Article
Biochemistry & Molecular Biology
Guangcheng Wang, Wenjing Liu, Meiyan Fan, Min He, Yongjun Li, Zhiyun Peng
Summary: A novel series of thiazole-naphthalene derivatives were designed, synthesised, and evaluated for their anti-proliferative activities. Among them, compound 5b showed the highest activity as a tubulin polymerisation inhibitor, inducing apoptosis in cancer cells by arresting the cell cycle at G2/M phase.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Rahman Md Moshikur, Md Korban Ali, Rie Wakabayashi, Muhammad Moniruzzaman, Masahiro Goto
Summary: This study transformed methotrexate (MTX) into a series of five ionic liquids to improve its oral bioavailability, with proline ethyl ester MTX (IL[ProEt][MTX]) showing the highest oral bioavailability in mice. IL[ProEt][MTX] had significantly higher plasma concentration, longer half-life, larger area under the plasma concentration, longer absorption time, and lower body clearance compared to MTX sodium, indicating improved in vivo absorption and reduced systemic toxicity. Mechanistic studies suggested that the spherical structures formed by IL[ProEt][MTX] solution contributed to its improved oral absorption performance. Antitumor studies also showed that IL[ProEt][MTX] had better tumor growth inhibition than MTX sodium.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Article
Polymer Science
Sijoon Lee, Kyung-Ku Kang, Soo-Eun Sung, Joo-Hee Choi, Minkyoung Sung, Keum-Yong Seong, Jian Lee, Subin Kang, Seong Yun Yang, Sunjong Lee, Kyeong-Ryoon Lee, Min-Soo Seo, KilSoo Kim
Summary: The increased use of plastics has caused significant environmental pollution, especially in the form of microplastics. This study assessed the toxicity and pharmacokinetics of PTFE microplastics and found no observed toxic effects in mice administered doses of 2000 mg/kg or higher in both short-term and long-term exposures.
Article
Oncology
Sharon Elad, Noam Yarom, Yehuda Zadik, Michal Kuten-Shorrer, Stephen T. Sonis
Summary: Oral mucositis is a common and highly symptomatic complication of cancer therapy, affecting patients' quality of life and treatment tolerance. Research on managing oral mucositis is ongoing, with reports of oral mucosal toxicities in other therapies as well.
CA-A CANCER JOURNAL FOR CLINICIANS
(2022)
Article
Cell Biology
Peter Gennemark, Katrin Walter, Niclas Clemmensen, Dinko Rekic, Catarina A. M. Nilsson, Jane Knochel, Mikko Holtta, Linda Wernevik, Birgitta Rosengren, Dorota Kakol-Palm, Yanfeng Wang, Rosie Z. Yu, Richard S. Geary, Stan J. Riney, Brett P. Monia, Rikard Isaksson, Rasmus Jansson-Lofmark, Cristina S. J. Rocha, Daniel Linden, Eva Hurt-Camejo, Rosanne Crooke, Lloyd Tillman, Tina Ryden-Bergsten, Bjorn Carlsson, Ulf Andersson, Marie Elebring, Anna Tivesten, Nigel Davies
Summary: In this study, a chemically modified PCSK9 antisense oligonucleotide (ASO) with potential for oral delivery was developed and shown to effectively reduce LDL cholesterol levels. Animal experiments demonstrated liver targeting and significant reductions in PCSK9 and LDL cholesterol levels after oral administration.
SCIENCE TRANSLATIONAL MEDICINE
(2021)
Review
Medicine, Research & Experimental
Cheng Wang, Shu Dai, Xingtao Zhao, Yafang Zhang, Lihong Gong, Ke Fu, Cheng Ma, Cheng Peng, Yunxia Li
Summary: This review comprehensively summarizes the molecular mechanisms of the anticancer effects of celastrol, a pentacyclic triterpenoid extracted from Tripterygium wilfordii Hook F. It has been found to exhibit significant broad-spectrum anticancer activities by inhibiting tumor cell proliferation, migration and invasion, inducing cell apoptosis, suppressing autophagy, hindering angiogenesis, and inhibiting tumor metastasis. Various signaling pathways have been identified as important molecular targets for its anticancer effects. However, celastrol also has adverse effects, low oral bioavailability, and a narrow therapeutic window, which present challenges for its development as an anticancer drug.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Article
Chemistry, Medicinal
Azizah M. Malebari, Gabriela Duffy Morales, Brendan Twamley, Darren Fayne, Mohemmed Faraz Khan, Eavan C. McLoughlin, Niamh M. O'Boyle, Daniela M. Zisterer, Mary J. Meegan
Summary: This study describes the synthesis, characterization, and mechanism of action of a series of 3-fluoro and 3,3-difluoro substituted beta-lactams as analogues of the tubulin-targeting agent CA-4. These compounds showed potent activity in breast cancer cells and low toxicity in non-cancerous cells. Mechanistic studies demonstrated that these compounds inhibit tubulin polymerization and induce apoptosis, making them potential candidates for the development of novel cancer therapeutics.
Article
Oncology
Silpa Narayanan, Qiu-Xu Teng, Zhuo-Xun Wu, Urooj Nazim, Nishant Karadkhelkar, Nikita Acharekar, Sabesan Yoganathan, Najia Mansoor, Feng-Feng Ping, Zhe-Sheng Chen
Summary: A compound called ITH-6 demonstrates favorable anticancer activity against p53 mutant colorectal cancer cells by arresting cell cycle and inducing apoptosis. It also reduces tumor size and volume, and inhibits the expression of related genes, indicating its cytotoxic action.
FRONTIERS IN ONCOLOGY
(2022)
Article
Chemistry, Multidisciplinary
Lotfi M. Aroua, Ahmed N. Al-Hakimi, Mahfoudh A. M. Abdulghani, Sadeq K. Alhag
Summary: Novel mononuclear complexes derived from urea Schiff base were synthesized and their bioactivity was tested. Copper-urea Schiff base complex showed excellent activity against three cancer cell lines and demonstrated good safety in vivo toxicity test.
ARABIAN JOURNAL OF CHEMISTRY
(2022)
Article
Environmental Sciences
Dahye Jeong, Hyosook Shin, Jinhee Lee, Junyoung Yang, Kikyung Jung, Jayoung Jeong, Hansol Won, Jaeho Oh
Summary: This study investigated the oral toxicity of chlorobutanol in Sprague Dawley rats. The results showed that the approximate lethal dose (ALD) of chlorobutanol was over 250 mg/kg b.w./day in the single-dose study, and the no adverse effect level (NOAEL) was over 50 and 12.5 mg/kg b.w./day for female and male rats in the repeated-dose toxicity study.
Article
Biochemistry & Molecular Biology
Hoda Abolhasani, Afshin Zarghi, Tahereh Komeili Movahhed, Ahmad Abolhasani, Bahram Daraei, Siavoush Dastmalchi
Summary: The newly synthesized spiroisoxazoline derivatives showed promising selective COX-2 inhibitory activity and cytotoxicity, with compound 9f containing a 3,4-dimethoxyphenyl group demonstrating superior potency. Docking calculations revealed potential interactions with COX-2 enzyme, suggesting these compounds as potential candidates for anti-inflammatory and anticancer agents.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Yin-Ru Li, Fang-Fang Liu, Wen-Bo Liu, Yi-Fan Zhang, Xin-Yi Tian, Xiang-Jing Fu, Yan Xu, Jian Song, Sai-Yang Zhang
Summary: In this study, a novel aromatic amide derivative SY-65 was identified as a dual inhibitor of tubulin and histone deacetylase 1, showing potent anticancer activity in vitro and in vivo. The compound exhibited excellent antiproliferative activity against multiple cancer cell lines and demonstrated inhibition of tubulin polymerization and HDAC1 activity. It also induced cell cycle arrest and apoptosis in cancer cells. This study highlights the potential of compound SY-65 as a novel tubulin/HDAC1 inhibitor for future cancer therapeutics.
BIOCHEMICAL PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Abid Naeem, Chengqun Yu, Hetonghui, Zhenzhong Zang, Weifeng Zhu, Yongmei Guan
Summary: In order to improve the solubility and bioavailability of gallic acid, β-cyclodextrin/chitosan-based controlled release hydrogels were developed. The hydrogels showed the highest swelling and release at pH 7.4. Additionally, the hydrogels exhibited good antioxidant and antibacterial properties.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Chemistry, Medicinal
Shu-Yu Wang, Xu Liu, Ling-Wei Meng, Miao-Miao Li, Yin-Ru Li, Guang-Xi Yu, Jian Song, Hong-Yu Zhang, Ping Chen, Sai-Yang Zhang, Tao Hu
Summary: In this study, a series of indoline derivatives were designed and synthesized, among which compound 9d exhibited potent antiproliferative activity as a tubulin inhibitor. Molecular docking and cell experiments confirmed the anticancer potential of this compound.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Medicinal
Shu-Yu Wang, Xu Liu, Ling-Wei Meng, Miao-Miao Li, Yin-Ru Li, Guang-Xi Yu, Jian Song, Hong-Yu Zhang, Ping Chen, Sai-Yang Zhang, Tao Hu
Summary: In this study, indoline derivatives were designed, synthesized, and found to exhibit potent antiproliferative activity against various cell lines, with compound 9d identified as a tubulin inhibitor targeting the colchicine binding site. Molecular docking results confirmed the tight binding of compound 9d to the tubulin site, indicating its potential as a novel tubulin inhibitor with anticancer activity.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Food Science & Technology
Chandra Sekhar Mohanty, Naziya Syed, Deepak Kumar, Sonam Khare, Sagar Prasad Nayak, Kunwar Sarvendra, Rojalin Pattanayak, Anirban Pal, Chandan Singh Chanotiya, Prasant Kumar Rout
Summary: This study characterized and evaluated the physico-chemical properties of seed oil from winged bean, showing that the oil quality is comparable with soybean oil and has good thermal stability. Safety evaluation on albino mice also showed non-significant changes. Additionally, the nutritional components in the seed-cake of winged bean are closely comparable with soybean seed-cake.
JOURNAL OF FOOD MEASUREMENT AND CHARACTERIZATION
(2021)
Article
Biochemistry & Molecular Biology
Gaurav Raj Dwivedi, Sadiya Khwaja, Arvind Singh Negi, Swati S. Panda, A. Swaroop Sanket, Sanghamitra Pati, Amit Chand Gupta, Dnyaneshwar Umrao Bawankule, Debabrata Chanda, Rajni Kant, Mahendra P. Darokar
Summary: The study found that Van D, a curcumin mimic, can reduce multidrug resistant Pseudomonas aeruginosa resistance to tetracycline, inhibit biofilm synthesis, extend post-antibiotic effect, and decrease mutant prevention concentration of tetracycline.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Sadiya Khwaja, Kaneez Fatima, Divya Mishra, Vineet Babu, Yogesh Kumar, Sumera Banu Malik, Misbah Tabassum, Suaib Luqman, Dnyaneshwar U. Bawankule, Debabrata Chanda, Feroz Khan, Dilip M. Mondhe, Arvind S. Negi
Summary: This study focused on the total synthesis of indanocine and its analogues, which showed potential anticancer and anti-inflammatory activities. Benzylindanocine 12i exhibited microtubule destabilization and anti-inflammatory effects, reducing EAC tumor in mice and showing safety in rodent studies. The concurrent anticancer and anti-inflammatory activities of benzylindanocine suggest further optimization for better efficacy and druggability.
CHEMICAL BIOLOGY & DRUG DESIGN
(2021)
Article
Multidisciplinary Sciences
Kaneez Fatima, Nusrat Masood, Zahoor Ahmad Wani, Abha Meena, Suaib Luqman
Summary: Neomenthol shows promising antiproliferative activity against skin carcinoma cells by inhibiting tubulin polymerization and hyaluronidase activity, which are responsible for tumor growth, metastasis, and angiogenesis.
JOURNAL OF ADVANCED RESEARCH
(2021)
Article
Chemistry, Medicinal
Shilpi Singh, Pratik Narain Srivastava, Abha Meena, Suaib Luqman
Summary: This study identified the flavonoid narirutin as a potential antagonist of miRNAs through molecular docking simulation, which disrupts the synthesis and processing of miRNA and shows potential for cancer prevention and treatment.
PHYTOTHERAPY RESEARCH
(2022)
Review
Chemistry, Medicinal
K. M. Uma Kumari, Narayan Prasad Yadav, Suaib Luqman
Summary: This review focuses on the occurrence and etiology of dandruff, as well as the potential application of plant essential oils/extracts and novel treatment strategies. Current findings suggest that topical antifungals are the first line of treatment, but they have specific side effects. Alternative therapies, such as tea tree oil, thyme, and Aloe vera, have shown anti-dandruff activity by disrupting microbial growth.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Hilal Ahmad Mir, Roshia Ali, Zahoor Ahmad Wani, Firdous Ahmad Khanday
Summary: This study demonstrates the important role of vitamin C in breast cancer by binding with p66Shc to induce its phosphorylation, activate Rac1, increase ROS production, and promote apoptosis. This finding suggests that the p66Shc/Rac1 pathway could be a potential therapeutic target for breast cancer treatment.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2022)
Article
Plant Sciences
Saurabh Kumar, Deepak Singh Kapkoti, Pooja Rani Mina, Madhuri Gupta, Ravi Kumar, Parmanand Kumar, Priyanka Pathak, R. S. Bhakuni, Prasant Rout, Anirban Pal, Mahendra P. Darokar
Summary: A study found that liquiritigenin (LTG) has a positive interaction with chloroquine (CQ) in treating drug-resistant strains of Plasmodium falciparum. The combination therapy of LTG and CQ showed enhanced efficacy at lower concentrations compared to individual doses, both in vitro and in vivo.
Article
Food Science & Technology
Shilpi Singh, Akhilesh Kumar Maurya, Abha Meena, Nidhi Mishra, Suaib Luqman
Summary: This study investigated the binding affinity of myricitrin to CATD and found a strong affinity. The stability of the complex was confirmed through molecular dynamics simulation, and enzyme activity studies showed inhibitory concentration. The experimental findings suggest that myricitrin could be a potential therapeutic agent for CATD-mediated lung cancer.
FOOD AND CHEMICAL TOXICOLOGY
(2023)
Article
Agricultural Engineering
Pooja Gaur, Feroz Khan, Karuna Shanker
Summary: This study successfully isolated biologically active compounds from Andrographis paniculata root that have the ability to absorb dietary fat, making them potential candidates for obesity management. 7-O-methyl-dihydro wogonin (MDHW) exhibited the strongest pancreatic lipase inhibition activity and showed a synergistic effect with orlistat. MDHW acts as a competitive inhibitor through energy transfer from pancreatic lipase, and the binding interaction between MDHW and pancreatic lipase is hydrophobic. In vitro and in silico studies confirmed the potential of MDHW as an anti-obesity agent for pharmaceutical and food industry applications.
INDUSTRIAL CROPS AND PRODUCTS
(2023)
Article
Biochemistry & Molecular Biology
Waseem Raza, Abha Meena, Suaib Luqman
Summary: This study explores the potential of 3,5,7-trihydroxyflavone (THF) in inhibiting prostate cancer cell growth through reactive oxygen species (ROS) generation and also examines its tumor reduction potential in mice.
JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
(2023)
Article
Chemistry, Analytical
Pooja Gaur, Princi Gupta, Neerja Tiwari, Namita Gupta, Karuna Shanker
Summary: A novel HPTLC method was developed for the simultaneous quantification of six bioactive alkaloids in agro-waste of Piper longum. The method demonstrated excellent separation and specificity, and was successfully applied for accurate quantification in Piper longum roots. Additionally, the method was found to be environmentally friendly and energy efficient.
MICROCHEMICAL JOURNAL
(2023)
Article
Chemistry, Medicinal
Yusuf Hussain, Jyoti Singh, Abha Meena, Rohit Anthony Sinha, Suaib Luqman
Summary: This study explores the therapeutic potential of combining escin with sorafenib and finds that the combination treatment can significantly reduce the effective dose of sorafenib and inhibit autophagy in lung cancer cells, inducing late apoptosis.
PHYTOTHERAPY RESEARCH
(2023)
Review
Chemistry, Medicinal
Anurag Mathur, Abha Meena, Suaib Luqman
Summary: Monoterpenoids, a subclass of terpenoids, have been extensively studied for their antitumor properties, including antiproliferative, apoptotic, antiangiogenic, and antimetastatic effects. This review focuses on the effects of specific monoterpenoids on metastasis and relevant signaling pathways. Monoterpenoids exhibit complexity as natural products that regulate metastatic proteins through various signaling pathways. However, limited clinical trials hinder the drug usage of monoterpenoids in preventing cancer metastasis.
PHYTOTHERAPY RESEARCH
(2023)
Article
Agriculture, Multidisciplinary
Pooja Gaur, Neerja Tiwari, Karuna Shanker
Summary: This study demonstrates the potential of using agricultural wastes of Piper longum as antiobesity agents through the extraction of pseudoalkaloids. One of the compounds, pellitorine, showed strong pancreatic lipase inhibitory activity and exhibited synergistic effects with orlistat. The structural compactness of the interaction between pellitorine and pancreatic lipase was confirmed by Fourier transform infrared spectral studies. Molecular docking studies further revealed the binding interaction between pellitorine and the catalytic active amino side residue of the protein. These findings suggest that pellitorine has the potential to be developed as an anti-obesity supplement.
ACS AGRICULTURAL SCIENCE & TECHNOLOGY
(2022)
Article
Pharmacology & Pharmacy
Xuezhi Zhuo, Vito Fodera, Per Larsson, Zarah Schaal, Christel A. S. Bergstrom, Korbinian Lobmann, Aleksei Kabedev
Summary: Our previous work demonstrated that beta-lactoglobulin-stabilized amorphous solid dispersion (ASD) loaded with 70 % indomethacin remains stable for over 12 months. We further investigated the stabilization mechanisms by testing five other drug molecules and using experimental techniques and molecular dynamics simulations. The results showed that steric confinement, hydrogen bonding, and the glass transition temperature of the drug molecule play important roles in stabilizing ASDs with high drug loadings.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Sebastian Schmidt, Ulrike Holzgrabe
Summary: The binding of drugs to plasma proteins, such as human serum albumin (HSA), is crucial for determining pharmacokinetic parameters. This study investigated the enantioselective binding of S- and R-ketamine to HSA. It was found that ketamine has weak affinity to HSA, with no significant differences in binding behavior between the individual enantiomers and the racemate. The aromatic ring and N-methyl group were identified as the most strongly involved structural moieties in the binding of ketamine to HSA.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Yuchen Zhao, Han Wang, Lin Jin, Ziwei Zhang, Lianghu Liu, Mengqi Zhou, Xianzheng Zhang, Lingling Zhang
Summary: Interleukins (ILs) are important for communication between immune cells and non-immune cells, but dysregulation of ILs expression is a characteristic of autoinflammatory diseases. Drugs targeting ILs have significant clinical benefits, but may also cause adverse reactions. Fusion protein technology, with its ability to enhance therapeutic efficacy, has been explored for developing anti-inflammatory drugs. This review discusses the efficacy of fusion protein drugs developed with ILs or their receptors in treating autoinflammatory diseases, highlighting the potential of this technology in future anti-inflammatory drug development.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Serena Bertoni, Elena Simone, Stefano Sangiorgi, Beatrice Albertini, Nadia Passerini
Summary: This study investigated the correlation between the structure and release properties of solid lipid microparticles (MPs) with different liquid additives. The additives accelerated the conversion of the unstable alpha-form of tristearin to the stable beta-polymorph and caused structural modifications in the MPs. The presence of additives prolonged the drug release in water and resulted in higher release profiles in biorelevant media. The findings suggest that the release behavior can be influenced by the polymorphism and supramolecular-level structural modification of lipid formulations containing crystal modifiers.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Juulia Jarvinen, Ahmed B. Montaser, Santosh Kumar Adla, Jukka Leppanen, Marko Lehtonen, Kati-Sisko Vellonen, Tuomo Laitinen, Aaro Jalkanen, William F. Elmquist, Juri Timonen, Kristiina M. Huttunen, Jarkko Rautio
Summary: This study attempted to alter the brain distribution pattern of Palbociclib by creating and assessing two novel prodrugs. Although the prodrug design did not significantly improve Palbociclib brain delivery, the study provides valuable insights for future prodrug development and drug delivery strategies targeting specific transporters.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Review
Pharmacology & Pharmacy
Miao Wang, Xinyu Ma, Shiyu Zong, Yaqiong Su, Rui Su, Hong Zhang, Yang Liu, Chunliu Wang, Ye Li
Summary: This article discusses the potential and limitations of nasal administration in central nervous system drug delivery. Nasal gel viscosity can alleviate the impact of nasal mucociliary clearance on drug delivery, and materials such as gellan gum, chitosan, carbomer, cellulose, and poloxamer can be used to prepare nasal gels.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Bjarke Strom Larsen, Eric Kissi, Liebert Parreiras Nogueira, Natalja Genina, Ingunn Tho
Summary: This study investigates the influence of drug load and polymer molecular weight on the structure of 3D printed tablets. The results show that drug load and polymer molecular weight have a significant impact on the porosity and size of the tablets, while the effect of drug load on the total porosity of the tablets is minimal.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Zhentao Qiao, Fuhang Wang, Dongjian Han, Yuansong Zhuang, Qingjiao Jiang, Yi Zhang, Miaomiao Liu, Quanxu An, Zhiwei Wang, Deliang Shen
Summary: In this study, it was demonstrated that periadventitial delivery of rapamycin-fibrin glue (RPM-FG) can inhibit intimal hyperplasia (IH) in a rat carotid artery injury model without compromising re-endothelialization. This provides a promising direction for the future development of a safe, effective, and minimally invasive perivascular drug delivery method to treat vascular disease.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Neele Puhlmann, Rodrigo Vidaurre, Klaus Kuemmerer
Summary: Active pharmaceutical ingredients and their metabolites and transformation products are pollutants that can harm human and environmental health. Designing greener APIs is an effective strategy to address this issue. The drug discovery and development process can incorporate environmental parameters to achieve this design, and this process is highly flexible.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
