scholarly journals Bile Acid Conjugates with Anticancer Activity: Most Recent Research

Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 25
Author(s):  
Maria Luisa Navacchia ◽  
Elena Marchesi ◽  
Daniela Perrone
Keyword(s):  
Bile Acid ◽  
Cancer Therapy ◽  
Anticancer Activity ◽  
Bile Acids ◽  
Treatment Modality ◽  
Biological Properties ◽  
Therapeutic Agents ◽  
Bioactive Molecules ◽  
Hybrid Functional ◽  
Hybrid Molecules

The advantages of a treatment modality that combines two or more therapeutic agents in cancer therapy encourages the study of hybrid functional compounds for pharmacological applications. In light of this, we reviewed recent works on hybrid molecules based on bile acids. Due to their biological properties, as well as their different chemical/biochemical reactive moieties, bile acids can be considered very interesting starting molecules for conjugation with natural or synthetic bioactive molecules.

scholarly journals Developing Picornaviruses for Cancer Therapy

Cancers ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 685 ◽  
Author(s):  
Cormac McCarthy ◽  
Nadishka Jayawardena ◽  
Laura N. Burga ◽  
Mihnea Bostina
Keyword(s):  
Cancer Therapy ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Rna Viruses ◽  
Therapeutic Agents ◽  
Oncolytic Viruses ◽  
Wide Range ◽  
Positive Sense

Oncolytic viruses (OVs) form a group of novel anticancer therapeutic agents which selectively infect and lyse cancer cells. Members of several viral families, including Picornaviridae, have been shown to have anticancer activity. Picornaviruses are small icosahedral non-enveloped, positive-sense, single-stranded RNA viruses infecting a wide range of hosts. They possess several advantages for development for cancer therapy: Their genomes do not integrate into host chromosomes, do not encode oncogenes, and are easily manipulated as cDNA. This review focuses on the picornaviruses investigated for anticancer potential and the mechanisms that underpin this specificity.

Development and Advances of Drugs for Cancer Theranostics – PART-IV

2021 ◽  
Vol 21 (18) ◽  
pp. 1644-1644
Author(s):  
Lian-Shun Feng
Keyword(s):  
Drug Discovery ◽  
Side Effects ◽  
Anticancer Activity ◽  
Anticancer Drug ◽  
Anticancer Agents ◽  
Drug Repurposing ◽  
Biological Properties ◽  
Drug Candidates ◽  
Pharmacokinetic Profiles ◽  
Hybrid Molecules

Cancer, a highly heterogeneous disease at intra/inter patient levels, is one of the most serious threats to human health across the world [1, 2]. Notwithstanding the noteworthy advances in its treat-ment, the morbidity and mortality of cancer are projected to grow for a long period, and the global cancer burden is expected to be 28.4 million cases in 2040, a 47% rise from 2020 [3]. Accordingly, there is a constant need to explore novel anticancer agents. <p> There are several strategies to discover novel anticancer candidates: (1) new lead hits or candidates from natural resources [4] whichexhibit various biological properties and are a rich source of com-pounds in drug discovery due to the structural and mechanistic diversity, and more than 60% anti-cancer agents can be traced to a natural product; (2) Molecular hybridization is one of the most prom-ising strategies for the discovery of novel anticancer drug candidates since hybrid molecules have the potential to bind multiple targets or to enhance the effect through acting with another bio-target or to counterbalance the side effects caused by the other part of the hybrid [5]; (3) Dimerization is a useful tool to develop novel anticancer drug candidates with enhanced biological activity, reduced side effects and improved pharmacokinetic profiles [6]; (4) Drug repurposing strategy is is an attractive strategy and has been approved, along with non-anticancer macrolide drugs for the treatment of cancer, for anticancer drug discovery since toxicity and pharmacokinetic profiles have already been estab-lished [7]. <p> Heterocycles coumarin, β-lactone, macrolide and triazole are useful anticancer pharmacophores since their derivatives could exert the anticancer activity through diverse mechanisms, inclusive of inhibition of aromatase, carbonic anhydrase, ki-nase, P-glycoprotein, sulfatase, telomerase, vascular endothelial growth factor receptor 2 and tubulin [8-11]. In particular, nat-ural-derived coumarin, β-lactone and macrolide derivatives are important sources of new anticancer lead hits/candidates; mac-rolide repurposed drugs can circumvent high cost and long-time associated with traditional drug discovery strategies; couma-rin, β-lactone and macrolide hybrids as well as bis-triazole compounds have the potential to enhance the anticancer activity, overcome drug resistance, reduce the side effects and improve pharmacokinetic profiles.

scholarly journals Development and Validation of a Highly Sensitive LC-MS/MS Method for the Analysis of Bile Acids in Serum, Plasma, and Liver Tissue Samples

Metabolites ◽  
2020 ◽  
Vol 10 (7) ◽  
pp. 282
Author(s):  
Cristina Gómez ◽  
Simon Stücheli ◽  
Denise V. Kratschmar ◽  
Jamal Bouitbir ◽  
Alex Odermatt
Keyword(s):  
Bile Acid ◽  
Liver Injury ◽  
Bile Acids ◽  
Liver Tissue ◽  
Bioactive Molecules ◽  
Rodent Species ◽  
Drug Induced ◽  
Tissue Samples ◽  
Drug Induced Liver Injury ◽  
Bile Acid Profiles

Bile acids control lipid homeostasis by regulating uptake from food and excretion. Additionally, bile acids are bioactive molecules acting through receptors and modulating various physiological processes. Impaired bile acid homeostasis is associated with several diseases and drug-induced liver injury. Individual bile acids may serve as disease and drug toxicity biomarkers, with a great demand for improved bile acid quantification methods. We developed, optimized, and validated an LC-MS/MS method for quantification of 36 bile acids in serum, plasma, and liver tissue samples. The simultaneous quantification of important free and taurine- and glycine-conjugated bile acids of human and rodent species has been achieved using a simple workflow. The method was applied to a mouse model of statin-induced myotoxicity to assess a possible role of bile acids. Treatment of mice for three weeks with 5, 10, and 25 mg/kg/d simvastatin, causing adverse skeletal muscle effects, did not alter plasma and liver tissue bile acid profiles, indicating that bile acids are not involved in statin-induced myotoxicity. In conclusion, the established LC-MS/MS method enables uncomplicated sample preparation and quantification of key bile acids in serum, plasma, and liver tissue of human and rodent species to facilitate future studies of disease mechanisms and drug-induced liver injury.

scholarly journals Recent Advances in Exosome-Based Drug Delivery for Cancer Therapy

Cancers ◽  
2021 ◽  
Vol 13 (17) ◽  
pp. 4435
Author(s):  
Hyosuk Kim ◽  
Hochung Jang ◽  
Haeun Cho ◽  
Jiwon Choi ◽  
Kwang Yeon Hwang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cancer Therapy ◽  
Nucleic Acids ◽  
Extracellular Vesicles ◽  
Targeted Delivery ◽  
Drug Delivery Systems ◽  
Therapeutic Agents ◽  
Bioactive Molecules ◽  
Chemotherapeutic Drugs ◽  
Efficient Delivery

Exosomes are a class of extracellular vesicles, with a size of about 100 nm, secreted by most cells and carrying various bioactive molecules such as nucleic acids, proteins, and lipids, and reflect the biological status of parent cells. Exosomes have natural advantages such as high biocompatibility and low immunogenicity for efficient delivery of therapeutic agents such as chemotherapeutic drugs, nucleic acids, and proteins. In this review, we introduce the latest explorations of exosome-based drug delivery systems for cancer therapy, with particular focus on the targeted delivery of various types of cargoes.

scholarly journals Bile acid metabolites control Th17 and Treg cell differentiation

2018 ◽  
Author(s):  
Saiyu Hang ◽  
Donggi Paik ◽  
A. Sloan Devlin ◽  
Trinath Jamma ◽  
Jingping Lu ◽  
...  
Keyword(s):  
T Cells ◽  
Bile Acid ◽  
Cell Differentiation ◽  
Bile Acids ◽  
Treg Cell ◽  
Inflammatory Responses ◽  
Bioactive Molecules ◽  
Orphan Receptor ◽  
Adaptive Immune Cells ◽  
Acid Metabolites

AbstractBile acids are abundantly present in the mammalian gut, where they undergo bacteria-mediated transformation, generating a large pool of bioactive molecules. While they have been shown to affect host metabolism, cancer progression and innate immunity, it is unknown whether bile acids affect the function of adaptive immune cells such as T cells expressing IL-17a (Th17 cells) and regulatory T cells (Tregs) that mediate inflammatory and anti-inflammatory responses, respectively. By screening a small-molecule library primarily composed of bile acid metabolites, we identified two distinct derivatives of lithocholic acid (LCA), 3-oxoLCA and isoalloLCA, as specific regulators of Th17 and Treg cells. While 3-oxoLCA inhibited Th17 cell differentiation by directly binding to its key transcription factor RORγt (retinoid-related orphan receptor γ t), isoalloLCA enhanced differentiation of Tregs through mitochondrial-dependent metabolic changes, leading to an increased expression of Foxp3. IsoalloLCA-dependent Treg enhancement required an intronic Foxp3 enhancer, the conserved noncoding sequence 3 (CNS3), which acts as an epigenetic switch that confers a poised state to the Foxp3 promoter. Lastly, oral administration of 3-oxoLCA and isoalloLCA to mice led to reduced Th17 and increased Treg cell differentiation in the intestinal lamina propria. Altogether, our data suggest novel mechanisms by which bile acid metabolites control host immune responses by directly modulating the Th17 and Treg balance.

scholarly journals Synthesis of New Cisplatin Derivatives from Bile Acids

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 655
Author(s):  
Barbara Seroka ◽  
Zenon Łotowski ◽  
Agnieszka Hryniewicka ◽  
Lucie Rárová ◽  
Rafal R. Sicinski ◽  
...  
Keyword(s):  
Bile Acid ◽  
Bile Acids ◽  
Cytotoxicity Assays ◽  
Cytotoxic Compound ◽  
Hybrid Molecules

A series of bile acid derived 1,2- and 1,3-diamines as well as their platinum(II) complexes were designed and synthesized in hope to get a highly cytotoxic compound by the combination of two bioactive moieties. All complexes obtained were subjected to cytotoxicity assays in vitro and some hybrid molecules showed an expected activity.

Bile acids and bile acid derivatives: use in drug delivery systems and as therapeutic agents

2016 ◽  
Vol 13 (8) ◽  
pp. 1133-1148 ◽  
Author(s):  
Célia Faustino ◽  
Cláudia Serafim ◽  
Patrícia Rijo ◽  
Catarina Pinto Reis
Keyword(s):  
Drug Delivery ◽  
Bile Acid ◽  
Bile Acids ◽  
Drug Delivery Systems ◽  
Therapeutic Agents ◽  
Delivery Systems ◽  
Bile Acid Derivatives

Bio-organometallic Peptide Conjugates: Recent Advances in Their Synthesis and Prospects for Biomedical Application

2020 ◽  
Vol 24 (21) ◽  
pp. 2508-2523
Author(s):  
Johana Gómez ◽  
Diego Sierra ◽  
Constanza Cárdenas ◽  
Fanny Guzmán
Keyword(s):  
Amino Acids ◽  
Biomedical Application ◽  
Structural Diversity ◽  
Biological Properties ◽  
Therapeutic Agents ◽  
Organometallic Complexes ◽  
Chemical Behavior ◽  
Metal Compounds ◽  
Bioorganometallic Chemistry ◽  
Pharmacological Control

One area of organometallic chemistry that has attracted great interest in recent years is the syntheses, characterization and study of organometallic complexes conjugated to biomolecules with different steric and electronic properties as potential therapeutic agents against cancer and malaria, as antibiotics and as radiopharmaceuticals. This minireview focuses on the unique structural diversity that has recently been discovered in α- amino acids and the reactions of metallocene complexes with peptides having different chemical behavior and potential medical applications. Replacing α-amino acids with metallocene fragments is an effective way of selectively influencing the physicochemical, structural, electrochemical and biological properties of the peptides. Consequently, research in the field of bioorganometallic chemistry offers the opportunity to develop bioactive metal compounds as an innovative and promising approach in the search for pharmacological control of different diseases.

Synthesis and Biological Properties of some New Lead Sulphonamide and Carboxamide Scaffolds Bearing Coumarin Moiety (Mini Review)

2020 ◽  
Vol 20 ◽  
Author(s):  
Cosmas Chinweike Eze ◽  
Mercy Amarachukwu Ezeokonkwo ◽  
Benjamin Ebere Ezema ◽  
Abraham Efeturi Onoabedje ◽  
David Izuchukwu Ugwu
Keyword(s):  
Biological Properties ◽  
Therapeutic Agents ◽  
Amide Group ◽  
Pharmacological Properties ◽  
Important Class ◽  
Synthetic Route ◽  
Therapeutic Activities

: Coumarin, sulphonamide and amide scaffolds exhibit diverse pharmacological features and constitute an important class of therapeutic agents. In this review, we have discussed the synthesis, biological properties, and SAR of coumarins containing sulphonamide or amide group in the last seven years. Many reviews on the therapeutic activities of coumarins, sulphonamides, and amides have been published, hence the authors focused on coumarin-linked sulphonamide or amide scaffolds. The review provides information on the synthetic route to new coumarins containing sulphonamide or amide groups with improved pharmacological properties.

Coumarin Hybrids: Promising Scaffolds in the Treatment of Breast Cancer

2019 ◽  
Vol 19 (17) ◽  
pp. 1443-1458 ◽  
Author(s):  
Rohit Bhatia ◽  
Ravindra K. Rawal
Keyword(s):  
Breast Cancer ◽  
Lung Cancer ◽  
Therapeutic Agents ◽  
Toxicity Profile ◽  
Biological Targets ◽  
Organ Systems ◽  
Hybrid Molecules ◽  
Cause Of Deaths ◽  
Low Toxicity ◽  
Diverse Mode

: Breast cancer is the most common invasive cancer in women, and the second main cause of deaths in women, after lung cancer. There is continuous advancement in the development of therapeutic agents against breast cancer in recent years and it is still in progress. Development of hybrid molecules by combining different pharmacophores to obtain significant biological activity is an excellent approach. Coupling of coumarin scaffold with other distinct motifs has led to the design of newer compounds against breast cancer. These distinct pharmacophores possess a diverse mode of action as well as selectivity. It has been reported in the literature that coumarin hybrids possess significant potency against breast cancer by binding to various biological targets which are associated with breast cancer. Due to low toxicity profile on various organ systems, coumarin hybrids have nowadays attracted the keen attention of researchers to explore their therapeutic ability against breast cancer. Reported coumarin hybrids include coupling with isoxazole, thiazole, monastrol, chalcone, triazole, sulphonamide, triphenylethylene, benzimidazole, pyran, imidazole, stilbene, oestrogen, phenylsulphonylfuroxan, etc. In the present review, a description of various coumarin hybrid molecules has been presented along with their structural-activity relationships.

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