Article
Chemistry, Multidisciplinary
Zahra Rashidijahanabad, Sherif Ramadan, Nicholas A. O'Brien, Athar Nakisa, Shuyao Lang, Howard Crawford, Jeffrey C. Gildersleeve, Xuefei Huang
Summary: Researchers have successfully developed a sLe(a)-based anticancer vaccine, which generated strong and long-lasting antibody responses in mice, selectively killed cancer cells, and significantly reduced tumor development.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Pharmacology & Pharmacy
Beihua Xu, Li Yuan, Ying Hu, Zhiyuan Xu, Jiang-Jiang Qin, Xiang-Dong Cheng
Summary: In this study, fullerenol-DOX conjugates and folic acid-grafted FU-DOX conjugates were designed for improved selectivity and activity of DOX in cancer cells. Characterization showed that both conjugates had small diameter and low polydispersity, with pH sensitivity. The cellular uptake studies demonstrated enhanced intracellular accumulation of DOX and increased cytotoxicity against liver cancer cells.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Materials Science, Multidisciplinary
Puja Ghosh, Himja Tiwari, Jaya Lakkakula, Arpita Roy, Talha Bin Emran, Summya Rashid, Saad Alghamdi, Bodour S. Rajab, Mazen Almehmadi, Mamdouh Allahyani, Abdulelah Aljuaid, Ahad Amer Alsaiari, Rohit Sharma, Ahmad O. Babalghith
Summary: Despite advancements in the biomedical field, clinically approved cancer therapeutics are mostly limited to chemotherapy, surgery, and radiotherapy. There is a growing demand for targeted drug delivery using nanomaterials to mitigate the cardiotoxicity and side effects associated with current treatment strategies. In this review, the use of modified liposomes encapsulating the commonly used drug doxorubicin (DOX) is explored for the treatment of various types of cancer, showing potential for enhanced efficiency and site-specific drug delivery.
MATERIALS TODAY ADVANCES
(2022)
Article
Chemistry, Multidisciplinary
Tingting Xu, Ziyun Fan, Junqiao Lou, Qi Du, Yue Kong, Yujia Lu, Xueming Wu
Summary: In this study, vitexin was glycosylated using solvent-stable beta-fructosidase in organic solvents, resulting in a high yield of 90-99%. Two novel vitexin glycosides were synthesized from 1.5 g/L vitexin in a 50% ethyl acetate solvent system, and they showed higher anti-tumor activities compared to vitexin.
Review
Cell Biology
Mateusz Kciuk, Adrianna Gielecinska, Somdutt Mujwar, Damian Kolat, Zaneta Kaluzinska-Kolat, Ismail Celik, Renata Kontek
Summary: Doxorubicin (DOX) is a key component in current anti-cancer treatment regimens, but its precise mechanisms of action remain unclear. Recent evidence suggests that DOX exhibits pleiotropic anticancer activity, including DNA damage, reactive oxygen species (ROS) production, apoptosis, senescence, autophagy, ferroptosis, and pyroptosis induction, as well as immunomodulation. This review aims to gather information on the anticancer mechanisms of DOX and its impact on the anti-tumor immune response, providing a rationale for the importance of DOX in modern cancer therapy.
Article
Chemistry, Multidisciplinary
Dapeng Zhu, Mingyu Geng, Biao Yu
Summary: Starfish have developed a special type of secondary metabolite called starfish saponins to defend against predators and parasites. Among them, starfish cyclic steroid glycosides are structurally unique and pose a significant synthetic challenge.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Engineering, Multidisciplinary
Mohammed Hawash, Mohammed T. Qaoud, Nidal Jaradat, Samer Abdallah, Shahd Issa, Nawal Adnan, Marah Hoshya, Shorooq Sobuh, Zafer Hawash
Summary: This study synthesized thiophene carboxamide derivatives as biomimetics of the anticancer medication Combretastatin A-4 (CA-4) and compared their similarity in polar surface area (PSA) to CA-4. The results showed that most of the synthesized structures had biomimetic PSA to CA-4 and exhibited similar chemical and biological properties against Hep3B cancer cell line. Compounds 2b and 2e in the synthesized series showed the highest activity against Hep3B, and they had comparable interaction patterns to CA-4 and colchicine within the tubulin-colchicine-binding pocket.
Article
Polymer Science
Hamideh Gharnas-Ghamesh, Mojtaba Masoumi, Vahid Erfani-Moghadam
Summary: This study synthesized a nanocarrier for the chemotherapy drug doxorubicin (DOX) to enhance its anticancer efficacy while reducing side effects. The nanocarrier, made of PBMA-b-POEGMA diblock copolymer, demonstrated good physicochemical and biological properties. It efficiently encapsulated DOX and released the drug using the Korsmeyer-Peppas model. The DOX-loaded micelles showed high cellular uptake and induced apoptosis in cancer cells.
JOURNAL OF APPLIED POLYMER SCIENCE
(2022)
Article
Chemistry, Organic
Dancan K. Njeri, Justin R. Ragains
Summary: The assigned tetrasaccharide repeating subunit from the Acinetobacter baumannii KL4-associated capsular polysaccharide has been successfully synthesized through chemical synthetic efforts. A convergent synthetic strategy based on a 1,2-cis-selective [2+2] glycosylation was crucial for the synthesis of the fully protected tetrasaccharide.
Article
Pharmacology & Pharmacy
Bharat Pateliya, Vinod Burade, Sunita Goswami
Summary: The concomitant use of naringenin and metformin with doxorubicin chemotherapy showed increased cytotoxicity in TNBC cells in vitro and reduced tumor volume and weight in vivo, enhancing antitumor activity. Biopsies demonstrated increased necrosis and inhibited cell proliferation. No adverse effects were observed in organs, blood glucose, cardiac histology, or Troponin I levels. Additionally, the combination led to reduced dose-related body weight loss and increased cytokines compared to a high dose of doxorubicin alone, indicating its potential as an adjunct therapy for improved effectiveness against breast carcinoma.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Mingge Ding, Rui Shi, Shuli Cheng, Man Li, Dema De, Chaoyang Liu, Xiaoming Gu, Juan Li, Shumiao Zhang, Min Jia, Rong Fan, Jianming Pei, Feng Fu
Summary: This study found that inhibition of Mfn2-mediated mitochondrial fusion is associated with cardiac dysfunction and tumorigenesis. Restoring Mfn2-mediated mitochondrial fusion can enhance mitochondrial oxidative metabolism, reduce cellular injury and oxidative stress, and provide a dual therapeutic advantage in Dox-based chemotherapy by defending against Dox-induced cardiotoxicity and boosting its antitumor potency.
Article
Chemistry, Organic
Xingchun Sun, Zhiyuan Chen, Rui Yang, Mei Wang, Xiufang Wang, Qi Zhang, Guozhi Xiao
Summary: This study achieved the first stereoselective one-pot synthesis of the icosasaccharide motif of EPS-1A glycan from Cordyceps sinensis. The synthetic approach showed high stereoselectivity and efficiently assembled the target icosasaccharide through different strategies.
Review
Chemistry, Multidisciplinary
Wenli Wang, Yuxin Li, Ye He, Xing Jiang, Ying Yi, Xihan Zhang, Shiyu Zhang, Guangtong Chen, Min Yang, Jia-Lie Luo, Boyi Fan
Summary: This review summarizes the various efforts made in the last decade towards the synthesis of resin glycosides. It highlights the importance of their structural complexity and biological activities, as well as the insights they provide for the synthesis of glycoside compounds.
FRONTIERS IN CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Simms A. Adu, Matthew S. Twigg, Patrick J. Naughton, Roger Marchant, Ibrahim M. Banat
Summary: This study found that glycolipids have differential effects on skin cells, with lactonic sophorolipids and mono-rhamnolipids significantly detrimental to melanoma cell viability and inducing cell death via necrosis. Additionally, sophorolipids were shown to significantly inhibit melanoma cell migration.
Article
Chemistry, Applied
Mohamed A. El-Bindary, Mohamed G. El-Desouky, Ashraf A. El-Bindary
Summary: Metal-organic framework (MOF) hybrid materials, specifically Zr-MOF with encapsulated doxorubicin (DOX@Zr-MOF), have shown promising results in pH-responsive drug release and enhanced cytotoxicity against cancer cells. This simple one-pot approach could potentially serve as a multifunctional drug delivery vehicle for various applications, including cancer treatment. Further studies are needed to explore the potential of DOX@Zr-MOF in targeting specific cancer types and antimicrobial activities.
APPLIED ORGANOMETALLIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)