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Natural Toxins/Molecules (and Derivatives) from Animal Venoms: from Basic Research to Therapeutic Applications 2019

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (30 September 2019) | Viewed by 40055

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Guest Editor
Institute of Neurophysiopathology (INP), Aix-Marseille University, Faculté des sciences médicales et paramédicales, 27, Bd Jean Moulin, 13005 Marseille, France
Interests: antimicrobial peptides; antibacterial; antibiotics; structure-activity relationships; bacteriocins; drug design; peptide engineering
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Special Issue Information

Dear Colleagues,

Venomous animals (e.g., scorpions, snakes, sea anemones, cone snails, worms, wasps and frogs) are invaluable natural sources of biologically-active compounds that target a variety of receptors/molecules (ion channels, enzymes, etc.). These compounds are generally highly potent, but can display variable selectivities. Interestingly, a number of molecules from venoms reportedly possess some therapeutic potential to treat pain, microbial infections, and more or less severe pathologies such as cancer, autoimmune and neurological diseases. This special issue of Molecules is devoted to the many aspects of marine and non-marine toxins/molecules (and derivatives thereof) from animal venoms, including their pharmacological properties, structural characteristics, structure-function relationship, molecular engineering/drug design, and therapeutic value. All scientists and clinicians working in these emerging and promising fields of research are strongly encouraged to submit their original works for publication in this Special Issue. 

Dr. Jean-Marc Sabatier
Guest Editor

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Keywords

  • venom
  • animal toxin
  • venomous animal
  • toxin engineering
  • drug design
  • structure-activity
  • chemotherapeutic drug
  • therapy
  • ion channel
  • antimicrobial
  • analgesic
  • antitumor/anticancer
  • autoimmune disease
  • neurological disorder

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Published Papers (4 papers)

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Research

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21 pages, 4458 KiB  
Article
Chemical Profile and Multicomponent Quantitative Analysis for the Quality Evaluation of Toad Venom from Different Origins
by Yueting Cao, Jiheng Wu, Hongye Pan and Longhu Wang
Molecules 2019, 24(19), 3595; https://doi.org/10.3390/molecules24193595 - 6 Oct 2019
Cited by 28 | Viewed by 4458
Abstract
Toad venom (Chansu), a traditional Chinese medicine (TCM), has been widely used for treating various cancer. However, it is considerably difficult to evaluate the quality of Chansu due to its complex chemical compositions. Hence, finding the characteristic ingredients and developing a scientific and [...] Read more.
Toad venom (Chansu), a traditional Chinese medicine (TCM), has been widely used for treating various cancer. However, it is considerably difficult to evaluate the quality of Chansu due to its complex chemical compositions. Hence, finding the characteristic ingredients and developing a scientific and comprehensive quality evaluation method are essential for guaranteeing the safety and efficacy of Chansu. In this paper, the chemical composition database of Chansu was successfully established and HPLC-ESI-Q-TOF-MS/MS was applied for chemical profiling of the ingredients in Chansu. In total, 157 compounds were identified, including 22 amino acids, 8 alkaloids, 54 bufogenins, 63 bufotoxins, and 10 other compounds. Furthermore, HPLC fingerprints and quantitative analysis of its multicomponent were successfully developed to evaluate the quality consistency of Chansu from different origins. The results suggested that the HPLC fingerprint of Chansu could be divided into an amino acid and alkaloid region, as well as a bufogenins and bufotoxins region. The fingerprint profile of Chansu from different geographical origins were different, indicating that its quality was affected by the geographical factors. In addition, seven characteristic peaks were selected as the quantitative markers to evaluate the quality of the Chansu. The Kruskal–Wallis test illustrated that the contents of seven bufogenins in Chansu were significantly (p < 0.01) different among different origins. The total contents of the seven compounds ranged from 100.40 to 169.22 mg/g in 20 batches of Chansu samples. This study demonstrated that integrating HPLC-ESI-Q-TOF-MS/MS, HPLC fingerprints, and multicomponent quantitative analysis coupled with chemometrics was a comprehensive and reliable strategy for evaluation of Chansu in both qualitative and quantitative aspects. In addition, our study represented the most comprehensive characterization on the chemical compositions of Chansu, which could provide important reference information for the discovery of potential bioactive compounds. Full article
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Review

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13 pages, 1126 KiB  
Review
Bee Venom: Overview of Main Compounds and Bioactivities for Therapeutic Interests
by Rim Wehbe, Jacinthe Frangieh, Mohamad Rima, Dany El Obeid, Jean-Marc Sabatier and Ziad Fajloun
Molecules 2019, 24(16), 2997; https://doi.org/10.3390/molecules24162997 - 19 Aug 2019
Cited by 213 | Viewed by 23426
Abstract
Apitherapy is an alternate therapy that relies on the usage of honeybee products, most importantly bee venom for the treatment of many human diseases. The venom can be introduced into the human body by manual injection or by direct bee stings. Bee venom [...] Read more.
Apitherapy is an alternate therapy that relies on the usage of honeybee products, most importantly bee venom for the treatment of many human diseases. The venom can be introduced into the human body by manual injection or by direct bee stings. Bee venom contains several active molecules such as peptides and enzymes that have advantageous potential in treating inflammation and central nervous system diseases, such as Parkinson’s disease, Alzheimer’s disease, and amyotrophic lateral sclerosis. Moreover, bee venom has shown promising benefits against different types of cancer as well as anti-viral activity, even against the challenging human immunodeficiency virus (HIV). Many studies described biological activities of bee venom components and launched preclinical trials to improve the potential use of apitoxin and its constituents as the next generation of drugs. The aim of this review is to summarize the main compounds of bee venom, their primary biological properties, mechanisms of action, and their therapeutic values in alternative therapy strategies. Full article
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16 pages, 609 KiB  
Review
Hypotensive Snake Venom Components—A Mini-Review
by Orsolya Péterfi, Francisc Boda, Zoltán Szabó, Elek Ferencz and László Bába
Molecules 2019, 24(15), 2778; https://doi.org/10.3390/molecules24152778 - 31 Jul 2019
Cited by 51 | Viewed by 7422
Abstract
Hypertension is considered a major public health issue due to its high prevalence and subsequent risk of cardiovascular and kidney diseases. Thus, the search for new antihypertensive compounds remains of great interest. Snake venoms provide an abundant source of lead molecules that affect [...] Read more.
Hypertension is considered a major public health issue due to its high prevalence and subsequent risk of cardiovascular and kidney diseases. Thus, the search for new antihypertensive compounds remains of great interest. Snake venoms provide an abundant source of lead molecules that affect the cardiovascular system, which makes them prominent from a pharmaceutical perspective. Such snake venom components include bradykinin potentiating peptides (proline-rich oligopeptides), natriuretic peptides, phospholipases A2, serine-proteases and vascular endothelial growth factors. Some heparin binding hypotensive factors, three-finger toxins and 5′ nucleotidases can also exert blood pressure lowering activity. Great advances have been made during the last decade regarding the understanding of the mechanism of action of these hypotensive proteins. Bradykinin potentiating peptides exert their action primarily by inhibiting the angiotensin-converting enzyme and increasing the effect of endogenous bradykinin. Snake venom phospholipases A2 are capable of reducing blood pressure through the production of arachidonic acid, a precursor of cyclooxygenase metabolites (prostaglandins or prostacyclin). Other snake venom proteins mimic the effects of endogenous kallikrein, natriuretic peptides or vascular endothelial growth factors. The aim of this work was to review the current state of knowledge regarding snake venom components with potential antihypertensive activity and their mechanisms of action. Full article
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16 pages, 3135 KiB  
Review
Diverse Structural Features of Potassium Channels Characterized by Scorpion Toxins as Molecular Probes
by Yonghui Zhao, Zongyun Chen, Zhijian Cao, Wenxin Li and Yingliang Wu
Molecules 2019, 24(11), 2045; https://doi.org/10.3390/molecules24112045 - 29 May 2019
Cited by 19 | Viewed by 3920
Abstract
Scorpion toxins are well-known as the largest potassium channel peptide blocker family. They have been successfully proven to be valuable molecular probes for structural research on diverse potassium channels. The potassium channel pore region, including the turret and filter regions, is the binding [...] Read more.
Scorpion toxins are well-known as the largest potassium channel peptide blocker family. They have been successfully proven to be valuable molecular probes for structural research on diverse potassium channels. The potassium channel pore region, including the turret and filter regions, is the binding interface for scorpion toxins, and structural features from different potassium channels have been identified using different scorpion toxins. According to the spatial orientation of channel turrets with differential sequence lengths and identities, conformational changes and molecular surface properties, the potassium channel turrets can be divided into the following three states: open state with less hindering effects on toxin binding, half-open state or half-closed state with certain effects on toxin binding, and closed state with remarkable effects on toxin binding. In this review, we summarized the diverse structural features of potassium channels explored using scorpion toxin tools and discuss future work in the field of scorpion toxin-potassium channel interactions. Full article
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