Venom peptides – A comprehensive translational perspective in pain management

Vidya,; Achar, Raghu Ram; M.U, Himathi; Akshita, N; T, Yogish Somayaji; Vivek, H. K.; Byrappa, K.; Ramadas, Dinesha

doi:10.1016/j.crtox.2021.09.001

Cited by 18 publications

(11 citation statements)

References 118 publications

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“…These peptides block a set of acid-sensing ion channels to relieve pain. Naja atra [111] It has been reported that crotalphine a 14-amino acids peptide with a pyroglutamic acid and a disulfide bond (Table 8), isolated from the venom of the South American rattlesnake Crotalus durissus terrificus, produces an antinociception by displaying opioid activity [110]. It is worth noting that the antinociceptive effect of crotalphine is blocked by the KOR antagonist norbinaltorphimine and partially reversed by N,N-diallyl-Tyr-Aib-Phe-Leu-OH, DOR antagonist, whereas in a PGE2-induced hyperalgesia model the activity is reversed by intraplantar injection of dynorphin A antiserum, indicating the involvement of endogenous opioids [112,113].…”

Section: Peptides From Snake Venommentioning

confidence: 99%

“…The µ-EPTX-Na1a is a 62-residue polypeptide (Table 8) from the venom of the Chinese cobra (Naja atra). It was shown to be a potent inhibitor of the voltage-gated sodium channel Na v 1.8 subtypes and hence contributes to reducing inflammatory and neuropathic pain [111]. In vivo, in rodent inflammatory and neuropathic pain models, µ-EPTX-Na1a attenuates nociceptive behavior more strongly than morphine.…”

Section: Peptides From Snake Venommentioning

confidence: 99%

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Analgesic Peptides: From Natural Diversity to Rational Design

Gach-Janczak,

Biernat,

Kuczer

et al. 2024

Molecules

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Pain affects one-third of the global population and is a significant public health issue. The use of opioid drugs, which are the strongest painkillers, is associated with several side effects, such as tolerance, addiction, overdose, and even death. An increasing demand for novel, safer analgesic agents is a driving force for exploring natural sources of bioactive peptides with antinociceptive activity. Since the G protein-coupled receptors (GPCRs) play a crucial role in pain modulation, the discovery of new peptide ligands for GPCRs is a significant challenge for novel drug development. The aim of this review is to present peptides of human and animal origin with antinociceptive potential and to show the possibilities of their modification, as well as the design of novel structures. The study presents the current knowledge on structure-activity relationship in the design of peptide-based biomimetic compounds, the modification strategies directed at increasing the antinociceptive activity, and improvement of metabolic stability and pharmacodynamic profile. The procedures employed in prolonged drug delivery of emerging compounds are also discussed. The work summarizes the conditions leading to the development of potential morphine replacements.

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Section: Peptides From Snake Venommentioning

confidence: 99%

Section: Peptides From Snake Venommentioning

confidence: 99%

Analgesic Peptides: From Natural Diversity to Rational Design

Gach-Janczak,

Biernat,

Kuczer

et al. 2024

Molecules

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“…0.05 mg/kg (n = 5) AUC0-t (µg•min/mL) 1 11.8 ± 0.869 AUC0-inf (µg•min/mL) 2 11.8 ± 0.866 t1/2 (min) 3 8.10 ± 0.669 Vdss (mL/kg) 4 49.3 ± 1.79 MRT (min) 5 8.11 ± 1.07 CL (mL/min/kg) 6 4.24 ± 0.291 Ae24 h (% of dose) 7 ND 8 1 Total area under the plasma concentration-time curve from time zero to time last sampling time. 2 Total area under the plasma concentration-time curve from time zero to infinity.…”

Section: Pk Parametersmentioning

confidence: 99%

“…The major components of bee venom are known to have various biological activities, such as anti-cancer, anti-inflammatory, and neuronal activation [ 2 , 3 , 4 ]. Apitox ® , majorly composed of melittin, was approved for the treatment of patients with osteoarthritis by the US FDA following a phase 3 clinical study and is currently used for patients with arthritis in the Republic of Korea [ 5 , 6 ].…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics and Tissue Distribution of Bee Venom-Derived Phospholipase A2 Using a Sandwich ELISA after Subcutaneous Injection of New Composition Bee Venom in Rats

Chae

Lee

et al. 2023

IJMS

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Bee venom is a traditional drug used to treat the nervous system, musculoskeletal system, and autoimmune diseases. A previous study found that bee venom and one of its components, phospholipase A2, can protect the brain by suppressing neuroinflammation and can also be used to treat Alzheimer’s disease. Thus, new composition bee venom (NCBV), which has an increased phospholipase A2 content of up to 76.2%, was developed as a treatment agent for Alzheimer’s disease by INISTst (Republic of Korea). The aim of this study was to characterize the pharmacokinetic profiles of phospholipase A2 contained in NCBV in rats. Single subcutaneous administration of NCBV at doses ranging from 0.2 mg/kg to 5 mg/kg was conducted, and pharmacokinetic parameters of bee venom-derived phospholipase A2 (bvPLA2) increased in a dose-dependent manner. Additionally, no accumulation was observed following multiple dosings (0.5 mg/kg/week), and other constituents of NCBV did not affect the pharmacokinetic profile of bvPLA2. After subcutaneous injection of NCBV, the tissue-to-plasma ratios of bvPLA2 for the tested nine tissues were all <1.0, indicating a limited distribution of the bvPLA2 within the tissues. The findings of this study may help understand the pharmacokinetic characteristics of bvPLA2 and provide useful information for the clinical application of NCBV.

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“…There, they are exposed to harsher conditions, and disulfide bridges can exert an important stabilizing role to preserve their function [ 10 ]. Important examples include: Hormones, such as insulin, whose function is strongly dependent on correct disulfide formation [ 11 , 12 ]; Functional proteins of the immune system, such as antigen-presenting major histocompatibility complexes (MHCs) [ 13 ] and antibodies [ 14 ]; Natural antimicrobial peptides [ 15 ], such as defensins [ 16 , 17 ]; Respiratory complexes that are key for cell metabolism, such as cytochrome c [ 18 ]; Proteins of the extracellular matrix, such as collagen [ 19 ]; Focal adhesion complexes that link integrins to the cytoskeleton in key processes, such as cell adhesion and migration [ 20 , 21 ]; Several toxins and venom peptides [ 22 , 23 , 24 ]; Ubiquitin transfer between catalytic cysteines leading to protein degradation [ 25 , 26 ]; Enzymes controlling transduction pathways, such as phospodiesterases [ 27 ]. …”

Section: Introductionmentioning

confidence: 99%