keyword
https://read.qxmd.com/read/38531150/discovery-of-cinnamylaldehyde-derived-mono-carbonyl-curcumin-analogs-as-anti-gastric-cancer-agents-via-suppression-of-stat3-and-akt-pathway
#21
JOURNAL ARTICLE
Xi Chen, Peiqin Zhang, Huating Zhang, Xueqiang Ma, Ye Zhang, Yajie Wu, Kaiwen Jin, Jiabing Wang, Jianzhang Wu
The structural modification of curcumin has always been a hotspot in drug development. In this paper, a class of cinnamylaldehyde-derived mono-carbonyl curcumin analogs (MCAs) with 7-carbon-links were designed and synthesized and their anticancer properties were evaluated. Through screening anti-gastric cancer activity of these compounds, H1 exhibited the strongest cytotoxic activity by inhibiting cell viability and colony formation, inducing cell cycle G2/M phase arrest in vitro (SGC-7901 and AGS gastric cancer cells)...
March 24, 2024: Bioorganic Chemistry
https://read.qxmd.com/read/38530892/neofunctionalization-of-an-omt-cluster-dominates-polymethoxyflavone-biosynthesis-associated-with-the-domestication-of-citrus
#22
JOURNAL ARTICLE
Zhaoxin Peng, Lizhi Song, Minghua Chen, Zeyang Liu, Ziyu Yuan, Huan Wen, Haipeng Zhang, Yue Huang, Zhaowen Peng, Hongbin Yang, Gu Li, Huixian Zhang, Zhehui Hu, Wenyun Li, Xia Wang, Robert M Larkin, Xiuxin Deng, Qiang Xu, Jiajing Chen, Juan Xu
Polymethoxyflavones (PMFs) are a class of abundant specialized metabolites with remarkable anticancer properties in citrus. Multiple methoxy groups in PMFs are derived from methylation modification catalyzed by a series of hydroxylases and O -methyltransferases (OMTs). However, the specific OMTs that catalyze the systematic O -methylation of hydroxyflavones remain largely unknown. Here, we report that PMFs are highly accumulated in wild mandarins and mandarin-derived accessions, while undetectable in early-diverging citrus species and related species...
April 2, 2024: Proceedings of the National Academy of Sciences of the United States of America
https://read.qxmd.com/read/38530746/a-review-on-the-traditional-applications-phytochemistry-and-pharmacology-of-the-genus-physochlaina-g-don
#23
JOURNAL ARTICLE
Younas Rasheed Tantray, Ishrat Jan, Irshad Mohiuddin, Preeti Gorla, Charul Anand, Jagdesh Chandra Arya, Shahnawaz Ahmad Bhat, Vijay Kumar, Shiddamallayya Nagayya, Rabinaryana Acharya
Physochlaina is a genus of flowering plants belonging to the family Solanaceae and consists of 10 species distributed in various Asian countries. The species of the genus have been traditionally used to cure a variety of illnesses due to their highly valuable medicinal properties, including cancer, asthma, cough, weakness, stomachache, diarrhea, swelling, spasms, toothache, boils, ulcers, rheumatic pain, chronic bronchitis, gastric problems, abdominal pain, palpitation, and insomnia. The species have gained significant attention due to their remarkable ethnopharmacological and ethnomedicinal significance...
March 26, 2024: Chemistry & Biodiversity
https://read.qxmd.com/read/38529661/uracil-and-pyridine-containing-hdac-inhibitors-displayed-cytotoxicity-in-colorectal-and-glioblastoma-cancer-stem-cells
#24
JOURNAL ARTICLE
Francesco Fiorentino, Emanuele Fabbrizi, Alessia Raucci, Beatrice Noce, Rossella Fioravanti, Sergio Valente, Chantal Paolini, Ruggero De Maria, Christian Steinkühler, Paola Gallinari, Dante Rotili, Antonello Mai
Cancer stem cells (CSCs) are a niche of highly tumorigenic cells featuring self-renewal, activation of pluripotency genes, multidrug resistance, and ability to cause cancer relapse. Seven HDACi (1-7), showing either hydroxamate or 2'-aminoanilide function, were tested in colorectal cancer (CRC) and glioblastoma multiforme (GBM) CSCs to determine their effects on cell proliferation, H3 acetylation levels and in-cell HDAC activity. Two uracil-based hydroxamates, 5 and 6, which differ in substitution at C5 and C6 positions of the pyrimidine ring, exhibited the greatest cytotoxicity in GBM (5) and CRC (6) CSCs, followed by the pyridine-hydroxamate 2, with 2- to 6-fold higher potency than the positive control SAHA...
March 26, 2024: ChemMedChem
https://read.qxmd.com/read/38529192/brucine-entrapped-titanium-oxide-nanoparticle-for-anticancer-treatment-an-in-vitro-study
#25
JOURNAL ARTICLE
Rashed M Almuqbil
Backgroundand Objective . The public's health has been seriously threatened by cervical cancer during recent times. In terms of newly diagnosed cases worldwide, it ranks as the ninth most prevalent malignancy. Multiple investigations have proven that nanoparticles can effectively combat cancer due to their small dimensions and extensive surface area. In the meantime, bioactive compounds which are biocompatible are being loaded onto nanoparticles to promote cancer therapy. The current study investigates the anticancerous potential of Brucine-entrapped titanium oxide nanoparticles (TiO2 NPs) in cervical cancer cell line (HeLa)...
2024: Advances in pharmacological and pharmaceutical sciences
https://read.qxmd.com/read/38529189/sesquiterpene-lactones-as-emerging-biomolecules-to-cease-cancer-by-targeting-apoptosis
#26
REVIEW
Chou-Yi Hsu, Sadegh Rajabi, Maryam Hamzeloo-Moghadam, Abhinav Kumar, Marc Maresca, Pallavi Ghildiyal
Apoptosis is a programmed cell death comprising two signaling cascades including the intrinsic and extrinsic pathways. This process has been shown to be involved in the therapy response of different cancer types, making it an effective target for treating cancer. Cancer has been considered a challenging issue in global health. Cancer cells possess six biological characteristics during their developmental process known as cancer hallmarks. Hallmarks of cancer include continuous growth signals, unlimited proliferation, resistance to proliferation inhibitors, apoptosis escaping, active angiogenesis, and metastasis...
2024: Frontiers in Pharmacology
https://read.qxmd.com/read/38528700/piperine-mitigates-oxidative-stress-inflammation-and-apoptosis-in-the-testicular-damage-induced-by-cyclophosphamide-in-mice
#27
JOURNAL ARTICLE
Fatemeh Fani, Seyed Jalal Hosseinimehr, Mehryar Zargari, Mansoureh Mirzaei, Abbasali Karimpour Malekshah, Fereshteh Talebpour Amiri
Although cyclophosphamide (CP) has been approved as an anticancer drug, its toxic effect on most organs, especially the testis, has been established. Piperine (PIP) is an alkaloid that has antioxidant, antiapoptotic, and anti-inflammatory activities. This study was investigated the protective effects of PIP on CP-induced testicular toxicity in the mice. In this experimental study, 48 adult male BALB/c mice (30-35 g) were divided into six groups (n = 8), receiving normal saline (C), 5 mg/kg of PIP (PIP5), 10 mg/kg of PIP (PIP10), 200 mg/kg of CP, 200 mg/kg of CP + PIP5, and 200 mg/kg of CP + PIP10...
April 2024: Journal of Biochemical and Molecular Toxicology
https://read.qxmd.com/read/38527981/cyclophosphamide-stimulates-endoplasmic-reticulum-stress-and-induces-apoptotic-cell-death-in-human-glioblastoma-cell-lines
#28
JOURNAL ARTICLE
Mustafa Oztatlici, Hulya Oztatlici, Suna Karadeniz Saygili, Ismail Kaya, Ilker Deniz Cingoz
Cyclophosphamide (CP) is an alkylating chemotherapeutic agent commonly used in cancer treatments. In this study, we aimed to investigate the effects of 4-Hydroperoxy cyclophosphamide (4-HC), which is active form of CP, on glucose-regulated protein 78 (GRP78), activating transcription factor 6 (ATF6), phospho-protein kinase R (PKR)-like endoplasmic reticulum (ER) kinase (p-PERK), phospho-inositol-requiring enzyme 1 alpha (p-IRE1α), eukaryotic translation initiation factor 2 alpha (eIF2α), and caspase-3 messenger ribonucleic acids (mRNAs) and proteins that play roles in the ER stress pathway and apoptosis in U87 and T98 human glioblastoma cell lines...
2024: Romanian Journal of Morphology and Embryology
https://read.qxmd.com/read/38527038/combination-of-ethyl-acetate-fraction-from-calotropis-gigantea-stem-bark-and-sorafenib-induces-apoptosis-in-hepg2-cells
#29
JOURNAL ARTICLE
Pattaraporn Chaisupasakul, Dumrongsak Pekthong, Apirath Wangteeraprasert, Worasak Kaewkong, Julintorn Somran, Naphat Kaewpaeng, Supawadee Parhira, Piyarat Srisawang
The cytotoxicity of the ethyl acetate fraction of the Calotropis gigantea (L.) Dryand. (C. gigantea) stem bark extract (CGEtOAc) has been demonstrated in many types of cancers. This study examined the improved cancer therapeutic activity of sorafenib when combined with CGEtOAc in HepG2 cells. The cell viability and cell migration assays were applied in HepG2 cells treated with varying concentrations of CGEtOAc, sorafenib, and their combination. Flow cytometry was used to determine apoptosis, which corresponded with a decline in mitochondrial membrane potential and activation of DNA fragmentation...
2024: PloS One
https://read.qxmd.com/read/38526670/machine-learning-aided-search-for-ligands-of-p2y-6-and-other-p2y-receptors
#30
JOURNAL ARTICLE
Ana C Puhl, Sarah A Lewicki, Zhan-Guo Gao, Asmita Pramanik, Vadim Makarov, Sean Ekins, Kenneth A Jacobson
The P2Y6 receptor, activated by uridine diphosphate (UDP), is a target for antagonists in inflammatory, neurodegenerative, and metabolic disorders, yet few potent and selective antagonists are known to date. This prompted us to use machine learning as a novel approach to aid ligand discovery, with pharmacological evaluation at three P2YR subtypes: initially P2Y6 and subsequently P2Y1 and P2Y14 . Relying on extensive published data for P2Y6 R agonists, we generated and validated an array of classification machine learning model using the algorithms deep learning (DL), adaboost classifier (ada), Bernoulli NB (bnb), k-nearest neighbors (kNN) classifier, logistic regression (lreg), random forest classifier (rf), support vector classification (SVC), and XGBoost (XGB) classifier models, and the common consensus was applied to molecular selection of 21 diverse structures...
March 25, 2024: Purinergic Signalling
https://read.qxmd.com/read/38526661/molecular-identification-and-phytochemical-analysis-and-bioactivity-assessment-of-catharanthus-roseus%C3%A2-leaf-extract-exploring-antioxidant-potential-and-antimicrobial-activities
#31
JOURNAL ARTICLE
Velusamy Arulvendhan, Periyakali Saravana Bhavan, Rajapandian Rajaganesh
Plants have long been at the main focus of the medical industry's attention due to their extensive list of biological and therapeutic properties and ethnobotanical applications. Catharanthus roseus, sometimes referred to as Nithyakalyani in Tamil, is an Apocynaceae family member used in traditional Indian medicine. It also examines the plant's potential antimicrobial and antioxidant activities as well as its preliminary phytochemical makeup. Leaf material from C. roseus was analyzed and found to include a variety of phytochemicals including alkaloids, terpenoids, flavonoids, tannins, phenols, saponins, glycosides, quinones, and steroids...
March 25, 2024: Applied Biochemistry and Biotechnology
https://read.qxmd.com/read/38526657/physical-characterization-and-bioavailability-assessment-of-5-fluorouracil-based-nanostructured-lipid-carrier-nlc-in-vitro-drug-release-hemolysis-and-permeability-modulation
#32
JOURNAL ARTICLE
Mainuddin, Anoop Kumar, Ratneshwar Kumar Ratnesh, Jay Singh, Shweta Dumoga, Nitin Sharma, Amulya Jindal
5-Fluorouracil (5-FU) is an anticancer agent belonging to BCS Class III that exhibits poor release characteristics and low retention in the biological system. The main objective of this investigation was to develop a drug delivery system, i.e., Nanostructure Lipid Carriers (NLCs) loaded with 5-FU to prolong its biological retention through 5-FU-loaded NLCs (5-FUNLC) were designed to manipulate physicochemical characteristics and assessment of in vitro and in vivo performance. The developed NLCs underwent comprehensive characterization, including assessments for particle size, zeta potential, morphological evaluation, and FT-IR spectroscopy...
March 25, 2024: Medical Oncology
https://read.qxmd.com/read/38526651/ginsenoside-rg5-as-an-anticancer-drug-a-comprehensive-review-on-mechanisms-structure-activity-relationship-and-prospects-for-clinical-advancement
#33
REVIEW
Tilal Elsaman, Ali Mahmoud Muddathir, Ebtihal A M Mohieldin, Irmanida Batubara, Min Rahminiwati, Kosei Yamauchi, Magdi Awadalla Mohamed, Shadila Fira Asoka, Dietrich Büsselberg, Solomon Habtemariam, Javad Sharifi-Rad
Cancer remains one of the leading causes of death in the world. Despite the considerable success of conventional treatment strategies, the incidence and mortality rates are still high, making developing new effective anticancer therapies an urgent priority. Ginsenoside Rg5 (Rg5) is a minor ginsenoside constituent obtained exclusively from ginseng species and is known for its broad spectrum of pharmacological activities. This article aimed to comprehensively review the anticancer properties of Rg5, focusing on action mechanisms, structure-activity relationship (SAR), and pharmacokinetics attributes...
March 25, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38526569/the-beneficial-roles-of-sargassum-spp-in-skin-disorders
#34
JOURNAL ARTICLE
Min-Kyeong Lee, Hyeon Hak Jeong, Myeong-Jin Kim, Jae Seong Seo, Ji Young Hwang, Won-Kyo Jung, Kyoung Mi Moon, Incheol Lee, Bonggi Lee
As the body's largest organ, the skin is located at the internal and external environment interface, serving as a line of defense against various harmful stressors. Recently, marine-derived physiologically active ingredients have attracted considerable attention in the cosmeceutical industry due to their beneficial effects on skin health. Sargassum , a genus of brown macroalgae, has traditionally been consumed as food and medicine in several countries and is rich in bioactive compounds such as meroterpenoids, sulfated polysaccharides, fucoidan, fucoxanthin, flavonoids, and terpenoids...
March 22, 2024: Journal of Medicinal Food
https://read.qxmd.com/read/38526421/cycloplatinated-ii-complex-based-on-isoquinoline-alkaloid-elicits-ferritinophagy-dependent-ferroptosis-in-triple-negative-breast-cancer-cells
#35
JOURNAL ARTICLE
Feng-Yang Wang, Liang-Mei Yang, Shan-Shan Wang, Hui Lu, Xu-Sheng Wang, Yuan Lu, Wen-Xiu Ni, Hong Liang, Ke-Bin Huang
The development and optimization of metal-based anticancer drugs with novel cytotoxic mechanisms have emerged as key strategies to overcome chemotherapeutic resistance and side effects. Agents that simultaneously induce ferroptosis and autophagic death have received extensive attention as potential modalities for cancer therapy. However, only a limited set of drugs or treatment modalities can synergistically induce ferroptosis and autophagic tumor cell death. In this work, we designed and synthesized four new cycloplatinated (II) complexes harboring an isoquinoline alkaloid C∧ N ligand...
March 25, 2024: Journal of Medicinal Chemistry
https://read.qxmd.com/read/38526354/can-duvelisib-and-eganelisib-work-for-both-cancer-and-covid-19-molecular-level-insights-from-md-simulations-and-enhanced-samplings
#36
JOURNAL ARTICLE
Saroj Kumar Panda, Shaswata Karmakar, Parth Sarthi Sen Gupta, Malay Kumar Rana
SARS-CoV-2 has caused severe illness and anxiety worldwide, evolving into more dreadful variants capable of evading the host's immunity. Cytokine storms, led by PI3Kγ, are common in cancer and SARS-CoV-2. Naturally, there is a yearning to see whether any drugs could alleviate cytokine storms for both. Upon investigation, we identified two anticancer drugs, Duvelisib and Eganelisib, that could also work against SARS-CoV-2. This report is the first to decipher their synergic therapeutic effectiveness against COVID-19 and cancer with molecular insights from atomistic simulations...
March 25, 2024: Physical Chemistry Chemical Physics: PCCP
https://read.qxmd.com/read/38526199/antiviral-and-cytotoxic-indole-diterpenoids-from-the-antarctic-sponge-derived-fungus-aspergillus-candidus-hdn15-152
#37
JOURNAL ARTICLE
Bingying Tang, Runfang Zhang, Falei Zhang, Tianjiao Zhu, Qian Che, Dehai Li, Guojian Zhang
One new indole diterpenoid, ascandinine T ( 1 ), and three known analogues ( 2 - 4 ) were isolated from an Antarctic sponge-derived fungus Aspergillus candidus HDN15-152. The structures, including absolute configurations, were established based on NMR, HRESIMS, and electronic circular dichroism (ECD) calculations. All isolated compounds were tested for antiviral and anticancer activity. Compound 4 displayed antiviral activity against influenza A virus (IAV) of A/PR/8/34(H1N1) strain with an IC50 value of 39...
March 25, 2024: Natural Product Research
https://read.qxmd.com/read/38525971/therapeutic-implications-of-dietary-polyphenols-loaded-nanoemulsions-in-cancer-therapy
#38
REVIEW
Ritu Tomar, Sabya Sachi Das, Venkata Krishna Rao Balaga, Srusti Tambe, Jagannath Sahoo, Santosh Kumar Rath, Janne Ruokolainen, Kavindra Kumar Kesari
Cancer is one of the major causes of death worldwide, even the second foremost cause related to non-communicable diseases. Cancer cells typically possess several cellular and biological processes including, persistence, propagation, differentiation, cellular death, and expression of cellular-type specific functions. The molecular picture of carcinogenesis and progression is unwinding, and it appears to be a tangled combination of processes occurring within and between cancer cells and their surrounding tissue matrix...
March 25, 2024: ACS Applied Bio Materials
https://read.qxmd.com/read/38525947/water-soluble-pillar-5-arene-based-drug-candidates-for-lung-and-breast-cancer
#39
JOURNAL ARTICLE
Tugce Duran, Mehmet Ali Karaselek, Serkan Kuccukturk, Ahmed Nuri Kursunlu, Mustafa Ozmen
The objective of research was to examine the likely anticancer effectiveness of distinct pillar[5] arene derivatives, ws-penta-P[5] and ws-deca-P[5], on breast and lung cancer cell lines in vitro . To achieve this goal, breast cancer (MCF7) cells, lung cancer (A549) cells, healthy cells (HEK293) were utilized. The IC50 dose of ws-penta-P[5] and ws-deca-P[5] was determined using the MTT method. Both treatment (pillar[5] arene applied) and control (pillar[5] arene not applied) groups were established for all three cell lines...
March 25, 2024: Journal of Biomolecular Structure & Dynamics
https://read.qxmd.com/read/38525814/withaferin-a-alters-the-expression-of-micrornas-146a-5p-and-34a-5p-and-associated-hub-genes-in-mda-mb-231-cells
#40
JOURNAL ARTICLE
Mohd Shuaib, Smriti Chaudhri, Shashank Kumar
Triple-negative breast cancer (TNBC) is a highly metastatic subtype of breast cancer. Due to the absence of obvious therapeutic targets, microRNAs (miRNAs) provide possible hope to treat TNBC. Withaferin A (WA), a steroidal lactone, possesses potential anticancer activity with lesser side effects. The present study identifies hub genes ( CDKN3 , TRAF6 , CCND1 , JAK1 , MET , AXIN2 , JAG1 , VEGFA , BRCA1 , E2F3 , WNT1 , CDK6 , KRAS , MYB , MYCN , TGFβR2 , NOTCH1 , SIRT1 , MYCN , NOTCH2 , WNT3A ) from the list of predicted targets of the differentially expressed miRNAs (DEMs) in WA-treated MDA-MB-231 cells using in silico protein-protein interaction network analysis...
January 1, 2024: Biomolecular Concepts
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