scholarly journals Inhibitory Effect of Lactobacillus plantarum CQPC02 Isolated from Chinese Sichuan Pickles (Paocai) on Constipation in Mice

2019 ◽  
Vol 2019 ◽  
pp. 1-13 ◽  
Author(s):  
Bihui Liu ◽  
Xin Yang ◽  
Liujin Guo ◽  
Jing Zhang ◽  
Xianrong Zhou ◽  
...  
Keyword(s):  
Activated Carbon ◽  
Lactobacillus Plantarum ◽  
Transient Receptor Potential ◽  
Receptor Potential ◽  
Inhibitory Effect ◽  
Lactobacillus Delbrueckii ◽  
High Concentration ◽  
Inhibition Effect ◽  
Probiotic Potential ◽  
Transient Receptor

Sichuan pickles (Paocai) are a traditional Chinese fermented vegetable food that is rich in beneficial microorganisms. In this study, the inhibition of constipation by Lactobacillus plantarum CQPC02 (LP-CQPC02) isolated from Sichuan Paocai was studied by establishing a constipation model of mice using activated carbon. The constipation inhibition effect of LP-CQPC02 was determined by observing the defecation of mice, rate of active carbon propulsion, pathological section observation, serum index, and small intestinal mRNA expression. The results showed that LP-CQPC02 inhibited the decrease in body weight caused by constipation in mice. At the same time, LP-CQPC02 also increased the propulsion rate of activated carbon in the small intestine and shortened the time of discharge for the first black stool. LP-CQPC02 increased gastrin (Gas), motilin (MTL), endothelin (ET), and acetylcholinesterase (AChE) in constipated mice, and it also decreased the level of somatostatin (SS). qPCR results showed that LP-CQPC02 upregulated the expression of c-Kit, stem cell factor (SCF), and glial cell-derived neurotrophic factor (GDNF) and downregulated the expression of transient receptor potential cation channel subfamily V member 1 (TRPV1) and inducible nitric oxide synthase (iNOS) in mice with constipation, and a stronger effect was observed with a high concentration of LP-CQPC02. The experimental results showed that LP-CQPC02 has a stronger constipation inhibitory effect than the commonly used commercial Lactobacillus delbrueckii subsp. bulgaricus (LB), and the inhibitory effect of LP-CQPC02 on constipation increases with increasing concentration of LP-CQPC02. Therefore, LP-CQPC02 is a high-quality microbial resource with a good constipation inhibition effect and probiotic potential.

scholarly journals Eugenol Inhibits Sodium Currents in Dental Afferent Neurons

2006 ◽  
Vol 85 (10) ◽  
pp. 900-904 ◽  
Author(s):  
C.-K. Park ◽  
H.Y. Li ◽  
K.-Y. Yeon ◽  
S.J. Jung ◽  
S.-Y. Choi ◽  
...  
Keyword(s):  
Molecular Mechanisms ◽  
Transient Receptor Potential ◽  
Receptor Potential ◽  
Inhibitory Effect ◽  
Transient Receptor Potential Vanilloid ◽  
Afferent Neurons ◽  
Patch Clamp Technique ◽  
Independent Manner ◽  
Pre Treatment ◽  
Transient Receptor

Although eugenol is widely used in dentistry, little is known about the molecular mechanisms responsible for its anesthetic properties. In addition to calcium channels, recently demonstrated by our group, there could be another molecular target for eugenol. Using a whole-cell patch-clamp technique, we investigated the effect of eugenol on voltage-gated sodium channel currents ( I Na) in rat dental primary afferent neurons identified by retrograde labeling with a fluorescent dye in maxillary molars. Eugenol inhibited action potentials and I Na in both capsaicin-sensitive and capsaicin-insensitive neurons. The pre-treatment with capsazepine, a competitive antagonist of transient receptor potential vanilloid 1 (TRPV1), failed to block the inhibitory effect of eugenol on I Na, suggesting no involvement of TRPV1. Two types of I Na, tetrodotoxin (TTX)-resistant and TTX-sensitive I Na, were inhibited by eugenol. Our results demonstrated that eugenol inhibits I Na in a TRPV1-independent manner. We suggest that I Na inhibition by eugenol contributes to its analgesic effect.

scholarly journals A Molecular Basis for the Inhibition of Transient Receptor Potential Vanilloid Type 1 by Gomisin A

2017 ◽  
Vol 2017 ◽  
pp. 1-8 ◽  
Author(s):  
Sung Bae Lee ◽  
Shinhwa Noh ◽  
Hye Duck Yeom ◽  
Heejin Jo ◽  
Sanung Eom ◽  
...  
Keyword(s):  
Molecular Basis ◽  
Transient Receptor Potential ◽  
Receptor Potential ◽  
Inhibitory Effect ◽  
Transient Receptor Potential Vanilloid ◽  
Trpv1 Channel ◽  
Double Mutation ◽  
Extracellular Region ◽  
Gomisin A ◽  
Transient Receptor

Transient receptor potential (TRP) channel has critical actions as conditional sensors in primary afferent neurons. We studied the regulatory action of gomisin A on TRPV1 channel current in this report. Schisandra chinensis contains bioactive compounds such as the gomisin derivatives and their related compounds. Coapplication with gomisin A inhibited the capsaicin-mediated inward peak current. This inhibitory effect of gomisin A on capsaicin-induced inward current showed concentration-dependence and was reversible. The half maximal inhibitory concentration of gomisin A was 62.7±8.4 µM. In addition, this inhibition occurred in a noncompetition regulation mode and voltage insensitive manner. Furthermore, molecular docking studies of gomisin A on TRPV1 showed that it interacted predominantly with residues at cavities in the segments 1 and 2 of each subunit. Four potential binding sites for this ligand in the extracellular region at sensor domain of TRPV1 channel were identified. Point mutagenesis studies were undertaken, and gomisin A potency decreased for both the Y453A and N467A mutants. The double mutation of Y453 and N467 significantly attenuated inhibitory effects by gomisin A. In summary, this study revealed the molecular basis for the interaction between TRPV1 and gomisin A and provides a novel potent interaction ligand.

The Transient Receptor Potential Vanilloid 4 Agonist RN-1747 Inhibits the Calcium Response to Histamine

Pharmacology ◽  
2019 ◽  
Vol 104 (3-4) ◽  
pp. 166-172 ◽  
Author(s):  
Beatrix Pfanzagl ◽  
Roswitha Pfragner ◽  
Erika Jensen-Jarolim
Keyword(s):  
Hela Cells ◽  
Transient Receptor Potential ◽  
Receptor Potential ◽  
Inhibitory Effect ◽  
Cation Channels ◽  
Transient Receptor Potential Vanilloid ◽  
Calcium Response ◽  
Intestinal Hypersensitivity ◽  
Transient Receptor ◽  
Line P

Background: Sensitization of transient receptor potential (TRP) cation channels probably contributes to intestinal hypersensitivity, a hallmark of gastrointestinal disorders. Histamine acting via histamine 1 receptor (H1R) to open TRP cation channels might also be involved. Method: The enterochromaffin cell line P-STS, responsive to histamine via H1R, was used as model to study possible synergism between histamine and TRP vanilloid 4 (TRPV4) pathways. Results: The TRPV4 antagonist RN-1734, but not HC-067047, inhibited the cytoplasmic calcium response to histamine in P-STS cells. However, also pre-incubation with the TRPV4 agonist RN-1747 strongly inhibited the calcium response to histamine in P-STS as well as HeLa cells. This inhibitory effect of RN-1747 was not due to its known TRP melastatin 8 (TRPM8) antagonism, as the TRPM8 antagonist RQ-00203078 showed no significant effect on the histamine-induced calcium response of P-STS or HeLa cells. Conclusion: The TRPV4 agonist RN-1747, and possibly also the structurally similar TRPV4 antagonist RN-1734, should be used with caution because of yet unidentified interference with histamine signaling via H1R.

scholarly journals Teriparatide improves pain-related behavior and prevents bone loss in ovariectomized mice

2019 ◽  
Vol 28 (1) ◽  
pp. 230949901989319 ◽  
Author(s):  
Sho Kato ◽  
Hiroki Wakabayashi ◽  
Taro Nakagawa ◽  
Gaku Miyamura ◽  
Yohei Naito ◽  
...  
Keyword(s):  
Bone Loss ◽  
Transient Receptor Potential ◽  
Receptor Potential ◽  
Transient Receptor Potential Channel ◽  
Inhibitory Effect ◽  
Mechanical Hyperalgesia ◽  
Drg Neurons ◽  
Ovariectomized Mice ◽  
Hind Limbs ◽  
Transient Receptor

Purpose: The aim of this study was to examine the inhibitory effect of teriparatide (TPTD) on pain and on bone loss in ovariectomized (OVX) mice. The mechanism of osteoporotic pain in OVX mice was evaluated through an examination of pain-related behavior as well as immunohistochemical examinations. Methods: Eight-week-old female ddY mice were OVX and assigned to one of three groups: (1) OVX mice treated with vehicle (OVX), (2) OVX mice treated with teriparatide (OVX-TPTD), or (3) SHAM-operated mice treated with vehicle (SHAM). Starting immediately after surgery, vehicle or TPTD was injected subcutaneously. After a 4-week treatment, mechanical sensitivity was tested using von Frey filaments. The proximal tibial metaphyses were analyzed three-dimensionally by microcomputed tomography (μCT). Calcitonin gene-related peptide (CGRP) and transient receptor potential channel vanilloid 1 (TRPV1) expressions in L3–5 dorsal root ganglion (DRG) neurons were examined using immunohistochemistry. Results: Ovariectomy induced bone loss and mechanical hyperalgesia in the hind limbs with upregulation of CGRP and TRPV1 expressions in DRG neurons innervating the hind limbs. Bone loss was prevented more effectively in the OVX-TPTD mice than in the OVX mice. Furthermore, mechanical hyperalgesia and upregulation of CGRP and TRPV1 expressions were significantly lower in the OVX-TPTD mice than in the OVX mice. Conclusion: TPTD treatment prevented ovariectomy-induced bone loss and ovariectomy-induced mechanical hyperalgesia in hind limbs, and it suppressed CGRP and TRPV1 expressions in DRG neurons. These results suggest that TPTD is useful for the treatment of osteoporotic pain in postmenopausal women.

scholarly journals Coexpression and activation of TRPV1 suppress the activity of the KCNQ2/3 channel

2011 ◽  
Vol 138 (3) ◽  
pp. 341-352 ◽  
Author(s):  
Xu-Feng Zhang ◽  
Ping Han ◽  
Torben R. Neelands ◽  
Steve McGaraughty ◽  
Prisca Honore ◽  
...  
Keyword(s):  
Transient Receptor Potential ◽  
Neuronal Excitability ◽  
Receptor Potential ◽  
Inhibitory Effect ◽  
Negative Regulator ◽  
Hek293 Cells ◽  
Transient Receptor Potential Vanilloid ◽  
Hek 293 ◽  
Dorsal Root Ganglia Neurons ◽  
Transient Receptor

Transient receptor potential vanilloid 1 (TRPV1) is a ligand-gated nonselective cation channel expressed predominantly in peripheral nociceptors. By detecting and integrating diverse noxious thermal and chemical stimuli, and as a result of its sensitization by inflammatory mediators, the TRPV1 receptor plays a key role in inflammation-induced pain. Activation of TRPV1 leads to a cascade of pro-nociceptive mechanisms, many of which still remain to be identified. Here, we report a novel effect of TRPV1 on the activity of the potassium channel KCNQ2/3, a negative regulator of neuronal excitability. Using ion influx assays, we revealed that TRPV1 activation can abolish KCNQ2/3 activity, but not vice versa, in human embryonic kidney (HEK)293 cells. Electrophysiological studies showed that coexpression of TRPV1 caused a 7.5-mV depolarizing shift in the voltage dependence of KCNQ2/3 activation compared with control expressing KCNQ2/3 alone. Furthermore, activation of TRPV1 by capsaicin led to a 54% reduction of KCNQ2/3-mediated current amplitude and attenuation of KCNQ2/3 activation. The inhibitory effect of TRPV1 appears to depend on Ca2+ influx through the activated channel followed by Ca2+-sensitive depletion of phosphatidylinositol 4,5-bisphosphate and activation of protein phosphatase calcineurin. We also identified physical interactions between TRPV1 and KCNQ2/3 coexpressed in HEK293 cells and in rat dorsal root ganglia neurons. Mutation studies established that this interaction is mediated predominantly by the membrane-spanning regions of the respective proteins and correlates with the shift of KCNQ2/3 activation. Collectively, these data reveal that TRPV1 activation may deprive neurons from inhibitory control mediated by KCNQ2/3. Such neurons may thus have a lower threshold for activation, which may indirectly facilitate TRPV1 in integrating multiple noxious signals and/or in the establishment or maintenance of chronic pain.

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