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Molecular Diversity of Lupane Hybrids in Drug Design and Materials Science.

The need for new, more effective drugs to treat cancer, infectious diseases, various parasitic infestations, and metabolic disorders requires innovative approaches to the design of promising molecules. One of these areas is the creation of hybrid structures. Lupane triterpenoids are of significant interest for such research due to their high abundance in natural sources and their renewable nature, their molecular architecture, presence of several easily modifiable functional groups, enantiomeric purity, broad spectrum of biological activity, and low toxicity. Active research into the biologica

Recent Trends in anti-tumor mechanisms and molecular targets of celastrol.

Celastrol, a compound derived from traditional Chinese medicine, has therapeutic effects and has been used to treat inflammation-related diseases, cancer, cardiovascular diseases, and neurodegenerative diseases. However, current reviews lack a comprehensive and systematic summary of the anti-tumor mechanisms and molecular targets of celastrol. For this reason, this paper reviews the anticancer properties of celastrol and the molecular mechanisms underlying its anticancer effects. This paper primarily focuses on the mechanism of action of celastrol in terms of inhibition of cell proliferation a

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… cells and PC-3 | 0.5, 1.2, 4 µM | triggered autophagy and lipid droplet degradation, activated LXRα signaling | 49 gastric cancer | MKN1, MKN45, SNU216, SNU-668, and YCC-2 | 0, 0.25, 0.5, 1 µM | enhancement of autophagy-related proteins Atg 5↑, Atg 7↑, LC3 I↑, LC3 II and Beclin1↑ | 50 Inhibits cell … Celastrol induces apoptosis in non-small-cell lung cancer A549 cells through activation of mitochondria- and Fas/FasL-mediated pathways. Toxicol In Vitro. 2011;25:1027–32. doi: 10.1016/j.tiv.2011.03.023. 33. Cha Z, Cheng J, Xiang H, Qin J, He Y, Peng Z. et al. …

Каннабиноиды в раке: Молекулярные механизмы смерти клеток и возможности перевода.

Каннабиноиды представляют собой терпенофенолические соединения, полученные из Cannabis sativa L., которые осуществляют широкий спектр биологической и фармакологической деятельности. Растущие данные свидетельствуют об их потенциале как модуляторов развития рака, особенно посредством подавления роста клеток опухоли, ангиогенеза и метастаза в различных моделях опухоли. В настоящем обзоре содержится всеобъемлющий обзор молекулярных механизмов, с помощью которых природные и синтетические каннабиноиды вызывают регулируемую смерть раковых клеток. Текущие данные свидетельствуют о том, что каннабиноиды

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… . | [ 63 ] Lung cancer | A549 cells | Apoptosis | ↑ apoptosis-related proteins (p53, PARP, RIP1, RIP3, ATG12, Beclin). ↑ intracellular vesicle formation regulated by PPARγ. ↑ E-cadherin and vesicle-formation components (clathrin, β-adaptin, Tsg101). | [ 64 ] Colorectal cancer | HT-29, SW480, HCT-116, … cell viability ↑ chemotherapy drug efficacy | [ 79 ] CBD + CBG | Glioblastoma | U87, U373, and T98 cells | Apoptosis | Caspase 3 activation | [ 80 ] CBD + CBG + CBN | Ovarian cancer | HTB75 and HTB161 cells | Apoptosis | ↑ cleaved caspase 3 ↑ cleaved PARP ↑ DNA fragment | [ 81 ] CBN | Lung cancer | A549 …

Bioactivities and Mechanisms of Action of Sinomenine and Its Derivatives: A Comprehensive Review.

Sinomenine, an isoquinoline alkaloid extracted from the roots and stems of Sinomenium acutum, has been extensively studied for its derivatives as bioactive agents. This review concentrates on the research advancements in the biological activities and action mechanisms of sinomenine-related compounds until November 2023. The findings indicate a broad spectrum of pharmacological effects, including antitumor, anti-inflammation, neuroprotection, and immunosuppressive properties. These compounds are notably effective against breast, lung, liver, and prostate cancers, exhibiting IC50 values of appro

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… Jiang et al. reported that SIN (0.125–2.0 mM) reduced viability and induced apoptosis in A549 cells by diminishing JAK2, STAT3, p-STAT3, Snail, N-cadherin, and vimentin while increasing E-cadherin, highlighting the crucial role of the STAT3 signaling pathway in SIN’s anti-proliferative and anti-invasive … Liu. and co-workers reported that SIN (50–400 µM) counteracted cisplatin (3.8–16.8 µM) resistance in A549 cells. …

Targeting the p53 signaling pathway in cancers: Molecular mechanisms and clinical studies.

Tumor suppressor p53 can transcriptionally activate downstream genes in response to stress, and then regulate the cell cycle, DNA repair, metabolism, angiogenesis, apoptosis, and other biological responses. p53 has seven functional domains and 12 splice isoforms, and different domains and subtypes play different roles. The activation and inactivation of p53 are finely regulated and are associated with phosphorylation/acetylation modification and ubiquitination modification, respectively. Abnormal activation of p53 is closely related to the occurrence and development of cancer. While targeted t

Autophagic mechanisms in longevity intervention: role of natural active compounds.

The term 'autophagy' literally translates to 'self-eating' and alterations to autophagy have been identified as one of the several molecular changes that occur with aging in a variety of species. Autophagy and aging, have a complicated and multifaceted relationship that has recently come to light thanks to breakthroughs in our understanding of the various substrates of autophagy on tissue homoeostasis. Several studies have been conducted to reveal the relationship between autophagy and age-related diseases. The present review looks at a few new aspects of autophagy and speculates on how they m

A Recent Review on Cancer Nanomedicine.

Cancer is one of the most prevalent diseases globally and is the second major cause of death in the United States. Despite the continuous efforts to understand tumor mechanisms and various approaches taken for treatment over decades, no significant improvements have been observed in cancer therapy. Lack of tumor specificity, dose-related toxicity, low bioavailability, and lack of stability of chemotherapeutics are major hindrances to cancer treatment. Nanomedicine has drawn the attention of many researchers due to its potential for tumor-specific delivery while minimizing unwanted side effects

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… In A549 cells, with barely any expression of folate receptors, its cytotoxic effects were less pronounced. … N -acetyl- d -glucosamine (NAG)-conjugated PAMAM dendrimers were prepared to enhance camptothecin delivery to A549 cells expressing lectin receptors and glucose transporters [ 165 ]. NAG-coupled dendrimer was 4.5-fold more toxic to A549 cells than the free drug. …

Lung cancer immunotherapy: progress, pitfalls, and promises.

Lung cancer is the primary cause of mortality in the United States and around the globe. Therapeutic options for lung cancer treatment include surgery, radiation therapy, chemotherapy, and targeted drug therapy. Medical management is often associated with the development of treatment resistance leading to relapse. Immunotherapy is profoundly altering the approach to cancer treatment owing to its tolerable safety profile, sustained therapeutic response due to immunological memory generation, and effectiveness across a broad patient population. Different tumor-specific vaccination strategies are

The Hedgehog-GLI pathway in embryonic development and cancer: implications for pulmonary oncology therapy.

Transcriptional regulation and epigenetic mechanisms closely control gene expression through diverse physiological and pathophysiological processes. These include the development of germ layers and post-natal epithelial cell-tissue differentiation, as well as, involved with the induction, promotion and/or progression of human malignancies. Diverse studies have shed light on the molecular similarities and differences involved in the stages of embryological epithelial development and dedifferentiation processes in malignant tumors of epithelial origin, of which many focus on lung carcinomas. In

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… A549 cells possess higher level of expression of SHH, PTCH1, SMO and GLI-1, confirming previous reports where A549 remains the most adequate cellular model for the study of the SHH pathway in pulmonary, epithelial neoplasms (126). … cells and their histone code on the GLI1 promoter region, in presence of pharmacological challenge with cisplatin 8 μM at 48 hours, an enrichment of the activation marking H3K4me3 is seen, as well as a significant positioning of an activated RNA Pol II after the pharmacological challenge, suggesting …

Exploiting the Ref-1-APE1 node in cancer signaling and other diseases: from bench to clinic.

Reduction-oxidation factor 1-apurinic/apyrimidinic endonuclease (Ref-1/APE1) is a critical node in tumor cells, both as a redox regulator of transcription factor activation and as part of the DNA damage response. As a redox signaling protein, Ref-1/APE1 enhances the transcriptional activity of STAT3, HIF-1α, nuclear factor kappa B, and other transcription factors to promote growth, migration, and survival in tumor cells as well as inflammation and angiogenesis in the tumor microenvironment. Ref-1/APE1 is activated in a variety of cancers, including prostate, colon, pancreatic, ovarian, lung an

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… Decreasing Ref-1/APE1 levels in A549 cells in vitro and in vivo increases the effectiveness of photodynamic therapy. 204 Ref-1/APE1 knockdown with shRNA enhances the anti-tumor activity of oxymatrine, an alkaloid compound that inhibits proliferation of A549 cells. 205 Collectively, this demonstrates … cells to cisplatin and increased cell apoptosis. 202 Both of these studies point to Ref-1/APE1 function as critical in the cells’ response to cisplatin, especially in apoptosis signaling through STAT3. …

Applications of nanotechnologies for miRNA-based cancer therapeutics: current advances and future perspectives.

MicroRNAs (miRNAs) are short (18-25 nt), non-coding, widely conserved RNA molecules responsible for regulating gene expression via sequence-specific post-transcriptional mechanisms. Since the human miRNA transcriptome regulates the expression of a number of tumor suppressors and oncogenes, its dysregulation is associated with the clinical onset of different types of cancer. Despite the fact that numerous therapeutic approaches have been designed in recent years to treat cancer, the complexity of the disease manifested by each patient has prevented the development of a highly effective disease

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… Confocal microscopy demonstrated the efficient and selective uptake of the nano-complex by A549 cells. … Viability tests also evidenced that AMR-RF-exposed A549 cells displayed less survival rates ( Arrizabalaga et al., 2022 ) ( Figure 4B ). According to the results of the studies herein, the delivery of miRNAs via NPs holds promise as a potential treatment strategy for lung cancer. …

An Overview of Polymeric Nanoparticles-Based Drug Delivery System in Cancer Treatment.

Cancer is recognized as one of the world's deadliest diseases, with more than 10 million new cases each year. Over the past 2 decades, several studies have been performed on cancer to pursue solutions for effective treatment. One of the vital benefits of utilizing nanoparticles (NPs) in cancer treatment is their high adaptability for modification and amalgamation of different physicochemical properties to boost their anti-cancer activity. Various nanomaterials have been designed as nanocarriers attributing nontoxic and biocompatible drug delivery systems with improved bioactivity. The present

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… . | Carbon Nanotube (DTX-CNTP-Tf) | 241-483 nm in length | Higher cytotoxicity, low ROS generation, and low toxic profile when conjugated with transferrin | Lung cancer (A549 cells) | Docetaxel | 44 9. | Silica Nanoparticle | 4 nm | Cell internalization improved in the simulated medium | Prostate cancer … Sl. no. | Types of Polymers | Encapsulated Drug | Size (nm) | Loading Amount | Types of Cancer Treatment/mice Used/(in Vivo, in Vitro) | Effectiveness | Ref. 1. | PEO-PPO-PEO | Curcumin | 270-310 | 14.6% | Lung (A549 cell) and skin (A375 cell) cancer; in vivo | 34-fold (lung), 32-fold (skin) decrease …

Natural bioactive molecules and chemotherapeutics synergism for enhanced cancer therapy.

BACKGROUND: Chemotherapy remains a foundation of cancer care but is limited by multidrug resistance, systemic toxicities, and suboptimal selectivity, prompting interest in adjunctive strategies that improve efficacy and tolerability without adding significant burden to patients or healthcare systems. AIMS/OBJECTIVES: This review highlights evidence on natural bioactive compounds, including polyphenols, alkaloids, terpenoids, and fungal metabolites, as adjuvants to standard chemotherapeutics, with objectives to: first, delineate mechanisms by which these agents enhance cytotoxic efficacy and o

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… In this context, oridonin is one these natural bioactives that has shown promise in sensitizing cisplatin-induced apoptosis via AMPK/Akt/mTOR-dependent autophagosome accumulation in A549 cells [ 300 ]. …

CPUY201112, a novel synthetic small-molecule compound and inhibitor of heat shock protein Hsp90, induces p53-mediated apoptosis in MCF-7 cells.

Heat-shock protein 90 (Hsp90) is highly expressed in many tumor cells and is associated with the maintenance of malignant phenotypes. Targeting Hsp90 has had therapeutic success in both solid and hematological malignancies, which has inspired more studies to identify new Hsp90 inhibitors with improved clinical efficacy. Using a fragment-based approach and subsequent structural optimization guided by medicinal chemistry principles, we identified the novel compound CPUY201112 as a potent Hsp90 inhibitor. It binds to the ATP-binding pocket of Hsp90 with a kinetic dissociation (Kd) constant of 27

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… A549 cells were cultured in F12K supplemented with 10% fetal calf serum and antibiotics. Hep-G2 and MCF-7 cells were cultured in MEM. HCT116, SAOS, and HT29 cells were cultured in McCOY’s 5A, and other cancer cell lines were cultured in supplemented RPMI-1640 medium. …

Osteolytic Breast Cancer Causes Skeletal Muscle Weakness in an Immunocompetent Syngeneic Mouse Model.

Muscle weakness and cachexia are significant paraneoplastic syndromes of many advanced cancers. Osteolytic bone metastases are common in advanced breast cancer and are a major contributor to decreased survival, performance, and quality of life for patients. Pathologic fracture caused by osteolytic cancer in bone (OCIB) leads to a significant (32%) increased risk of death compared to patients without fracture. Since muscle weakness is linked to risk of falls which are a major cause of fracture, we have investigated skeletal muscle response to OCIB. Here, we show that a syngeneic mouse model of

Targeting the AMP-Activated Protein Kinase for Cancer Prevention and Therapy.

Despite the advances in biomedical research and clinical applications, cancer remains a leading cause of death worldwide. Given the limitations of conventional chemotherapeutics, including serious toxicities and reduced quality of life for patients, the development of safe and efficacious alternatives with known mechanism of action is much needed. Prevention of cancer through dietary intervention may hold promise and has been investigated extensively in the recent years. AMP-activated protein kinase (AMPK) is an energy sensor that plays a key role in the regulation of protein and lipid metabol

Диметилфумарат способствует разложению HNF1B и подавляет прогрессирование чистой почечной карциномы.

Чистая почечная карцинома (ccRCC) является самым смертельным подтипом рака почек, и его варианты лечения по-прежнему ограничены. Поэтому необходимо срочно найти лечебные агенты для лечения CCRCC. Здесь мы показываем, что диметилфумарат (ДМФ), одобренное лекарство от множественных склерозов [1] и псориаза, может сдерживать распространение клеток ЦКЦК. Механистически, гепатоцитовый ядерный фактор 1β (HNF1B), коэффициент транскрипции, ярко выраженный в CCRCC, поддерживается DMF в остатках цистейна, что ведет к его протеасомальной деградации. Кроме того, HNF1B взаимодействует с протеином, связанны

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… A549 cells were cultured in F-12 medium, while H1299 and KTC-1 cells were maintained in RPMI 1640. All media were supplemented with 10% fetal bovine serum (FBS) (Biological Industries, Israel) and 1% penicillin/streptomycin (P/S). …

Gossypol and Its Natural Derivatives: Multitargeted Phytochemicals as Potential Drug Candidates for Oncologic Diseases.

Despite the vast amounts of research and remarkable discoveries that have been made in recent decades, cancer remains a leading cause of death and a major public health concern worldwide. Gossypol, a natural polyphenolic compound derived from the seeds, roots, and stems of cotton (Gossypium hirsutum L.), was first used as a male contraceptive agent. Due to its diverse biological properties, including antifertility, antiviral, antioxidant, antibacterial, antimalarial, and most notably antitumor activities, gossypol has been the subject of numerous studies. Nevertheless, no systematic review has

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… In contrast, the combination of Pluronic P85 and (−)-gossypol substantially reduced clonogenic survival of A549 cells and increased radiation cancer cell death. …

The role and mechanisms of action of microRNAs in cancer drug resistance.

MicroRNAs (miRNAs) are small non-coding RNAs with a length of about 19-25 nt, which can regulate various target genes and are thus involved in the regulation of a variety of biological and pathological processes, including the formation and development of cancer. Drug resistance in cancer chemotherapy is one of the main obstacles to curing this malignant disease. Statistical data indicate that over 90% of the mortality of patients with cancer is related to drug resistance. Drug resistance of cancer chemotherapy can be caused by many mechanisms, such as decreased antitumor drug uptake, modified

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… Let-7c is able to target ABCC2 and Bcl-xl simultaneously, reducing their expression, and promoting sensitivity of A549 cells to CDDP [ 57 ]. … Zhan M Qu Q Wang G Zhou HH Let-7c sensitizes acquired cisplatin-resistant A549 cells by targeting ABCC2 and Bcl-XL Pharmazie 2013 68 12 955 961 24400442 58. …

Cuproptosis Inducers in Cancer Therapy: State of the Art and Challenges.

Cancer continues to be the primary cause of death despite significant progress in medicine, and finding effective therapies remains a challenge. New treatments are needed to minimize the harmful effects on the body and increase the selectivity of drugs. These therapies must also overcome cancer cell resistance and prevent metastasis. Metal-based drugs are becoming increasingly crucial for treating tumors, and copper ion-based systems and nanoparticles have been identified as having unique properties and anticancer potential. Given the key role exerted by Cu in the etiology, severity, and progr

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… Li et al. investigated the combination of DSF and anti‐PD‐L1 therapy in A549 cells, a human NSCLC cell line [ 64 ]. They found that DSF treatment increased the expression of ATP7B and PD‐L1. …