Review
Pharmacology & Pharmacy
Yan Li, Yu-Feng Du, Feng Gao, Jin-Bu Xu, Ling-Li Zheng, Gang Liu, Yu Lei
Summary: Microtubule stabilizers are effective agents for cancer treatment, and taccalonolides, as a novel class of microtubule-stabilizing agents, not only possess similar activity but also reverse multi-drug resistance. Taccalonolides have gained attention due to their structural diversity, unique mechanism of action, and low toxicity.
FRONTIERS IN PHARMACOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Tingting Liang, Lu Lu, Xueting Song, Jianguo Qi, Jianhong Wang
Summary: This article reviews the combinations of microtubule targeting agents (MTAs) with other anticancer drugs to overcome toxicities, resistance, and improve treatment efficacy for cancer. It provides helpful information for combination therapy based on MTAs.
BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER
(2022)
Article
Biochemistry & Molecular Biology
Weiguo Xiang, Tasdique M. Quadery, Ernest Hamel, Lerin R. Luckett-Chastain, Michael A. Ihnat, Susan L. Mooberry, Aleem Gangjee
Summary: A series of methoxy naphthyl substituted cyclopenta [d]pyrimidine compounds were designed and synthesized to study the influence of 3-D conformation on microtubule depolymerizing and antiproliferative activities. The NOESY studies showed that the rotational flexibility and conformational dissimilarity between two compounds, 4 and 5, led to significant differences in biological activities. Compound 5 exhibited potent microtubule depolymerizing effects and strong antitumor activity, making it a potential preclinical candidate for further studies.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Jiayu Song, Shuran Liu, Yuan Ren, Xiaohui Zhang, Baojin Zhao, Xinxu Wang, Yunlan Li
Summary: The antitumor effects of four different organotin benzohydroxamate compounds (OTBH) were studied in vitro and in vivo, showing that they all exhibited notable antitumor activity. The study also found that the electronegativity and structural symmetry of the substituents influenced their biochemical capacity against cancer. Molecular docking analysis suggested that the colchicine-binding site was the target for these compounds' action, which was further confirmed by experimental competition and inhibition tests. These derivatives have potential for developing microtubule-targeting agents (MTAs) that disrupt cancer cell microtubule networks, halt mitosis, and induce apoptosis.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Huiting Zhao, Ling Li, Jin Liu, Ruiyao Mai, Jingxuan Chen, Jianjun Chen
Summary: K20 is a potential KRas G12C inhibitor with high anti-proliferative potency against cancer cells with KRas G12C mutation, displaying better selectivity and potential tumor-suppressing effects.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Zhonghua Li, Yong Yuan, Pan Wang, Zijuan Zhang, Huifen Ma, Yiran Sun, Xiaowei Zhang, Xiaofang Li, Yonghui Qiao, Feiyu Zhang, Yunfang Su, Junying Song, Zhishen Xie, Lixin Li, Liying Ma, Jinlian Ma, Zhenqiang Zhang
Summary: In this study, a novel pool of TCP derivatives with triazolopyrimidine as a privileged heterocyclic motif was reported, which showed nanomolar inhibitory potency against LSD1 and broad-spectrum antiproliferative activities against tumor cells. Compound 9j was identified as a selective and cellular active inhibitor, and showed remarkable efficacy in reducing tumor size and extending survival in a mouse model.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Medicine, General & Internal
Xi Jiang, Zhongxiu Jiang, Min Jiang, Yan Sun
Summary: This review provides beneficial evidence for the utilization of berberine (BBR) in the management and treatment of colorectal cancer (CRC), highlighting its potential mechanisms of action involving gene expression regulation, cell cycle modulation, inflammatory response control, oxidative stress regulation, and modulation of signaling pathways. Additionally, BBR also displays antitumor effects in CRC through the regulation of gut microbiota and mucosal barrier function.
FRONTIERS IN MEDICINE
(2022)
Article
Pharmacology & Pharmacy
Jun Yan, Qizhen Zhuang, Zhenzhen Li, Yujuan Xiong, Min He, Cunmin Kang, Qiaoxuan Zhang, Liqiao Han, Enyu Liang, Hongcan Liu, Peifeng Ke, Xianzhang Huang
Summary: A novel compound, MIL-1, designed and synthesized in this study, showed significantly better antitumor activity than millepachine. It targeted microtubules by interfering with their dynamics and binding irreversibly. MIL-1 demonstrated remarkable antitumor effects across various human cancer cell lines without causing toxicity to normal cells, suggesting its potential for further study in hepatocellular carcinoma treatment.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2021)
Article
Chemistry, Multidisciplinary
Jiao Yang Lu, Wei Tao Huang, Kexuan Zhou, Xiaoli Zhao, Shuqing Yang, Liqiu Xia, Xuezhi Ding
Summary: The fatty chain in microbial-derived amphiphilic CLP bacillomycin Lb (B-Lb) was found to be key in maintaining self-assembled form and antitumor activity, with its supramolecular assemblies serving as a novel cell death inducer. This study will promote the construction of customized CLP micro/nanostructures and the design of new antitumor drugs based on structure-activity relationship.
Article
Nanoscience & Nanotechnology
Yuan Zou, Xiangtao Wang, Dongdong Bi, Jingxin Fu, Jianwei Han, Yifei Guo, Li Feng, Meihua Han
Summary: Pterostilbene-loaded nanoparticles (PTE-NPs) show significantly increased antitumor activity against breast cancer and cervical cancer cells. The enhanced water solubility of PTE-NPs, achieved through nanotechnology, leads to improved therapeutic effects similar to conventional drugs in in vivo studies.
Article
Pharmacology & Pharmacy
J. S. Dileep Kumar, Andrei Molotkov, Michael C. Salling, Patrick Carberry, Jaya Prabhakaran, John Castrillon, Akiva Mintz
Summary: This study utilized Positron Emission Tomography to investigate the effects of chronic alcohol consumption on brain microtubules in mice, revealing a trend of decreased microtubule binding in the chronic alcohol group. These findings suggest the potential of [C-11]MPC-6827 as a PET ligand for further in vivo imaging studies on alcohol use disorder.
PHARMACOLOGICAL REPORTS
(2022)
Article
Pharmacology & Pharmacy
Michelyne Haroun, Heba S. Elsewedy, Tamer M. Shehata, Christophe Tratrat, Bandar E. Al Dhubiab, Katharigatta N. Venugopala, Mervt M. Almostafa, Hafedh Kochkar, Hanan M. Elnahas
Summary: This study aimed to enhance the therapeutic efficacy of brucine (BRU) by using PEGylated niosomal as a nanocarrier. The results showed that the PEGylated niosomal formulation loaded with BRU had considerable anti-cancer activity against breast cancer cells and improved survival time.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2022)
Article
Cell Biology
Agnieszka Wojtczak
Summary: The present study examined the effects of propyzamide, a microtubule-disrupting agent, on spermiogenesis in the alga Chara vulgaris. It was found that propyzamide disrupted the functioning of microtubules, leading to distorted sperm nuclei and altered chromatin arrangement in the nucleus. Changes in the cytoplasm, such as the presence of autolytic vacuoles and a dilated endoplasmic reticulum, were also observed. The study suggests that microtubules play a crucial role in intramanchette transport during spermatid differentiation.
Article
Chemistry, Applied
Lijuan Hua, Wenge Li, Yan Chen, Kai Liang, He Cai, Jing Wang, Siyu Wang, Tianyue Yin, Lili Liang
Summary: The hexanuclear Nd (III) complex exhibits promising antitumor and antifungal activities, with a trinuclear cluster structure and high inhibition rates against human hepatocellular carcinoma and Candida albicans.
APPLIED ORGANOMETALLIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Yichuan Chen, Wenlong Li, Yan Yang, Ruitong Zhong, Huiyan Hu, Chunxia Huang, Jing Chen, Lijuan Liang, Yunjun Liu
Summary: Two polypyridyl ruthenium(II) complexes were synthesized and their cytotoxic activities against cancer cells were investigated. However, the complexes were not effective in inhibiting cancer cell proliferation. To enhance the anticancer effect, the complexes were encapsulated into liposomes, resulting in increased anticancer efficacy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)