scholarly journals Therapeutic Effects of Apamin as a Bee Venom Component for Non-Neoplastic Disease

Toxins ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 195 ◽  
Author(s):  
Hyemin Gu ◽  
Sang Mi Han ◽  
Kwan-Kyu Park
Keyword(s):  
Disulfide Bonds ◽  
Dry Weight ◽  
Bee Venom ◽  
Neoplastic Disease ◽  
Therapeutic Effects ◽  
Amino Acid Residues ◽  
Sk Channels ◽  
Central Nervous System Diseases ◽  
Venom Component ◽  
Bee Colonies

Bee venom is a natural toxin produced by honeybees and plays an important role in defending bee colonies. Bee venom has several kinds of peptides, including melittin, apamin, adolapamine, and mast cell degranulation peptides. Apamin accounts for about 2%–3% dry weight of bee venom and is a peptide neurotoxin that contains 18 amino acid residues that are tightly crosslinked by two disulfide bonds. It is well known for its pharmacological functions, which irreversibly block Ca2+-activated K+ (SK) channels. Apamin regulates gene expression in various signal transduction pathways involved in cell development. The aim of this study was to review the current understanding of apamin in the treatment of apoptosis, fibrosis, and central nervous system diseases, which are the pathological processes of various diseases. Apamin’s potential therapeutic and pharmacological applications are also discussed.

Goblet Cell Mucin of Rat Small Intestine. Chemical and Physical Characterization

1973 ◽  
Vol 51 (8) ◽  
pp. 1154-1166 ◽  
Author(s):  
Janet F. Forstner ◽  
Inderjit Jabbal ◽  
Gordon G. Forstner
Keyword(s):  
Molecular Weight ◽  
Small Intestine ◽  
Goblet Cell ◽  
Disulfide Bonds ◽  
Axial Ratio ◽  
Dry Weight ◽  
Subunit Structure ◽  
Rat Small Intestine ◽  
Minor Components ◽  
Sulfur Containing

Goblet cell mucin (GCM) of rat small intestine has been isolated previously, and its location established by immunofluorescence techniques. In the present study, GCM was characterized more fully by chemical and physical methods. It was found to be a flexible negatively charged macromolecule with a molecular weight of about 2.0 × 106, an intrinsic viscosity of 15.3 dl/g, and an axial ratio of about 225:1. Its composition was protein 12%, total hexose 23%, hexosamine 22.4%, sialic acid 10%, fucose 6.6%, and sulfate < 1% of the dry weight. It contained approximately 34 disulfide bonds per molecule. Like most mucin glycoproteins it was rich in serine, threonine, and proline (45.5 mol %) and poor in hydrophobic and sulfur containing amino acids. One major and two minor components were identified by acrylamide disc gel electrophoresis and analytic ultracentrifugation. The components appeared to represent different molecular weight species of GCM. No evidence of subunit structure could be obtained using a variety of techniques, including the disruption of ionic, hydrophobic, and disulfide bonds by detergents, denaturants, or reducing agents.

scholarly journals Therapeutic effects of bee venom on experimental atopic dermatitis

2018 ◽  
Author(s):  
Hyemin Gu ◽  
Woon‑Hae Kim ◽  
Hyun‑Jin An ◽  
Jung‑Yeon Kim ◽  
Mi‑Gyeong Gwon ◽  
...  
Keyword(s):  
Atopic Dermatitis ◽  
Bee Venom ◽  
Therapeutic Effects

scholarly journals Expression and characterization of a truncated murine Fc gamma receptor.

1988 ◽  
Vol 167 (3) ◽  
pp. 1195-1210 ◽  
Author(s):  
Z X Qu ◽  
J Odin ◽  
J D Glass ◽  
J C Unkeless
Keyword(s):  
B Cells ◽  
Cell Line ◽  
Immune Complexes ◽  
Disulfide Bonds ◽  
Peritoneal Macrophages ◽  
Eukaryotic Expression ◽  
Amino Acid Residues ◽  
Gamma Receptor ◽  
Sds Page ◽  
And Function

We have isolated a recombinant secreted Fc gamma R beta molecule by deletion of the transmembrane and cytoplasmic domains encoding sequence from a Fc gamma R beta 1 cDNA clone, and insertion of the truncated cDNA into a eukaryotic expression vector, pcEXV-3. To express and amplify the production of the truncated Fc gamma R beta molecule, we transfected the truncated cDNA plasmid into a dihydrofolate reductase-minus CHO cell line along with a dhfr minigene, and amplified the gene products with methotrexate. The resulting cell line secretes 2-3 micrograms/ml/24 h of truncated Fc gamma R beta, which can be readily purified by affinity chromatography on IgG-Sepharose. The truncated Fc gamma R beta has a Mr of 31-33,000 on SDS-PAGE and is glycosylated. N-glycosidase F cleavage reduces the Mr to 19,000, consistent with the size of the truncated product, 176 amino acid residues. There are two disulfide bonds in the protein. Binding of immune complexes formed between DNP20BSA and anti-DNP mAbs reveals better binding of IgG1 aggregates than that of IgG2b and IgG2a aggregates. The binding of the immune complexes was somewhat better at more acidic pH, in contrast to previous experiments with binding of purified Fc gamma R to immune complex-coated beads. We were surprised to observe that the truncated Fc gamma R beta did not react with the anti-Fc gamma R mAb 6B7C. Previous work had shown that 6B7C reacts with Fc gamma R on immunoblots, fails to bind to the surface of resting B cells and peritoneal macrophages, but does bind to macrophage cell lines and LPS-stimulated B cells. We show, by binding of mAb 6B7C to a peptide conjugate, that the 6B7C epitope lies within residues 169-183 of the intact Fc gamma R beta, which is just outside the plasma membrane. The availability of the truncated Fc gamma R beta in microgram quantities should facilitate further analysis of structure and function of these receptors.

scholarly journals A Novel Spider Toxin Inhibits Fast Inactivation of the Nav1.9 Channel by Binding to Domain III and Domain IV Voltage Sensors

2021 ◽  
Vol 12 ◽  
Author(s):  
Shuijiao Peng ◽  
Minzhi Chen ◽  
Zhen Xiao ◽  
Xin Xiao ◽  
Sen Luo ◽  
...  
Keyword(s):  
Disulfide Bonds ◽  
Receptor Site ◽  
Site Directed Mutagenesis ◽  
Amino Acid Residues ◽  
Fast Inactivation ◽  
Toxin Binding ◽  
Isolation And Characterization ◽  
Peptide Toxin ◽  
Functional Features ◽  
Domain Iii

Venomous animals have evolved to produce peptide toxins that modulate the activity of voltage-gated sodium (Nav) channels. These specific modulators are powerful probes for investigating the structural and functional features of Nav channels. Here, we report the isolation and characterization of δ-theraphotoxin-Gr4b (Gr4b), a novel peptide toxin from the venom of the spider Grammostola rosea. Gr4b contains 37-amino acid residues with six cysteines forming three disulfide bonds. Patch-clamp analysis confirmed that Gr4b markedly slows the fast inactivation of Nav1.9 and inhibits the currents of Nav1.4 and Nav1.7, but does not affect Nav1.8. It was also found that Gr4b significantly shifts the steady-state activation and inactivation curves of Nav1.9 to the depolarization direction and increases the window current, which is consistent with the change in the ramp current. Furthermore, analysis of Nav1.9/Nav1.8 chimeric channels revealed that Gr4b preferentially binds to the voltage-sensor of domain III (DIII VSD) and has additional interactions with the DIV VSD. The site-directed mutagenesis analysis indicated that N1139 and L1143 in DIII S3-S4 linker participate in toxin binding. In sum, this study reports a novel spider peptide toxin that may slow the fast inactivation of Nav1.9 by binding to the new neurotoxin receptor site-DIII VSD. Taken together, these findings provide insight into the functional role of the Nav channel DIII VSD in fast inactivation and activation.

scholarly journals The Responsiveness of Bee Venom Phospholipase A2 on Regulatory T Cells Correlates with the CD11c+CD206+Population in Human Peripheral Blood Mononuclear Cells

Toxins ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 717
Author(s):  
Heejin Jo ◽  
Hyunjung Baek ◽  
Seon-Young Park ◽  
Bonhyuk Goo ◽  
Woo-Sang Jung ◽  
...  
Keyword(s):  
T Cells ◽  
Regulatory T Cells ◽  
Phospholipase A2 ◽  
Peripheral Blood ◽  
Mononuclear Cells ◽  
Human Peripheral Blood ◽  
Bee Venom ◽  
Control Group ◽  
Therapeutic Effects ◽  
Healthy Human

Bee venom phospholipase A2 (bvPLA2) has been reported to have therapeutic effects such as neuroprotection, anti-inflammation, anti-nociception, anti-cancer properties, caused by increasing regulatory T cells (Tregs). The mechanism of Tregs modulation by bvPLA2 has been demonstrated by binding with the mannose receptor, CD206 in experimental models of several diseases. However, it remains unknown whether this mechanism can also be applied in human blood. In this study, we collected peripheral blood samples from healthy donors and analyzed the percentages of monocyte-derived dendritic cells with CD206 (CD206+ DCs) before expansion, the proportion of Tregs, and the subpopulations after expansion treated with bvPLA2 or PBS using flow cytometry and the correlations among them. The percentage of Tregs tended to be higher in the bvPLA2 group than in the control group. There were significant positive correlations between the CD206 population in hPBMC and the proportions of Tregs treated with bvPLA2, especially in the Treg fold change comparing the increase ratio of Tregs in bvPLA2 and in PBS. These findings indicate that bvPLA2 increased the proportion of Tregs in healthy human peripheral blood and the number of CD206+ DCs could be a predictor of the bvPLA2 response of different individuals.

Cloning and functional expression of a liver isoform of the small conductance Ca2+-activated K+ channel SK3

2001 ◽  
Vol 280 (4) ◽  
pp. C836-C842 ◽  
Author(s):  
Elisabeth T. Barfod ◽  
Ann L. Moore ◽  
Steven D. Lidofsky
Keyword(s):  
Rat Liver ◽  
Metabolic Stress ◽  
Functional Expression ◽  
Mammalian Brain ◽  
K Channel ◽  
Molecular Characteristics ◽  
Amino Acid Residues ◽  
Sk Channels ◽  
Hek 293 ◽  
Small Conductance

Small conductance Ca2+-activated K+(SK) channels have been cloned from mammalian brain, but little is known about the molecular characteristics of SK channels in nonexcitable tissues. Here, we report the isolation from rat liver of an isoform of SK3. The sequence of the rat liver isoform differs from rat brain SK3 in five amino acid residues in the NH3terminus, where it more closely resembles human brain SK3. SK3 immunoreactivity was detectable in hepatocytes in rat liver and in HTC rat hepatoma cells. Human embryonic kidney (HEK-293) cells transfected with liver SK3 expressed 10 pS K+ channels that were Ca2+ dependent (EC50 630 nM) and were blocked by the SK channel inhibitor apamin (IC50 0.6 nM); whole cell SK3 currents inactivated at membrane potentials more positive than −40 mV. Notably, the Ca2+ dependence, apamin sensitivity, and voltage-dependent inactivation of SK3 are strikingly similar to the properties of hepatocellular and biliary epithelial SK channels evoked by metabolic stress. These observations raise the possibility that SK3 channels influence membrane K+ permeability in hepatobiliary cells during liver injury.

Buckwheat trypsin inhibitor with helical hairpin structure belongs to a new family of plant defence peptides

2012 ◽  
Vol 446 (1) ◽  
pp. 69-77 ◽  
Author(s):  
Peter B. Oparin ◽  
Konstantin S. Mineev ◽  
Yakov E. Dunaevsky ◽  
Alexander S. Arseniev ◽  
Mikhail A. Belozersky ◽  
...  
Keyword(s):  
Trypsin Inhibitor ◽  
Disulfide Bonds ◽  
Plant Defence ◽  
Three Dimensional ◽  
Structural Similarity ◽  
Reversed Phase ◽  
Dimensional Structure ◽  
Amino Acid Residues ◽  
New Family ◽  
Helical Hairpin

A new peptide trypsin inhibitor named BWI-2c was obtained from buckwheat (Fagopyrum esculentum) seeds by sequential affinity, ion exchange and reversed-phase chromatography. The peptide was sequenced and found to contain 41 amino acid residues, with four cysteine residues involved in two intramolecular disulfide bonds. Recombinant BWI-2c identical to the natural peptide was produced in Escherichia coli in a form of a cleavable fusion with thioredoxin. The 3D (three-dimensional) structure of the peptide in solution was determined by NMR spectroscopy, revealing two antiparallel α-helices stapled by disulfide bonds. Together with VhTI, a trypsin inhibitor from veronica (Veronica hederifolia), BWI-2c represents a new family of protease inhibitors with an unusual α-helical hairpin fold. The linker sequence between the helices represents the so-called trypsin inhibitory loop responsible for direct binding to the active site of the enzyme that cleaves BWI-2c at the functionally important residue Arg19. The inhibition constant was determined for BWI-2c against trypsin (1.7×10−10 M), and the peptide was tested on other enzymes, including those from various insect digestive systems, revealing high selectivity to trypsin-like proteases. Structural similarity shared by BWI-2c, VhTI and several other plant defence peptides leads to the acknowledgement of a new widespread family of plant peptides termed α-hairpinins.

scholarly journals The Potential Therapeutic Effects of Artesunate on Stroke and Other Central Nervous System Diseases

2016 ◽  
Vol 2016 ◽  
pp. 1-16 ◽  
Author(s):  
Shilun Zuo ◽  
Qiang Li ◽  
Xin Liu ◽  
Hua Feng ◽  
Yujie Chen
Keyword(s):  
Neurological Disorders ◽  
Therapeutic Effects ◽  
Nervous System Diseases ◽  
Foreseeable Future ◽  
Central Nervous System Diseases ◽  
Pharmacological Activities ◽  
Pharmacological Mechanism ◽  
Single Mechanism ◽  
Anti Inflammation ◽  
Pathophysiologic Mechanisms

Artesunate is an important agent for cerebral malaria and all kinds of other severe malaria because it is highly efficient, lowly toxic, and well-tolerated. Loads of research pointed out that it had widespread pharmacological activities such as antiparasites, antitumor, anti-inflammation, antimicrobes activities. As we know, the occurrence and development of neurological disorders usually refer to intricate pathophysiologic mechanisms and multiple etiopathogenesis. Recent progress has also demonstrated that drugs with single mechanism and serious side-effects are not likely the candidates for treatment of the neurological disorders. Therefore, the pluripotent action of artesunate may result in it playing an important role in the prevention and treatment of these neurological disorders. This review provides an overview of primary pharmacological mechanism of artesunate and its potential therapeutic effects on neurological disorders. Meanwhile, we also briefly summarize the primary mechanisms of artemisinin and its derivatives. We hope that, with the evidence presented in this review, the effect of artesunate in prevention and curing for neurological disorders can be further explored and studied in the foreseeable future.

scholarly journals Evaluation of Phytochemical and Antioxidant Properties of 15 Italian Olea europaea L. Cultivar Leaves

Molecules ◽  
2019 ◽  
Vol 24 (10) ◽  
pp. 1998 ◽  
Author(s):  
Francesca Nicolì ◽  
Carmine Negro ◽  
Marzia Vergine ◽  
Alessio Aprile ◽  
Eliana Nutricati ◽  
...  
Keyword(s):  
Superoxide Anion ◽  
Olea Europaea ◽  
Antioxidant Activities ◽  
Antioxidant Properties ◽  
Dry Weight ◽  
Total Phenolic ◽  
Therapeutic Effects ◽  
Leaf Extracts ◽  
Olea Europaea L ◽  
Olea Europaéa

Olive leaf extracts are of special interest due to their proven therapeutic effects. However, they are still considered a by-product of the table olive and the oil industries. In order to learn possible ways of exploiting this waste for health purposes, we investigated the phytochemical profiles and antioxidant activities in the leaves of 15 Italian Olea europaea L. cultivars grown in the same pedoclimatic conditions. The phenolic profiles and amounts of their seven representative compounds were analyzed using HPLC ESI/MS-TOF. The antioxidant activities were determined using three different antioxidant assays (DPPH, ORAC, and superoxide anion scavenging assay). Wide ranges of total phenolic content (11.39–48.62 g GAE kg−1 dry weight) and antioxidant activities (DPPH values: 8.67–29.89 µmol TE mg−1 dry weight, ORAC values: 0.81–4.25 µmol TE mg−1 dry weight, superoxide anion scavenging activity values: 27.66–48.92 µmol TE mg−1 dry weight) were found in the cultivars. In particular, the cultivars Itrana, Apollo, and Maurino, showed a high amount of total phenols and antioxidant activity, and therefore represent a suitable natural source of biological compounds for use in terms of health benefits.

scholarly journals Therapeutic Effects of Bee Venom

2019 ◽  
pp. 1-5
Author(s):  
Rezzan Aliyazicioglu
Keyword(s):  
Inflammatory Diseases ◽  
Scientific Evidence ◽  
Bee Venom ◽  
Therapeutic Effects ◽  
Active Components ◽  
The Central Nervous System ◽  
Underlying Mechanisms ◽  
Analgesic Activities ◽  
History Of Use ◽  
Pain Symptoms

Bee venom (BV) has a long history of use in Korea for the relief of pain symptoms and for the treatment of various inflammatory diseases, including rheumatoid arthritis. There is some evidence for the underlying mechanisms involved in the venom’s anti-inflammatory and analgesic activities. Recent clinical and experimental reearch has confirmed that the venom and its active components can be applied to a broad spectrum of immunological and neurodegenerative diseases, including autoimmune diseases and Parkinson’s disease. BV has been shown to exhibit these effects by modulating immune cells in the periphery, together with glial cells and neurons in the central nervous system. This review sets out the latest scientific evidence concerning the therapeutic effects of BV and various components thereof in the context of a number of diseases, and provides a detailed description of the mechanisms.

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