Article
Biochemistry & Molecular Biology
Juan Zou, Jianghai Ye, Chenliang Zhao, Jingjie Zhang, Yahua Liu, Lutai Pan, Kang He, Hongjie Zhang
Summary: Two undescribed ent-kaurene diterpenes, named guidongnins I and J, were isolated from Isodon rubescens. Compound 1 has an unprecedented structure with 23 carbons in the skeleton, while compound 2 is unique with two fused tetrahydrofuran rings. Their structures and absolute configurations were determined using spectroscopic and X-ray diffraction data. Guidongnin J exhibited cytotoxic activity against HepG2 cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Margarida Espadinha, Valentina Barcherini, Lidia M. Goncalves, Elies Molins, Alexandra M. M. Antunes, Maria M. M. Santos
Summary: The research team developed a series of enantiomerically pure tryptophanol-derived small molecules targeting human gastric adenocarcinoma cells, which showed selectivity for gastric cells over other types of cancer cells and were non-toxic in normal cells. The growth inhibition of AGS cells induced by these compounds is mediated by apoptosis.
Article
Chemistry, Medicinal
Run-Zhu Fan, Lin Chen, Tong Su, Wei Li, Jia-Luo Huang, Jun Sang, Gui-Hua Tang, Sheng Yin
Summary: In this study, a series of highly potent anti-TNBC small molecule compounds were isolated through bioassay-guided isolation, with 8,9-seco-ent-kaurane 6 showing promising activity and selectivity. The compounds may induce apoptosis, autophagy, and metastasis suppression in TNBC cells by inhibiting Akt, and demonstrate significant tumor growth suppression effects in vivo. These results suggest that these compounds hold potential for future development as novel anti-TNBC agents.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Dominika Radomska, Robert Czarnomysy, Dominik Radomski, Krzysztof Bielawski
Summary: This review discusses the research on the anticancer activity of selenium compounds, including the different classes of selenium compounds and their mechanisms of action, which are important for developing more effective cancer treatments.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Medicine, Research & Experimental
Guo Qiang Li, Shi Xiang Gao, Fu Han Wang, Le Kang, Ze Yao Tang, Xiao Dong Ma
Summary: Pyroptosis, a type of inflammatory cell death, can be regulated by Oridonin (Ori) through multiple pathways. Ori can inhibit the activation of pyroptosis by inhibiting caspase-1 and NLRP3, as well as activate pyroptosis by activating caspase-3 and caspase-8. Additionally, Ori regulates pyroptosis by promoting ROS accumulation and inhibiting the ncRNA and NLRP3 pathways. In summary, Ori has extensive anti-cancer effects by modulating pyroptosis.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Article
Biochemistry & Molecular Biology
Xiang Ni, Chen He, Yilin Jia, Xiuyuan Wu, Kunyu Zhou, Shengtao Xu, Jinyi Xu, Hong Yao
Summary: In this study, a series of novel spirolactone-type and enmein-type derivatives were designed and synthesized, and they exhibited better anti-tumor activities than the parent compound. Mechanistic studies revealed that the optimal compound could inhibit cell proliferation and induce apoptosis in K562 cells through multiple pathways. These results suggest that the most potent compound may serve as a potential anti-tumor agent and warrant further investigation.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Review
Oncology
Saeed Khoshnood, Hadis Fathizadeh, Foroogh Neamati, Babak Negahdari, Piyush Baindara, Mohd Azmuddin Abdullah, Mohammad Hossein Haddadi
Summary: Bacterial toxins have the potential to be used as effective anticancer agents, especially when used in combination with chemotherapy. Chimeric toxins, with their targeting moieties, can specifically kill cancer cells.
FRONTIERS IN ONCOLOGY
(2022)
Article
Chemistry, Inorganic & Nuclear
Muneebah Adams, Matthew P. Sullivan, Kelvin K. H. Tong, David C. Goldstone, Muhammad Hanif, Stephen M. F. Jamieson, Christian G. Hartinger
Summary: This study reports a series of platinum complexes that target DNA through coordination and/or alkylation, demonstrating strong antiproliferative activity. Investigations on their aqueous stability and reactivity with various small biomolecules were conducted. Furthermore, protein crystallography identified the binding site of platinum complex PtL3 with the model protein.
INORGANIC CHEMISTRY
(2021)
Article
Biology
Lotfi M. Aroua, Sadeq K. Alhag, Laila A. Al-Shuraym, Sabri Messaoudi, Jazem A. Mahyoub, Mohammad Y. Alfaifi, Wafa Mohammed Al-Otaibi
Summary: The condensation of (1H-benzimidazole-2-yl) methanamine with 2-hydroxy naphthaldehyde resulted in the formation of a Schiff base ligand (H2L) (1). This ligand was further reacted with metal salts (ZnCl2, CrCl3.6H2O, and MnCl2.4H2O) to obtain the corresponding metal complexes. The metal complexes exhibited promising activity against Escherichia coli and Bacillus subtilis, moderate activity against Aspergillus niger, and potent anticancer activity against human cell lines.
SAUDI JOURNAL OF BIOLOGICAL SCIENCES
(2023)
Review
Chemistry, Medicinal
Tathagata Pradhan, Ojasvi Gupta, Gurpreet Singh, Vikramdeep Monga
Summary: Aurora kinases, a family of regulatory proteins playing a crucial role in cell proliferation, have emerged as validated drug targets for anticancer drug discovery. The design and development of Aurora kinase inhibitors have been widely explored as potential anticancer agents, showing promising results in growth inhibition and apoptosis in tumor cells.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Abdur Rauf, Tareq Abu-Izneid, Anees Ahmed Khalil, Muhammad Imran, Zafar Ali Shah, Talha Bin Emran, Saikat Mitra, Zidan Khan, Fahad A. Alhumaydhi, Abdullah S. M. Aljohani, Ishaq Khan, Md Mominur Rahman, Philippe Jeandet, Tanweer Aslam Gondal
Summary: Berberine, a potential bioactive agent, shows remarkable health benefits and promising anticancer activity. It inhibits cancer cell proliferation, invasion, and metastasis through various mechanisms, and also plays a role in the early stages of cancer development. Despite its potential, pure berberine preparations for specific ailments are currently not approved, but research on its sources, extraction methods, pharmacokinetics, and proposed mechanisms of action related to its anticancer potential continues.
Article
Chemistry, Medicinal
Jin-Ling Huo, Shuai Wang, Xiao-Han Yuan, Bin Yu, Wen Zhao, Hong-Min Liu
Summary: Compound 6i showed potent anti-proliferative activity against MGC-803 with good safety in vivo. Mechanistic studies revealed that 6i induced apoptosis in MGC-803 cells through multiple pathways, suggesting its potential as a template for anti-cancer agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Valeria Stefanizzi, Antonella Minutolo, Elena Valletta, Martina Carlini, Franca M. M. Cordero, Anna Ranzenigo, Salvatore Pasquale Prete, Daniel Oscar Cicero, Erica Pitti, Greta Petrella, Claudia Matteucci, Francesca Marino-Merlo, Antonio Mastino, Beatrice Macchi
Summary: Metal-derived platinum complexes are commonly used in the treatment of solid tumors. However, the toxicity and resistance of these drugs necessitate the search for alternative compounds. Organotin compounds have shown potential in inhibiting cell growth and inducing cell death and autophagy. In this study, the biological activities of different organotin compounds were evaluated, and it was found that tributyltin compounds were more cytotoxic than cisplatin. Additionally, the mechanism of action was attributed to the inhibition of glucose uptake. Furthermore, the tumorigenicity of the cells influenced their susceptibility to the compounds, with highly tumorigenic cells being less affected.
Article
Biochemistry & Molecular Biology
Dilipkumar Pal, In-ho Song, Shrikant Dashrath Warkad, Keum-soo Song, Gyu Seong Yeom, Supriyo Saha, Pramod B. Shinde, Satish Balasaheb Nimse
Summary: This review presents the research advances on compounds containing indazole scaffolds as microtubule targeting agents based on articles published in the last two decades. Several compounds have shown potent microtubule inhibition and anticancer activity, with some of them having the lowest IC50 values observed in cell line studies.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Er-Jun Hao, Gong-Xin Li, Yu-Ru Liang, Ming-Sheng Xie, Dong-Chao Wang, Xiao-Han Jiang, Jia-Yi Cheng, Zhi-Xian Shi, Yang Wang, Hai-Ming Guo
Summary: The study designed, synthesized, and evaluated 103 novel acyclic nucleosides for their anticancer activities, with compound 9b showing promising inhibitory effects on colon cancer cells. All (R)-configured derivatives displayed stronger anticancer activity, with compound 9b inducing apoptosis and inhibiting colony formation. Importantly, compound 9b exhibited low systemic toxicity and inhibited tumor growth in a mouse model, suggesting it as a potential lead compound for future anticancer drug discovery.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Pharmacology & Pharmacy
Lei Zhang, Biwei Ye, Zhuo Chen, Zhe-Sheng Chen
Summary: Chemotherapy is an important method for treating cancer, but multi-drug resistance (MDR) is a major reason for its failure. Almost all anti-tumor drugs develop drug resistance over time, reducing their effectiveness in killing cancer cells. Chemoresistance can lead to rapid cancer recurrence and patient death.
ACTA PHARMACEUTICA SINICA B
(2023)
Article
Chemistry, Multidisciplinary
Shaowen Xie, Feiyan Zhan, Jingjie Zhu, Yuan Sun, Huajian Zhu, Jie Liu, Jian Chen, Zheying Zhu, Dong-Hua Yang, Zhe-Sheng Chen, Hong Yao, Jinyi Xu, Shengtao Xu
Summary: Hydrophobic tagging (HyT) is a potential therapeutic strategy for targeted protein degradation (TPD). In this study, norbornene was discovered as an unprecedented hydrophobic tag and successfully used to degrade ALK fusion protein and EZH2. The most promising degrader, Hyt-9, showed effective reduction of ALK levels without compensatory upregulation of ALK in vitro and exhibited significant tumor inhibition effect in vivo with moderate oral bioavailability. The discovery of novel hydrophobic norbornene tags shows promise for the future development of TPD technology.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Biochemistry & Molecular Biology
Jichao Chen, Yiping Duan, Kan Yang, Jiahe Wang, Junjie Yan, Chenglei Gu, Shanglong Wang, Zheying Zhu, E-Hu Liu, Jinyi Xu
Summary: Novel 9-N-substituted-13-alkylberberine derivatives were synthesized and showed improved anti-hepatocellular carcinoma (HCC) activities. The optimal compound 4d demonstrated strong cytotoxicity against HCC cells and cisplatin-resistant cells, while exhibiting low toxicity in normal cells. Mechanism studies revealed that 4d stabilized G-quadruplex DNA, leading to downregulation of c-MYC expression and inducing apoptosis through a ROS-promoted PI3K/Akt-mitochondrial pathway. Furthermore, 4d displayed good pharmacokinetic properties and inhibited tumor growth in a liver cancer xenograft mouse model without toxicity.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Editorial Material
Pharmacology & Pharmacy
Ting Wang, Zhe-Sheng Chen, Chen Shi, Liang Ouyang, Hongtao Xiao
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Materials Science, Multidisciplinary
Tingting Guo, Zixu Sa, Pengfei Wei, Yuxuan Jian, Xiang Chen, Zhesheng Chen, Jose Avila, Pavel Dudin, Zai-xing Yang, Xiufeng Song, Fengjing Liu, Shengli Zhang
Summary: Flexible broadband optoelectronic devices have great potential in various applications such as wearable optoelectronic systems, health care, and bio-imaging systems. This study demonstrates a high-performance photodetector based on Ta2NiSe5 nanosheets, which exhibit adjustable bandgap and excellent optical and electrical properties. The photodetector shows broad photodetection capability in the visible-infrared spectrum and retains its performance after bending cycles, indicating the great potential of 2D Ta2NiSe5 semiconductor in future wearable IR optoelectronic devices.
Review
Pharmacology & Pharmacy
Jia Fu, Wei Qin, Lu-Qi Cao, Zhe-Sheng Chen, Hui-Ling Cao
Summary: This review summarizes the applications and immobilization methods of receptor chromatography, which is widely used for high-throughput separation and accurate drug screening. The review focuses on screening active compounds in natural products, as well as the design and application of receptor chromatography in drug-receptor interactions.
DRUG DISCOVERY TODAY
(2023)
Review
Pharmacology & Pharmacy
Juan Jin, Yuhao Xie, Jin-Shi Zhang, Jing-Quan Wang, Shi-Jie Dai, Wen-fang He, Shou-Ye Li, Charles R. Ashby Jr, Zhe-Sheng Chen, Qiang He
Summary: Renal cell carcinoma (RCC) is the most prevalent type of kidney cancer, and targeted therapy with Sunitinib has become the main treatment option due to the lack of efficacy in radiation therapy and chemotherapy. However, many patients develop resistance to Sunitinib within months of therapy. In this review, we discuss the molecular mechanisms of Sunitinib resistance, strategies to overcome it, and potential predictive biomarkers.
DRUG RESISTANCE UPDATES
(2023)
Review
Pharmacology & Pharmacy
Jiaqi Xuan, Weiguo Feng, Jiaye Wang, Ruichen Wang, Bowen Zhang, Letao Bo, Zhe-Sheng Chen, Hui Yang, Leming Sun
Summary: The long-term use of antibiotics leading to drug resistance has become a major concern. As the problem worsens, infections caused by multiple bacteria are increasing rapidly and posing serious threats to human health. Antimicrobial peptides (AMPs) offer a promising alternative to traditional antibiotics as they exhibit strong antimicrobial activity and unique mechanisms against drug-resistant bacterial infections. Current research on AMPs focuses on integrating new technologies, such as modifying the amino acid structure and exploring different delivery methods. This article provides valuable insights into the properties, mechanisms, and advancements of AMPs in combating drug-resistant bacterial infections.
DRUG RESISTANCE UPDATES
(2023)
Article
Chemistry, Medicinal
Xinnan Li, Xiaotong Ze, Shengnan Zhou, Zhaoxin Hu, Chen He, Yilin Jia, Lihua Liu, Tao Wang, Junda Li, Shengtao Xu, Dong-Hua Yang, Zhe-Sheng Chen, Hequan Yao, Jinyi Xu, Hong Yao
Summary: A novel compound D26, identified through the exploration and optimization of the first-in-class POLRMT inhibitor IMT1B, exhibits a strong antiproliferative effect on cancer cells and decreases mitochondrial-related gene expression. Mechanism studies revealed that D26 arrests the cell cycle at the G1 phase without affecting apoptosis, mitochondrial depolarization, or reactive oxidative stress generation. In vivo studies further demonstrated that D26 has more potent anticancer activity than the lead compound IMT1B, and no toxicity was observed.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Mingying Wang, Xiaoyuan Chen, Ying Qu, Qingyinglu Ma, Huaqi Pan, Haonan Li, Huiming Hua, Dahong Li
Summary: A total of 25 brefeldin A-isothiocyanate derivatives were synthesized and tested. Most derivatives showed selectivity between HeLa and L-02 cells. In particular, derivative 6 exhibited potent antiproliferative activity against HeLa cells with no cytotoxic effects on L-02 cells. Mechanism studies revealed that derivative 6 induced cell cycle arrest at G1 phase and apoptosis through the mitochondrial-dependent pathway.
Article
Chemistry, Multidisciplinary
Longyang Liu, Chunlin Chen, Ping Liu, Jing Li, Zhanjun Pang, Jiayu Zhu, Zhongqiu Lin, Haixu Zhou, Yingying Xie, Tiancai Lan, Zhe-Sheng Chen, Zhaoyang Zeng, Weiyi Fang
Summary: In this study, the expression and function of MYH10 in serous ovarian cancer (SOC) were investigated. It was found that MYH10 is associated with the invasive capacity and cisplatin resistance of SOC cells. Further experiments revealed that MYH10 interacts with MYH9 to promote tumorigenesis, progression, and cisplatin resistance in SOC. Clinical samples also showed elevated expression of MYH10 in SOC samples, which correlated positively with MYH9 expression. Co-expression of MYH10+/MYH9+ was identified as an independent prognostic factor for SOC patient survival.
Editorial Material
Immunology
Jingxian Chen, Zhesheng Chen, Barkat Ali Khan, Kaijian Hou
FRONTIERS IN IMMUNOLOGY
(2023)
Review
Oncology
Letao Bo, Youyou Wang, Yidong Li, John N. D. Wurpel, Zoufang Huang, Zhe-Sheng Chen
Summary: The survival rate for pediatric cancers has significantly improved in recent years. Conventional chemotherapy is crucial, especially in low- and middle-income countries with limited access to advanced treatments. Despite the expanded FDA approval of chemotherapy drugs for children, patients still face side effects and multidrug resistance remains a major challenge. This review focuses on the severe side effects of pediatric chemotherapy, mechanisms of multidrug resistance, and potential therapeutic options offered by drug transporters in pediatric tumors.
Article
Chemistry, Medicinal
Zhaoxin Hu, Shengnan Zhou, Junda Li, Xinnan Li, Yang Zhou, Zheying Zhu, Jinyi Xu, Jie Liu
Summary: Based on a multitarget design strategy, a series of novel indanone-1-benzyl-1,2,3,6-tetrahydropyridin hybrids were identified for potential treatment of Alzheimer's disease (AD). The optimal compound A1 exhibited excellent dual AChE/MAO-B inhibition, moderate inhibitory effects on Aβ aggregation and antioxidant activity, and showed significant cognitive and spatial memory improvements in the AD mouse model induced by scopolamine.
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Sai Liu, Long Chen, Jinran Li, Yuan Sun, Yue Xu, Zhaoxing Li, Zheying Zhu, Xinuo Li
Summary: Alzheimer's disease (AD) is a neurodegenerative disorder characterized by the accumulation of amyloid-β plaques and neurofibrillary tangles. Asiaticoside (AS), derived from Centella asiatica, has been found to have anti-inflammatory and healing properties. Our study shows that AS can improve cognitive dysfunction and reduce neuroinflammation in AD mice by inhibiting microglia activation and proinflammatory factors. Mechanistic investigation suggests that AS may enhance cognitive function by inhibiting the p38 MAPK pathway and promoting synaptic repair.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)