549cisR) and efficiently inhibited tumour growth . The Pt complexes can target DNA, lead to DNA platination and cause cell cycle arrest in the S phase, thus impeding precise DNA synthesis.

Developing a Novel Indium(III) Agent Based on Liposomes to Overcome Cisplatin-Induced Resistance in Breast Cancer by Multitargeting the Tumor Microenvironment Components.

To overcome the resistance of cancer cells to platinum-based drugs and effectively suppress tumor growth, we developed a novel indium (In) agent based on liposomes (Lips). Thus, we not only obtained an In(III) thiosemicarbazone agent () with remarkable cytotoxicity by optimizing a series of In(III) thiosemicarbazone agents () but also successfully constructed a novel -loaded Lip () delivery system. Importantly, and results revealed that / overcame the tumor cell resistance and effectively inhibited MCF-7/DDP tumor growth.

Development of a multi-target anticancer Sn(ii) pyridine-2-carboxaldehyde thiosemicarbazone complex.

In this study, we proposed to design effective multi-target anticancer agents based on the chelation of nontoxic metals with ligands that possess anticancer activity. In total, five Sn(ii) pyridine-2-carboxaldehyde thiosemicarbazone complexes are synthesized and their activities are tested. Among these complexes, C5 is found to show the highest cytotoxicity on investigating their structure-activity relationships.