scholarly journals EUDESMANE SESQUITERPENE LACTONES OF THE GENUS INULA AND THEIR BIOLOGICAL ACTIVITY

2021 ◽  
pp. 19-38
Author(s):  
Sergey Aleksandrovich Pukhov ◽  
Sergey Georgievich Klochkov ◽  
Svetlana Vasilievna Afanas'yeva
Keyword(s):  
Biological Activity ◽  
Antitumor Agents ◽  
Sesquiterpene Lactones ◽  
Structural Type ◽  
Farnesyl Pyrophosphate ◽  
Biological Models ◽  
Natural Plant ◽  
Wide Range ◽  
Medical Chemistry ◽  
Plant Compounds

Sesquiterpene lactones (SL) are widely distributed in nature (formed biosynthetically in plants from farnesyl pyrophosphate) and are a structurally diverse class of terpenoids with 15 carbon atoms in the skeleton and, in addition to the lactone cycle, can contain various functional groups. Some of them exhibit biological activity both in a rather wide range and in relation to a specific target. An increase in the number of undescribed natural plant compounds of this class, as well as detection in various plant species, opens up new possibilities for their use for the purposes of medical chemistry, phytochemistry, pharmacognosy, chemotaxonomy, and related fields. Using the example of SL of the eudesmane structural type found in plants of the genus Inula, this review attempts to show the relevance of studies of such compounds that investigate the mechanism of action on various biological models, including the goal of developing new effective antitumor agents.

scholarly journals Potential Therapeutic Effects of Natural Plant Compounds in Kidney Disease

Molecules ◽  
2021 ◽  
Vol 26 (20) ◽  
pp. 6096
Author(s):  
Lorena Avila-Carrasco ◽  
Elda Araceli García-Mayorga ◽  
Daisy L. Díaz-Avila ◽  
Idalia Garza-Veloz ◽  
Margarita L Martinez-Fierro ◽  
...  
Keyword(s):  
Kidney Disease ◽  
Clinical Studies ◽  
Renal Damage ◽  
Therapeutic Potential ◽  
Therapeutic Effects ◽  
Protective Agent ◽  
Natural Plant ◽  
Wide Range ◽  
The Impact ◽  
Plant Compounds

Background: The blockade of the progression or onset of pathological events is essential for the homeostasis of an organism. Some common pathological mechanisms involving a wide range of diseases are the uncontrolled inflammatory reactions that promote fibrosis, oxidative reactions, and other alterations. Natural plant compounds (NPCs) are bioactive elements obtained from natural sources that can regulate physiological processes. Inflammation is recognized as an important factor in the development and evolution of chronic renal damage. Consequently, any compound able to modulate inflammation or inflammation-related processes can be thought of as a renal protective agent and/or a potential treatment tool for controlling renal damage. The objective of this research was to review the beneficial effects of bioactive natural compounds on kidney damage to reveal their efficacy as demonstrated in clinical studies. Methods: This systematic review is based on relevant studies focused on the impact of NPCs with therapeutic potential for kidney disease treatment in humans. Results: Clinical studies have evaluated NPCs as a different way to treat or prevent renal damage and appear to show some benefits in improving OS, inflammation, and antioxidant capacity, therefore making them promising therapeutic tools to reduce or prevent the onset and progression of KD pathogenesis. Conclusions: This review shows the promising clinical properties of NPC in KD therapy. However, more robust clinical trials are needed to establish their safety and therapeutic effects in the area of renal damage.

Enzymes as a Reservoir of Host Defence Peptides

2020 ◽  
Vol 20 (14) ◽  
pp. 1310-1323
Author(s):  
Andrea Bosso ◽  
Antimo Di Maro ◽  
Valeria Cafaro ◽  
Alberto Di Donato ◽  
Eugenio Notomista ◽  
...  
Keyword(s):  
Innate Immunity ◽  
Biological Activity ◽  
Internal Structure ◽  
Catalytic Properties ◽  
Cellular Responses ◽  
Host Defence ◽  
Present Review ◽  
Active Peptides ◽  
Wide Range

Host defence peptides (HDPs) are powerful modulators of cellular responses to various types of insults caused by pathogen agents. To date, a wide range of HDPs, from species of different kingdoms including bacteria, plant and animal with extreme diversity in structure and biological activity, have been described. Apart from a limited number of peptides ribosomally synthesized, a large number of promising and multifunctional HDPs have been identified within protein precursors, with properties not necessarily related to innate immunity, consolidating the fascinating hypothesis that proteins have a second or even multiple biological mission in the form of one or more bio-active peptides. Among these precursors, enzymes constitute certainly an interesting group, because most of them are mainly globular and characterized by a fine specific internal structure closely related to their catalytic properties and also because they are yet little considered as potential HDP releasing proteins. In this regard, the main aim of the present review is to describe a panel of HDPs, identified in all canonical classes of enzymes, and to provide a detailed description on hydrolases and their corresponding HDPs, as there seems to exist a striking link between these structurally sophisticated catalysts and their high content in cationic and amphipathic cryptic peptides.

Studies on the EC50 of Natural Monoterpenes as Fungal Inhibitors with Quantitative Structure-Activity Relationships (QSARs)

2020 ◽  
Vol 10 (1) ◽  
pp. 44-60
Author(s):  
Mohamed E.I. Badawy ◽  
Entsar I. Rabea ◽  
Samir A.M. Abdelgaleil
Keyword(s):  
Biological Activity ◽  
Plant Pathogens ◽  
Molecular Descriptors ◽  
Microbial Pathogens ◽  
Quantitative Structure ◽  
Qsar Study ◽  
Qsar Analysis ◽  
Pharmacophore Modelling ◽  
Structure Activity ◽  
Wide Range

Background:Monoterpenes are the main constituents of the essential oils obtained from plants. These natural products offered wide spectra of biological activity and extensively tested against microbial pathogens and other agricultural pests.Methods:Antifungal activity of 10 monoterpenes, including two hydrocarbons (camphene and (S)- limonene) and eight oxygenated hydrocarbons ((R)-camphor, (R)-carvone, (S)-fenchone, geraniol, (R)-linalool, (+)-menthol, menthone, and thymol), was determined against fungi of Alternaria alternata, Botrytis cinerea, Botryodiplodia theobromae, Fusarium graminearum, Phoma exigua, Phytophthora infestans, and Sclerotinia sclerotiorum by the mycelia radial growth technique. Subsequently, Quantitative Structure-Activity Relationship (QSAR) analysis using different molecular descriptors with multiple regression analysis based on systematic search and LOOCV technique was performed. Moreover, pharmacophore modelling was carried out using LigandScout software to evaluate the common features essential for the activity and the hypothetical geometries adopted by these ligands in their most active forms.Results:The results showed that the antifungal activities were high, but depended on the chemical structure and the type of microorganism. Thymol showed the highest effect against all fungi tested with respective EC50 in the range of 10-86 mg/L. The QSAR study proved that the molecular descriptors HBA, MR, Pz, tPSA, and Vp were correlated positively with the biological activity in all of the best models with a correlation coefficient (r) ≥ 0.98 and cross-validated values (Q2) ≥ 0.77.Conclusion:The results of this work offer the opportunity to choose monoterpenes with preferential antimicrobial activity against a wide range of plant pathogens.

Accurate prediction of 195Pt NMR chemical shifts for a series of Pt(ii) and Pt(iv) antitumor agents by a non-relativistic DFT computational protocol

2014 ◽  
Vol 43 (14) ◽  
pp. 5409-5426 ◽  
Author(s):  
Athanassios C. Tsipis ◽  
Ioannis N. Karapetsas
Keyword(s):  
Dft Calculations ◽  
Anticancer Agents ◽  
Antitumor Agents ◽  
Chemical Shifts ◽  
Accurate Prediction ◽  
Nmr Chemical Shifts ◽  
Relativistic Dft ◽  
Square Planar ◽  
Wide Range ◽  
Computational Protocol

Exhaustive benchmark DFT calculations reveal that the non-relativistic GIAO-PBE0/SARC-ZORA(Pt)∪6-31+G(d)(E) computational protocol predicts accurate 195Pt NMR chemical shifts for a wide range of square planar Pt(ii) and octahedral Pt(iv) anticancer agents.

Synthesis and biological activity of selenopsammaplin A and its analogues as antitumor agents with DOT1L inhibitory activity

2021 ◽  
Vol 35 ◽  
pp. 116072 ◽  
Author(s):  
Hae Ju Han ◽  
Woong Sub Byun ◽  
Gyu Ho Lee ◽  
Won Kyung Kim ◽  
Kyungkuk Jang ◽  
...  
Keyword(s):  
Biological Activity ◽  
Inhibitory Activity ◽  
Antitumor Agents

scholarly journals Synthesis of Novel Tryptamine Derivatives and Their Biological Activity as Antitumor Agents

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 683
Author(s):  
Giorgia Simonetti ◽  
Carla Boga ◽  
Joseph Durante ◽  
Gabriele Micheletti ◽  
Dario Telese ◽  
...  
Keyword(s):  
Biological Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Solid Tumor ◽  
Antitumor Agents ◽  
Cancer Cell Lines ◽  
Hematological Cancer ◽  
Selective Effect ◽  
Ht29 Cells ◽  
High Level

We synthesized five novel tryptamine derivatives characterized by the presence of an azelayl chain or of a 1,1,1-trichloroethyl group, in turn connected to another heterocyclic scaffold. The combination of tryptamin-, 1,1,1-trichloroethyl- and 2-aminopyrimidinyl- moieties produced compound 9 identified as the most active compound in hematological cancer cell lines (IC50 = 0.57–65.32 μM). Moreover, keeping constant the presence of the tryptaminic scaffold and binding it to the azelayl moiety, the compounds maintain biological activity. Compound 13 is still active against hematological cancer cell lines and shows a selective effect only on HT29 cells (IC50 = 0.006 µM) among solid tumor models. Compound 14 loses activity on all leukemic lines, while showing a high level of toxicity on all solid tumor lines tested (IC50 0.0015–0.469 µM).

1-Methyl-3H-pyrazolo[1,2-a]benzo[1,2,3,4]tetrazin-3-ones. Design, Synthesis, and Biological Activity of New Antitumor Agents

2005 ◽  
Vol 48 (8) ◽  
pp. 2859-2866 ◽  
Author(s):  
Anna Maria Almerico ◽  
Francesco Mingoia ◽  
Patrizia Diana ◽  
Paola Barraja ◽  
Antonino Lauria ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antitumor Agents ◽  
Design Synthesis

scholarly journals Design, Synthesis, and Biological Activity of Sulfonamide Analogues of Antofine and Cryptopleurine as Potent and Orally Active Antitumor Agents

2015 ◽  
Vol 58 (19) ◽  
pp. 7749-7762 ◽  
Author(s):  
Yongseok Kwon ◽  
Jayoung Song ◽  
Honggu Lee ◽  
Eun-Yeong Kim ◽  
Kiho Lee ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antitumor Agents ◽  
Design Synthesis ◽  
Orally Active

Synthesis and biological activity of stable and potent antitumor agents, aniline nitrogen mustards linked to 9-anilinoacridines via a urea linkage

2008 ◽  
Vol 16 (10) ◽  
pp. 5413-5423 ◽  
Author(s):  
Naval Kapuriya ◽  
Kalpana Kapuriya ◽  
Xiuguo Zhang ◽  
Ting-Chao Chou ◽  
Rajesh Kakadiya ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antitumor Agents ◽  
Nitrogen Mustards

Pyridine moiety: An insight into recent advances in treatment of cancer

2021 ◽  
Vol 21 ◽  
Author(s):  
Rakesh Sahu ◽  
Rakhi Mishra ◽  
Rajnish Kumar ◽  
Salahuddin ◽  
Chandana Majee ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Antitumor Agents ◽  
Pyridine Moiety ◽  
Structure Activity ◽  
Wide Range ◽  
Global Health Issue ◽  
Effective Drugs ◽  
Published Research ◽  
Insight Into

: The incidence of cancer is increasing worldwide, affecting a vast majority of the human population. As new different anticancer agents are being developed now, the requirement is to deal somehow with them and evaluate their safety. Among them, pyridine based drugs are contributing a lot, as it is one of the imperative pharmacophores occurring synthetically as well as naturally in heterocyclic compounds, and having a wide range of therapeutic applications in the area of drug discovery, thereby offering many chances for further improvement in antitumor agents via acting onto numerous receptors of extreme prominence. Many pyridine derivatives have been reported to inhibit enzymes, receptors and many other targets for controlling and curing the global health issue of cancer. Nowadays, in combination with other moieties, researchers are focusing on the development of pyridine-based new derivatives for cancer treatment. Therefore, this review sheds light on the recent therapeutic expansions of pyridine together with its molecular docking, structure-activity-relationship, availability in the market, and a summary of recently patented and published research works that shall jointly help the scientists to produce effective drugs with the desired pharmacological activity.

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