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Toxins
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Animals Venom in Drug Discovery: A Valuable Therapeutic Tool
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Animals Venom in Drug Discovery: A Valuable Therapeutic Tool

A special issue of Toxins (ISSN 2072-6651). This special issue belongs to the section "Animal Venoms".

Deadline for manuscript submissions: 31 August 2025 | Viewed by 6981

Special Issue Editors

Dr. Mohamad Rima

E-Mail Website
Guest Editor
Department of Natural Sciences, Lebanese American University, Byblos P.O. Box 36, Lebanon
Interests: snake venom; senescence; aging; bioactive molecules; calcium channels
Prof. Dr. Ziad Fajloun

E-Mail Website
Guest Editor
1. Laboratory of Applied Biotechnology (LBA3B), Azm Center for Research in Biotechnology and Its Applications, EDST, Lebanese University, Tripoli 1300, Lebanon
2. Department of Biology, Faculty of Sciences 3, Campus Michel Slayman Ras Maska, Lebanese University, Tripoli 1352, Lebanon
Interests: toxins; venoms; pharmacology; scorpion venoms; biological therapy; biomolecular interactions
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Animal venoms are a rich source of valuable pharmaceutical molecules. These complex mixtures of proteins and other bioactive molecules are mainly used for predation and defense. However, venom compounds exhibit many interesting biological activities including anti-oxidant, anti-coagulant, anti-inflammatory, and anti-cancer properties, thus offering unique bioactive molecules with high specificity and potency that make them interesting candidates for drug development. Technological advancements, such as high-throughput screening, genomics, and proteomics, support the discovery and development of new drugs from venoms. The broad sources of venoms (snake, spider, bee, scorpions, etc.) combined with the large panel of biological activities associated with diseases position animal venoms as a major resource for biological research. This being said, a vast majority of venomous animals and their therapeutic potential have not yet been explored.

In this Special Issue, we aim to provide scholars with the latest research on animal venom-based drug discovery, covering everything from the early phases of venom collection to advanced clinical trials, including fractionation, bioactivity, and characterization. To enhance our understanding of these processes, we invite experts in the field of animal venoms to contribute via research papers and reviews dissecting the molecular complexity of animal venoms in drug discovery. All aspects of animal venom-based drug discovery, including cellular, molecular, structural, and -omics studies, are of great interest.

Dr. Mohamad Rima
Prof. Dr. Ziad Fajloun
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a double-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Toxins is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • venoms
  • toxins
  • calcium channels
  • proteomics
  • transcriptomics
  • bioactive molecules
  • bioinformatics
  • venomous animals

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Published Papers (8 papers)

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Research

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15 pages, 6359 KiB  
Article
An Elastase Inhibitor ShSPI from Centipede Attenuates Bleomycin-Induced Pulmonary Fibrosis
by Xi Lian, Bin Liu, Dan Li, Xinyao Wang, Chengbo Long, Xing Feng, Qiong Liao and Mingqiang Rong
Toxins 2025, 17(5), 213; https://doi.org/10.3390/toxins17050213 - 24 Apr 2025
Viewed by 82
Abstract
Idiopathic pulmonary fibrosis (IPF) is a chronic lung disease characterized by the fibrotic thickening of the alveolar walls, resulting in compromised gas exchange, restricted ventilation, and respiratory failure. It has been indicated that elastase inhibitors reduced the severity of IPF by neutralizing excessive [...] Read more.
Idiopathic pulmonary fibrosis (IPF) is a chronic lung disease characterized by the fibrotic thickening of the alveolar walls, resulting in compromised gas exchange, restricted ventilation, and respiratory failure. It has been indicated that elastase inhibitors reduced the severity of IPF by neutralizing excessive elastase levels in the lungs. ShSPI is an elastase inhibitor derived from centipede toxin. The present study evaluates the therapeutic effects of ShSPI in a bleomycin-induced idiopathic pulmonary fibrosis model. According to the results, ShSPI markedly reduced the weight loss, showing the improvement of health status in bleomycin-induced mice. Its robust antifibrotic effects were evidenced by the mitigation of alveolar structural damage, reduction in inflammatory cell infiltration, inhibition of collagen deposition, and suppression of fibrotic nodule formation. ShSPI effectively attenuated inflammatory responses by downregulating pro-inflammatory factors (IL-6, IL-1β, and MCP-1) and upregulating the anti-inflammatory factor interleukin-10 (IL-10). After delivered via inhalation, ShSPI exhibited favorable pharmacokinetic properties. It could be detected at 8 h at doses of 1 mg/kg and achieved maximum plasma concentrations (Cmax) of 188.00 ± 64.40 ng/mL in vivo. At high doses (160 mg/kg), ShSPI maintained a strong safety profile, with no detectable toxicity observed. This feature shows the therapeutic potential of ShSPI in the treatment of idiopathic pulmonary fibrosis and provides valuable evidence for its development as a novel peptide-based therapy. Full article
(This article belongs to the Special Issue Animals Venom in Drug Discovery: A Valuable Therapeutic Tool)
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25 pages, 4262 KiB  
Article
Selective Modulation of Osteoclast Function by Bothrops moojeni Venom and Its Fractions: Implications for Therapeutic Targeting in Bone Diseases
by Fernanda D’Amélio, Hugo Vigerelli, Isabel de Fátima Correia Batista, Rodrigo Pinheiro Araldi, Álvaro R. B. Prieto-da-Silva, Daniel Carvalho Pimenta and Irina Kerkis
Toxins 2025, 17(3), 141; https://doi.org/10.3390/toxins17030141 - 15 Mar 2025
Viewed by 483
Abstract
Our study explores the differential effects of Bothrops moojeni venom and its fractions on osteoclast (OC) morphology, function, and osteoclastogenesis. The crude venom and its high-molecular-weight (HMW) fraction disrupt critical OC processes, including F-actin ring formation and mitochondrial distribution, thereby impairing bone resorption. [...] Read more.
Our study explores the differential effects of Bothrops moojeni venom and its fractions on osteoclast (OC) morphology, function, and osteoclastogenesis. The crude venom and its high-molecular-weight (HMW) fraction disrupt critical OC processes, including F-actin ring formation and mitochondrial distribution, thereby impairing bone resorption. These components primarily target cytoskeletal integrity and transcription regulation, with the OBSCN gene playing a direct role in OC function. In contrast, the low-molecular-weight (LMW) fraction selectively modulates OCs without significant cytoskeletal alterations. It influences vital cellular signaling pathways, notably through FNIP1 and FNIP2, essential for OC differentiation and function. This suggests a more targeted therapeutic approach with potentially fewer off-target effects. The venom also alters cytokine production, increasing IL-6 and IL-10 levels. Elevated IL-6 levels promote osteoclastogenesis and bone resorption, while IL-10 appears to counterbalance these effects through a regulatory feedback mechanism. Secretome analysis reveals that the crude venom and HMW fraction disrupt proteins involved in membrane trafficking and structural integrity. In contrast, the LMW fraction influences matrix remodeling, energy metabolism, and gene regulation. Gene interaction analysis LMW fraction post-treatment identifies FNIP1 and FNIP2 as critical targets involved in osteoclastogenesis. The observed changes in gene expression, including those related to immune response, energy metabolism, and chromatin remodeling, provide insights into the venom’s impact on bone health. Overall, the LMW fraction shows promise for drug development due to its selective implications and potential for fewer side effects, offering a more precise approach to treating bone diseases. Full article
(This article belongs to the Special Issue Animals Venom in Drug Discovery: A Valuable Therapeutic Tool)
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Graphical abstract

22 pages, 3779 KiB  
Article
Insights into the Role of Proteolytic and Adhesive Domains of Snake Venom Metalloproteinases from Bothrops spp. in the Control of Toxoplasma gondii Infection
by Samuel C. Teixeira, Thales A. M. Fernandes, Guilherme de Souza, Luana C. Luz, Marina Paschoalino, Joed P. de L. Junior, Alessandra M. Rosini, Aryani F. F. Martínez, Vitor de Freitas, Daiana S. Lopes, Patrícia B. Clissa, Vinícius C. de Souza, Milton Y. Nishiyama-Jr., Bellisa F. Barbosa, Eloisa A. V. Ferro and Veridiana de M. R. Ávila
Toxins 2025, 17(2), 95; https://doi.org/10.3390/toxins17020095 - 18 Feb 2025
Viewed by 861
Abstract
Toxoplasmosis is an alarming public health problem that affects more than one-third of the world’s population. In our work, we investigated the antiparasitic effects of catalytically active [BpMP-I and Jararhagin (Jar)] and catalytically inactive [Jararhagin-C (Jar-C)] snake venom metalloproteinases (SVMPs) in human HeLa [...] Read more.
Toxoplasmosis is an alarming public health problem that affects more than one-third of the world’s population. In our work, we investigated the antiparasitic effects of catalytically active [BpMP-I and Jararhagin (Jar)] and catalytically inactive [Jararhagin-C (Jar-C)] snake venom metalloproteinases (SVMPs) in human HeLa cells. These toxins impaired the parasite invasion and intracellular growth, and modulated IL-6, IL-8, and MIF cytokines that control the cell susceptibility and response against T. gondii. Furthermore, we verified that the antiprotozoal activities are not restricted to the presence of the proteolytic domain, and the adhesive domains participate in the control of T. gondii infection. Also, by analyzing the structures of Jar and Jar-C through molecular modeling and dynamics, we observed that the adhesive domains in Jar-C are more exposed due to the absence of the proteolytic domain, which could favor the interaction with different targets. Our investigation on the role of SVMP domains in combating T. gondii infection highlights their potential application as biotechnological tools for creating more effective treatments for toxoplasmosis. Full article
(This article belongs to the Special Issue Animals Venom in Drug Discovery: A Valuable Therapeutic Tool)
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13 pages, 9161 KiB  
Article
Improvement in XIa Selectivity of Snake Venom Peptide Analogue BF9-N17K Using P2′ Amino Acid Replacements
by Li Ding, Zhiping Zhai, Tianxiang Qin, Yuexi Lin, Zhicheng Shuang, Fang Sun, Chenhu Qin, Hongyi Luo, Wen Zhu, Xiangdong Ye, Zongyun Chen and Xudong Luo
Toxins 2025, 17(1), 23; https://doi.org/10.3390/toxins17010023 - 5 Jan 2025
Viewed by 809
Abstract
Coagulation factor XIa is a new serine-protease family drug target for next-generation anticoagulants. With the snake venom Kunitz-type peptide BF9 as the scaffold, we obtained a highly active XIa inhibitor BF9-N17K in our previous work, but it also inhibited the hemostatic target plasmin. [...] Read more.
Coagulation factor XIa is a new serine-protease family drug target for next-generation anticoagulants. With the snake venom Kunitz-type peptide BF9 as the scaffold, we obtained a highly active XIa inhibitor BF9-N17K in our previous work, but it also inhibited the hemostatic target plasmin. Here, in order to enhance the selectivity of BF9-N17K toward XIa, four mutants, BF9-N17K-L19A, BF9-N17K-L19S, BF9-N17K-L19D, and BF9-N17K-L19K, were further designed using the P2′ amino acid classification scanning strategy. The anticoagulation assay showed that the four P2′ single-point mutants still had apparent inhibitory anticoagulation activity that selectively inhibited the human intrinsic coagulation pathway and had no influence on the extrinsic coagulation pathway or common coagulation pathway, which indicated that the single-point mutants had minimal effects on the anticoagulation activity of BF9-N17K. Interestingly, the enzyme inhibitor assay experiments showed that the XIa and plasmin inhibitory activities were significantly changed by the P2′ amino acid replacements. The XIa inhibitory activity of BF9-N17K-L19D was apparently enhanced, with an IC50 of 19.28 ± 2.53 nM, and its plasmin inhibitory was significantly weakened, with an IC50 of 459.33 ± 337.40 nM. BF9-N17K-L19K was the opposite to BF9-N17K-L19D, which had enhanced plasmin inhibitory activity and reduced XIa inhibitory activity. For BF9-N17K-L19A and BF9-N17K-L19S, no apparent changes were found in the serine protease inhibitory activity, and they had similar XIa and plasmin inhibitory activities to the template peptide BF9-N17K. These results suggested that the characteristics of the charge of the P2′ site might be associated with the drug selectivity between the anticoagulant target XIa and hemostatic target plasmin. In addition, according to the molecular diversity and sequence conservation, a common motif GR/PCR/KA/SXIP-XYGGC is proposed in the XIa-inhibitory Kunitz-type peptides, which might provide a new clue for further peptide engineering. In conclusion, through P2′ amino acid classification scanning with the snake venom Kunitz-type peptide scaffold, a new potent and selective XIa inhibitor, BF9-N17K-L19D, was discovered, which provides a new XIa-targeting lead drug template for the treatment of thrombotic-related diseases. Full article
(This article belongs to the Special Issue Animals Venom in Drug Discovery: A Valuable Therapeutic Tool)
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10 pages, 2020 KiB  
Article
Influence of Apis mellifera syriaca Bee Venom on Nociception and Inflammatory Cytokine Profiles in Experimental Hyperalgesia
by Mohamad Ayoub, Salma Fayjaloun, Rabih Roufayel, Dany El Obeid, Ziad Fajloun, Mohamad Rima and Marc Karam
Toxins 2025, 17(1), 18; https://doi.org/10.3390/toxins17010018 - 1 Jan 2025
Cited by 1 | Viewed by 1236
Abstract
Hyperalgesia is a condition marked by an abnormal increase in pain sensitivity, often occurring in response to tissue injury, inflammation, or prolonged exposure to certain medications. Inflammatory mediators, such as cytokines IL-1β, IL-6, and TNF-α, play a central role in this process, amplifying [...] Read more.
Hyperalgesia is a condition marked by an abnormal increase in pain sensitivity, often occurring in response to tissue injury, inflammation, or prolonged exposure to certain medications. Inflammatory mediators, such as cytokines IL-1β, IL-6, and TNF-α, play a central role in this process, amplifying pain perception. Developing effective treatments that address the underlying mechanisms of hyperalgesia is an active field of research. Apis mellifera syriaca venom demonstrated potential immunomodulatory activity associated with cytokine release in vivo. Therefore, the aim of this study is to evaluate the effect of Apis mellifera syriaca bee venom (AmsBV) on pain sensitivity in a formalin-induced hyperalgesia mice model and to evaluate the potential role of cytokines associated with the nociception of pain. The hotplate test, used to measure pain latency, showed that hypersensitivity to pain was induced in formalin-injected male mice only, with no changes in females, suggesting a sex-based response to formalin. When applied, AmsBV reduced pain sensitivity in males, suggesting pain relief potential. At the molecular level, AmsBV was able to reduce pro-inflammatory interleukin IL-4 and cytokine IFN-γ, emphasizing its immunomodulatory potential. Interestingly, the venom restored anti-inflammatory IL-10 levels that were significantly decreased in hyperalgesia males. Together, these findings highlight the therapeutic potential for AmsBV in managing inflammation and reducing pain, particularly hyperalgesia. Full article
(This article belongs to the Special Issue Animals Venom in Drug Discovery: A Valuable Therapeutic Tool)
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13 pages, 6199 KiB  
Article
Bicistronic Vector Expression of Recombinant Jararhagin-C and Its Effects on Endothelial Cells
by Karla Fernanda Ferraz, Lhiri Hanna De Lucca Caetano, Daniele Pereira Orefice, Paula Andreia Lucas Calabria, Maisa Splendore Della-Casa, Luciana Aparecida Freitas-de-Sousa, Emidio Beraldo-Neto, Sabri Saeed Sanabani, Geraldo Santana Magalhães and Patricia Bianca Clissa
Toxins 2024, 16(12), 524; https://doi.org/10.3390/toxins16120524 - 3 Dec 2024
Cited by 1 | Viewed by 1012
Abstract
Jararhagin-C (JarC) is a protein from the venom of Bothrops jararaca consisting of disintegrin-like and cysteine-rich domains. JarC shows a modulating effect on angiogenesis and remodeling of extracellular matrix constituents, improving wound healing in a mouse experimental model. JarC is purified from crude [...] Read more.
Jararhagin-C (JarC) is a protein from the venom of Bothrops jararaca consisting of disintegrin-like and cysteine-rich domains. JarC shows a modulating effect on angiogenesis and remodeling of extracellular matrix constituents, improving wound healing in a mouse experimental model. JarC is purified from crude venom, and the yield is less than 1%. The aim of this work was to obtain the recombinant form of JarC and to test its biological activity. For this purpose, the bicistronic vector pSUMOUlp1 was used. This vector allowed the expression of the recombinant toxin JarC (rJarC) in fusion with the small ubiquitin-related modifier (SUMO) as well as the SUMO protease Ulp1. After expression, this protease was able to efficiently remove SUMO from rJarC inside the bacteria. rJarC free from SUMO was purified at the expected molecular mass and recognized by polyclonal anti-jararhagin antibodies. In terms of biological activity, both the native and recombinant forms showed no toxicity to the HUVEC cell line CRL1730 and were effective in modulating cell migration activity in the experimental in vitro model. These results demonstrate the successful production of rJarC and the preservation of its biological activity, which may facilitate further investigations into the therapeutic potential of this snake venom-derived protein. Full article
(This article belongs to the Special Issue Animals Venom in Drug Discovery: A Valuable Therapeutic Tool)
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Review

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26 pages, 1953 KiB  
Review
Short Peptides from Asian Scorpions: Bioactive Molecules with Promising Therapeutic Potential
by Kaiyun Xin, Ruize Sun, Wanyang Xiao, Weijie Lu, Chenhui Sun, Jietao Lou, Yanyan Xu, Tianbao Chen, Di Wu and Yitian Gao
Toxins 2025, 17(3), 114; https://doi.org/10.3390/toxins17030114 - 28 Feb 2025
Viewed by 1123
Abstract
Scorpion venom peptides, particularly those derived from Asian species, have garnered significant attention, offering therapeutic potential in pain management, cancer, anticoagulation, and infectious diseases. This review provides a comprehensive analysis of scorpion venom peptides, focusing on their roles as voltage-gated sodium (Nav), potassium [...] Read more.
Scorpion venom peptides, particularly those derived from Asian species, have garnered significant attention, offering therapeutic potential in pain management, cancer, anticoagulation, and infectious diseases. This review provides a comprehensive analysis of scorpion venom peptides, focusing on their roles as voltage-gated sodium (Nav), potassium (Kv), and calcium (Cav) channel modulators. It analyzed Nav1.7 inhibition for analgesia, Kv1.3 blockade for anticancer activity, and membrane disruption for antimicrobial effects. While the low targeting specificity and high toxicity of some scorpion venom peptides pose challenges to their clinical application, recent research has made strides in overcoming these limitations. This review summarizes the latest progress in scorpion venom peptide research, discussing their mechanisms of action, therapeutic potential, and challenges in clinical translation. This work aims to provide new insights and directions for the development of novel therapeutic drugs. Full article
(This article belongs to the Special Issue Animals Venom in Drug Discovery: A Valuable Therapeutic Tool)
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Other

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31 pages, 2052 KiB  
Systematic Review
Innovations in Snake Venom-Derived Therapeutics: A Systematic Review of Global Patents and Their Pharmacological Applications
by Diana Carolina Zona Rubio, Diana Marcela Aragón and Izabel Almeida Alves
Toxins 2025, 17(3), 136; https://doi.org/10.3390/toxins17030136 - 14 Mar 2025
Viewed by 1145
Abstract
Active compounds from natural sources, particularly snake venoms, are crucial for pharmaceutical development despite challenges in drug discovery. Snake venoms, historically used for medicinal purposes, contain bioactive peptides and enzymes that show therapeutic potential for conditions such as arthritis, asthma, cancer, chronic pain, [...] Read more.
Active compounds from natural sources, particularly snake venoms, are crucial for pharmaceutical development despite challenges in drug discovery. Snake venoms, historically used for medicinal purposes, contain bioactive peptides and enzymes that show therapeutic potential for conditions such as arthritis, asthma, cancer, chronic pain, infections and cardiovascular diseases. The objective of this study was to examine pharmacological and biomedical innovations by identifying the key research trends, the most studied snake species, and their therapeutic applications. A systematic review of patents related to snake venoms was conducted using the European Patent Office database, Espacenet, covering 2014 to mid-2024. The search employed the keyword “venom,” applying IPC classification A61K38/00, resulting in 31 patents after screening. A PubMed survey on “snake venom derivatives innovations” was conducted to compare the scientific literature volume with the identified patents. This review highlights the therapeutic potential of snake venom-derived products for coagulation disorders, cancer, inflammation, and pain management. Despite challenges in pharmacokinetics and venom variability, advancements in biotechnology offer promise for personalized therapies. The future of snake venom-based treatments appears promising for addressing complex medical conditions. Full article
(This article belongs to the Special Issue Animals Venom in Drug Discovery: A Valuable Therapeutic Tool)
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