Toxins Are an Excellent Source of Therapeutic Agents against Cardiovascular Diseases

2018 ◽  
Vol 44 (07) ◽  
pp. 691-706 ◽  
Author(s):  
Cho Yeow Koh ◽  
Cassandra Modahl ◽  
Namrata Kulkarni ◽  
R. Manjunatha Kini
Keyword(s):  
Cardiovascular Diseases ◽  
Biological Activities ◽  
Antiplatelet Agents ◽  
Therapeutic Agents ◽  
Bioactive Molecules ◽  
Function Mechanism ◽  
Physiological Processes ◽  
Self Defense ◽  
Diagnostic Agents ◽  
Proteins And Peptides

AbstractVenomous and hematophagous animals use their venom or saliva for survival, to obtain food, and for self-defense. Venom and saliva from these animals are cocktails of bioactive molecules primarily composed of proteins and peptides. These molecules are called toxins because they cause unwanted consequences on prey. They exhibit unique, diverse, and specific biological activities that perturb normal physiological processes of their prey and host. However, the potential of toxins as inspirations for the development of therapeutic agents or pharmacological tools has also long been recognized. In addition to their small size, the exquisite selectivity and structural stability of toxins make them attractive as starting molecule in the development of therapeutic and diagnostic agents. Drug discovery and development from venomous and hematophagous animals against cardiovascular diseases have been particularly successful. Some of the notable success include antihypertensive (captopril and enalapril) and antiplatelet agents (tirofiban and eptifibatide), as well as anticoagulants (lepirudin and bivalirudin). Highlighted in this review are many venom or saliva-derived cardiovascular-active proteins and peptides of therapeutic interest, including those that are currently in preclinical stages and those that have been approved by FDA and currently in the market. The authors attempt to summarize their structure, function, mechanism of action, and development with respect to cardiovascular diseases.

scholarly journals Extracellular Vesicles in Cardiovascular Diseases: Alternative Biomarker Sources, Therapeutic Agents, and Drug Delivery Carriers

2019 ◽  
Vol 20 (13) ◽  
pp. 3272 ◽  
Author(s):  
Suet Yen Chong ◽  
Choon Keong Lee ◽  
Chenyuan Huang ◽  
Yi Hsuan Ou ◽  
Christopher J. Charles ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cardiovascular Diseases ◽  
Extracellular Vesicles ◽  
Biological Fluids ◽  
Therapeutic Agents ◽  
Bioactive Molecules ◽  
Intrinsic Activity ◽  
Diagnostic Tools ◽  
Alternative Source ◽  
Technological Advantage

Cardiovascular diseases (CVD) represent the leading cause of morbidity and mortality globally. The emerging role of extracellular vesicles (EVs) in intercellular communication has stimulated renewed interest in exploring the potential application of EVs as tools for diagnosis, prognosis, and therapy in CVD. The ubiquitous nature of EVs in biological fluids presents a technological advantage compared to current diagnostic tools by virtue of their notable stability. EV contents, such as proteins and microRNAs, represent specific signatures of cellular activation or injury. This feature positions EVs as an alternative source of biomarkers. Furthermore, their intrinsic activity and immunomodulatory properties offer EVs unique opportunities to act as therapeutic agents per se or to serve as drug delivery carriers by acting as miniaturized vehicles incorporating bioactive molecules. In this article, we aim to review the recent advances and applications of EV-based biomarkers and therapeutics. In addition, the potential of EVs as a drug delivery and theranostic platform for CVD will also be discussed.

scholarly journals Bee Venom: An Updating Review of Its Bioactive Molecules and Its Health Applications

Nutrients ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 3360
Author(s):  
Maria Carpena ◽  
Bernabe Nuñez-Estevez ◽  
Anton Soria-Lopez ◽  
Jesus Simal-Gandara
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Bee Venom ◽  
Bioactive Molecules ◽  
Antitumor Effects ◽  
Ancient Medicine ◽  
Health Applications ◽  
Proteins And Peptides

Bee venom (BV) is usually associated with pain since, when humans are stung by bees, local inflammation and even an allergic reaction can be produced. BV has been traditionally used in ancient medicine and in acupuncture. It consists of a mixture of substances, principally of proteins and peptides, including enzymes as well as other types of molecules in a very low concentration. Melittin and phospholipase A2 (PLA2) are the most abundant and studied compounds of BV. Literature of the main biological activities exerted by BV shows that most studies focuses on the comprehension and test of anti-inflammatory effects and its mechanisms of action. Other properties such as antioxidant, antimicrobial, neuroprotective or antitumor effects have also been assessed, both in vitro and in vivo. Moreover, human trials are necessary to confirm those clinical applications. However, notwithstanding the therapeutic potential of BV, there are certain problems regarding its safety and the possible appearance of adverse effects. On this perspective, new approaches have been developed to avoid these complications. This manuscript is aimed at reviewing the actual knowledge on BV components and its associated biological activities as well as the latest advances on this subject.

scholarly journals The Arsenal of Bioactive Molecules in the Skin Secretion of Urodele Amphibians

2022 ◽  
Vol 12 ◽  
Author(s):  
Ana L. A. N. Barros ◽  
Abdelaaty Hamed ◽  
Mariela Marani ◽  
Daniel C. Moreira ◽  
Peter Eaton ◽  
...  
Keyword(s):  
Biological Activities ◽  
Therapeutic Agents ◽  
New Drugs ◽  
Bioactive Molecules ◽  
High Demand ◽  
Bioactive Properties ◽  
Skin Secretions ◽  
Immune System Modulation ◽  
New Compounds ◽  
Dermal Wound

Urodele amphibians (∼768 spp.), salamanders and newts, are a rich source of molecules with bioactive properties, especially those isolated from their skin secretions. These include pharmacological attributes, such as antimicrobial, antioxidant, vasoactive, immune system modulation, and dermal wound healing activities. Considering the high demand for new compounds to guide the discovery of new drugs to treat conventional and novel diseases, this review summarizes the characteristics of molecules identified in the skin of urodele amphibians. We describe urodele-derived peptides and alkaloids, with emphasis on their biological activities, which can be considered new scaffolds for the pharmaceutical industry. Although much more attention has been given to anurans, bioactive molecules produced by urodeles have the potential to be used for biotechnological purposes and stand as viable alternatives for the development of therapeutic agents.

A comprehensive review on pyranoindole-containing agents

2021 ◽  
Vol 28 ◽  
Author(s):  
Alessia Catalano ◽  
Domenico Iacopetta ◽  
Jessica Ceramella ◽  
Carmela Saturnino ◽  
Maria Stefania Sinicropi
Keyword(s):  
Natural Products ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Biologically Active ◽  
Bioactive Molecules ◽  
Structural Motif ◽  
Huge Number ◽  
Naturally Occurring ◽  
Active Natural

: A huge number of nitrogen-containing heterocyclic compounds are ubiquitous in natural products, pharmaceuticals, and bioactive molecules. Among these, the pyranoindole represents an important structural motif, as it constitutes the central subunit in both the biologically active natural products and therapeutic agents. Talathermophilins, notoamides, norgeamides, carneamides, and versicamides are examples of naturally occurring pyranoindoles, while the well-known etodolac and pemedolac are a tetrahydropyrano[3,4-b]indole deriving from synthetic procedures. Besides the well-known antiinflammatory and fibrinolytic activity, molecules comprising the pyranoindole framework have been demonstrated to exhibit various biological activities, such as antiulcer, antidepressant, analgesic, and antiproliferative. Herein, we report the most common natural and synthetic products bearing a pyranoindole nucleus, their syntheses, and biological activities.

Monocyclic Peptides: Types, Synthesis and Applications

2020 ◽  
Vol 22 (1) ◽  
pp. 123-135 ◽  
Author(s):  
Yalda Khazaei-poul ◽  
Shohreh Farhadi ◽  
Sepideh Ghani ◽  
Safar Ali Ahmadizad ◽  
Javad Ranjbari
Keyword(s):  
Drug Delivery ◽  
Cyclic Peptides ◽  
Rational Design ◽  
Bioactive Molecules ◽  
Synthesis Methods ◽  
Targeted Therapeutics ◽  
Diagnostic Agents ◽  
Linear Types ◽  
Microbial Agents ◽  
Structural Classes

: Peptides are considered to be appropriate tools in various biological fields. They can be primarily used for the rational design of bioactive molecules. They can act as ligands in the development of targeted therapeutics as well as diagnostics, can be used in the design of vaccines or can be employed in agriculture. Peptides can be classified in two broad structural classes: linear and cyclic peptides. Monocyclic peptides are a class of polypeptides with one macrocyclic ring that bears advantages, such as more selective binding and uptake by the target receptor, as well as higher potency and stability compared to linear types. This paper provides an overview of the categories, synthesis methods and various applications of cyclic peptides. The various applications of cyclic peptides include their use as pro-apoptotic and anti-microbial agents, their application as targeting ligands in drug delivery and diagnostic agents, as well as agricultural and therapeutics applications that are elaborated and discussed in this paper.

Majra Honey Abrogated the Normal and Cancer Cells Proliferation Inhibition by Juniperus procera Extract and Extract/Honey Generated AgNPs

2020 ◽  
Vol 20 (8) ◽  
pp. 970-981
Author(s):  
Hamed A. Ghramh ◽  
Essam H. Ibrahim ◽  
Mona Kilnay
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Biological Activities ◽  
Sugar Content ◽  
Polyacrylamide Gel Electrophoresis ◽  
Sodium Dodecyl ◽  
Bioactive Molecules ◽  
Sds Page ◽  
Splenic Cells ◽  
Juniperus Procera

Background: Juniperus procera and Majra honey are well-known as a folk medicine in many countries. Objectives: This work aimed to study the immunomodulatory effects after mixing Majra honey, J. procera water leaves extract and silver Nanoparticles (AgNPs) on immune or cancer cells. Methods: Juniperus procera water leaves extract and 20% Majra honey were prepared. Both the extract and honey were used separately to synthesize AgNPs. AgNPs were characterized using UV/Vis spectrophotometry and electron microscopy. Bioactive molecules in honey and the extract were explored using Fourier Transform Infrared (FT-IR) spectroscopy. Protein profile of honey was explored using Sodium Dodecyl Sulfate- Polyacrylamide Gel Electrophoresis (SDS-PAGE) and honey sugar content was determined using High- Performance Liquid Chromatography (HPLC). Biological activities of honey and the extract were tested. Results: The results demonstrated the ability of the extract/honey to produce AgNPs in a spherical shape. The extract/honey contained many functional groups. SDS-PAGE of Majra honey showed many protein bands. HPLC revealed honey is of good quality and no external additives are added to it. The extract and extract+ AgNPs inhibited the growth of normal rat splenic cells while honey stimulated it. The extract+honey turned stimulatory to the splenic cells’ growth and significantly diminished the inhibitory potential of the extract containing AgNPs. Both the extract and honey have antimicrobial activities, this potential increased in the presence of AgNPs. Honey and Honey+AgNPs inhibited HepG2 cancer cell proliferation while Hela cell growth inhibited only with honey+AgNPs. Conclusion: Both honey and the extract have antibacterial and immunomodulatory potentials as well as the power to produce AgNPs. Majra honey alone showed anticancer activity against HepGe2 cells, but not against Hela cells, and when contained AgNPs had anticancer activity on both cell lines. Mixing of Majra honey with J. procera extract showed characterized immunomodulatory potentials that can be described as immunostimulant.

Natural Compounds and Drug Discovery: Can Cnidarian Venom Play a Role?

2019 ◽  
Vol 19 (2) ◽  
pp. 114-118
Author(s):  
Gian Luigi Mariottini ◽  
Irwin Darren Grice
Keyword(s):  
Biological Activity ◽  
Marine Species ◽  
Natural Compounds ◽  
Therapeutic Agents ◽  
Industrial Applications ◽  
Bioactive Molecules ◽  
Sea Anemones ◽  
Therapeutic Approaches ◽  
Ongoing Research ◽  
Biological Compounds

Natural compounds extracted from organisms and microorganisms are an important resource for the development of drugs and bioactive molecules. Many such compounds have made valuable contributions in diverse fields such as human health, pharmaceutics and industrial applications. Presently, however, research on investigating natural compounds from marine organisms is scarce. This is somewhat surprising considering that the marine environment makes a major contribution to Earth's ecosystems and consequently possesses a vast storehouse of diverse marine species. Interestingly, of the marine bioactive natural compounds identified to date, many are venoms, coming from Cnidarians (jellyfish, sea anemones, corals). Cnidarians are therefore particularly interesting marine species, producing important biological compounds that warrant further investigation for their development as possible therapeutic agents. From an experimental aspect, this review aims to emphasize and update the current scientific knowledge reported on selected biological activity (antiinflammatory, antimicrobial, antitumoral, anticoagulant, along with several less studied effects) of Cnidarian venoms/extracts, highlighting potential aspects for ongoing research towards their utilization in human therapeutic approaches.

scholarly journals Difluorocarbene enables to access 2-fluoroindoles from ortho-vinylanilines

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Jianke Su ◽  
Xinyuan Hu ◽  
Hua Huang ◽  
Yu Guo ◽  
Qiuling Song
Keyword(s):  
Fluorine Atom ◽  
High Efficiency ◽  
Addition Reaction ◽  
Bond Cleavage ◽  
Therapeutic Agents ◽  
Bioactive Molecules ◽  
General Strategy ◽  
Michael Addition Reaction ◽  
Fundamental Properties ◽  
Synthetic Approaches

Abstract2-Fluoroindoles as an important structural scaffold are widely existing in many bioactive or therapeutic agents. Despite their potential usefulness, efficient constructions of 2-fluoroindole derivatives are very sparce. The development of straightforward synthetic approaches to access 2-fluoroindoles is highly desirable for studying their fundamental properties and applications. Herein, we report an efficient and general strategy for the construction of 2-fluoroindoles in which a wide variety of 2-fluoroindoles were accessed with high efficiency and chemoselectivity. Instead of starting from indole skeletons, our strategy constructs indole scaffolds alongside the incorporation of fluorine atom on C2 position in a formal [4+1] cyclization from readily accessible ortho-vinylanilines and difluorocarbene. In our protocol, commercially accessible halodifluoroalkylative reagents provide one carbon and one fluorine atom by cleaving one C-N tertiary bond and forming one C-N bond and one C-C double bond with ortho-vinylanilines. Downstream transformations on 2-fluoroindoles lead to various valuable bioactive molecules which demonstrated significant synthetic advantages over previous reports. And mechanistic studies suggest that the reaction undergoes a cascade difluorocarbene-trapping and intramolecular Michael addition reaction followed by Csp3-F bond cleavage.

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.

Multivesicular liposome: A lipid-based drug delivery system for efficient drug delivery

2021 ◽  
Vol 27 ◽  
Author(s):  
Bapi Gorain ◽  
Bandar E. Al-Dhubiab ◽  
Anroop Nair ◽  
Prashant Kesharwani ◽  
Manisha Pandey ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Delivery System ◽  
Targeted Delivery ◽  
Drug Loading ◽  
Therapeutic Agents ◽  
Laboratory Research ◽  
Efficacy And Safety ◽  
Liposomal Delivery ◽  
Proteins And Peptides

: The advancement of delivery tools for therapeutic agents has brought several novel formulations with increased drug loading, sustained release, targeted delivery, and prolonged efficacy. Amongst the several novel delivery approaches, multivesicular liposome has gained potential interest because this delivery system possesses the above advantages. In addition, this multivesicular liposomal delivery prevents degradation of the entrapped drug within the physiological environment while administered. The special structure of the vesicles allowed successful entrapment of hydrophobic and hydrophilic therapeutic agents, including proteins and peptides. Furthermore, this novel formulation could maintain the desired drug concentration in the plasma for a prolonged period, which helps to reduce the dosing frequencies, improve bioavailability, and safety. This tool could also provide stability of the formulation, and finally gaining patient compliance. Several multivesicular liposomes received approval for clinical research, while others are at different stages of laboratory research. In this review, we have focused on the preparation of multivesicular liposomes along with their application in different ailments for the improvement of the performance of the entrapped drug. Moreover, the challenges of delivering multivesicular vesicles have also been emphasized. Overall, it could be inferred that multivesicular liposomal delivery is a novel platform of advanced drug delivery with improved efficacy and safety.

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