Evaluation of the Analgesic Activity of Standardized Aqueous Extract of Terminalia chebula in Healthy Human Participants Using Hot Air Pain Model

Kumar, Chiranjeevi Uday; Pokuri, Venkata Kishan; Pingali, Usharani

doi:10.7860/jcdr/2015/11369.5916

Cited by 15 publications

(13 citation statements)

References 13 publications

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“…The results in the present study are similar to other studies done in our department, where we have reported an increase in pain threshold and tolerance using thermal or mechanical pain models. [20][21][22] In our study, the observed analgesic activity could be attributed to increased GLP-1 concentrations due to inhibition of DPP4 enzyme by teneligliptin and probably to resultant activation of GLP-1 Rs in spinal microglia and release of endogenous endorphins as mentioned in the studies quoted above. The endorphins in turn may activate the peripheral opioid receptors resulting in analgesic activity of teneligliptin as evidenced by an increase in pain threshold and tolerance time.…”

Section: Discussionmentioning

confidence: 56%

Evaluation of the analgesic activity of single and multiple oral doses of teneligliptin (20 mg/day), using hot air analgesiometer in healthy human volunteers: a randomized, double blind, placebo controlled, cross over study

Butul

Pingali

Nutalapati

2020

Int J Basic Clin Pharmacol

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Background DPP-4inhibitors showed analgesic and anti-inflammatory activity in human and animal-studies. DPP-4 inhibitors improved nerve function and thermal nociception in animal models. Aim of the study was to explore analgesic activity of single and multiple doses of teneligliptin 20 mg/day using hot air analgesiometer in healthy human volunteers.Methods: After IEC approval and informed consent, subjects were randomized to receive either teneligliptin 20 mg or placebo in double-blinded manner with standard breakfast. Mean pain threshold and tolerance(sec) using hot air analgesiometer were recorded at baseline and 1 hr, 2 hrs post drug on day1, for single dose study. Subsequently drugs were administered under supervision daily for 6 days and same procedure repeated on day8 for multiple-dose study. After 2 weeks washout, subjects crossed over in period 2 to other formulation and same procedure repeated to determine study parameters. Fasting blood-sugar (FBS) monitored, ADRs recorded in CRF. Statistical analysis done with SPSS20.0.Results: Twelve-healthy subjects (8 males, 4 females) with mean age 33.08±4.69 years, mean BMI 22.6±1.37kg/m2 participated. Single dose teneligliptin produced significant increase in pain threshold (35.9%) and pain tolerance (25.1%) (p<0.0001) at 1hour compared to baseline. With multiple doses, pain threshold increased by 37.1% and pain tolerance by 25.4% (p<0.0001) at 1hour compared to baseline. The increase in pain threshold and tolerance values at 1 and 2 hours were similar. There was no significant change in pain threshold(p=0.4135) and tolerance (p=0.4476) at baseline on day1 and day 8. Placebo showed non-significant change in study parameters. Both treatments well tolerated. FBS of volunteers within normal limits during treatment period and no hypoglycemia reported.Conclusions: Results of our study suggest that teneligliptin20mg in healthy subjects demonstrated significant analgesic activity on day 1 and day 8 compared to baseline & placebo. Its role in painful diabetic conditions can be further explored.

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Section: Discussionmentioning

confidence: 56%

Evaluation of the analgesic activity of single and multiple oral doses of teneligliptin (20 mg/day), using hot air analgesiometer in healthy human volunteers: a randomized, double blind, placebo controlled, cross over study

Butul

Pingali

Nutalapati

2020

Int J Basic Clin Pharmacol

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“…This difference in the ability to detect minimal clinically relevant change acutely supports our observations in VAS that were not otherwise apparent sooner on mWOMAC. The work of both Kumar et al and Pokuri et al demonstrated potent, acute analgesic threshold and tolerance effects of aqueous Terminalia chebula extract (AyuFlex) at 1000 mg/day in healthy human subjects [ 22 , 35 ]. Improvements in VAS measures across multiple time points, global mKOOS, and mWOMAC physical function may stem from increased pain threshold and tolerance via central and peripheral mechanisms that include anti-inflammatory COX, LOX, and TNF-a inhibition [ 36 ].…”

Section: Discussionmentioning

confidence: 99%

Effects of dietary supplementation with a standardized aqueous extract of Terminalia chebula fruit (AyuFlex®) on joint mobility, comfort, and functional capacity in healthy overweight subjects: a randomized placebo-controlled clinical trial

Lopez¹,

Habowski²,

Sandrock³

et al. 2017

BMC Complement Altern Med

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BackgroundJoint and connective tissue integrity, comfort and function are paramount to optimal performance in exercise, recreational and occupational activities. The fruit of Terminalia chebula has been used extensively in various traditional health systems for different ailments, with additional preclinical and clinical data demonstrating antioxidant and anti-inflammatory potential. The aim of this study was to evaluate the effects of a standardized aqueous extract of Terminalia chebula fruit (AyuFlex®) dietary supplementation on joint mobility, comfort, and functional capacity in healthy overweight subjects.MethodsOne-hundred and five (105) overweight, apparently healthy male and female subjects (35–70 years of age) were pre-screened and randomized to one of three groups for 84 days: placebo, AyuFlex1 (250 mg twice daily) or AyuFlex2 (500 mg twice daily) in a randomized, double-blind, placebo-controlled design. A two-week placebo lead-in period was used to improve data quality/validity. All subjects had no knee joint discomfort at rest, but experienced knee joint discomfort only with activity/exercise of at least 30 on 100 mm Visual Analog Scale (VAS). Primary outcome measures included symptoms of joint health and function as measured by modified-Knee Injury & Osteoarthritis Outcomes Score (mKOOS) global & modified-Western Ontario and McMaster Universities Arthritis Index (mWOMAC) subscales (discomfort, stiffness and function). Secondary outcomes included VAS questionnaires on overall/whole-body joint health, low back health, knee mobility, willingness and ability to exercise, 6-min walk test for distance and range of motion (ROM) of pain-free knee flexion/extension. Tertiary outcome measures included inflammatory (high sensitivity C-reactive protein (hsCRP), tumor necrosis factor (TNF)-α) and extracellular matrix (ECM)/Connective Tissue (COMP) biomarkers, and safety (vital signs and blood markers) & tolerability (Adverse Event (AE)/ side effect profiles).ResultsCompared to placebo, at day 84 AyuFlex® treatment significantly: 1) improved mKOOS global scores in AyuFlex1 + AyuFlex2 (P = 0.023), and improved total and physical function subscale of mWOMAC relative to baseline, 2) improved VAS scores for Knee Discomfort with activity/exercise in AyuFlex1 + AyuFlex2 (P = 0.001) relative to baseline, 3) improved VAS scores for whole-body joint function in AyuFlex1 + AyuFlex2 (P < 0.029) relative to baseline, 4) improved VAS score for decreased knee joint soreness following leg extension challenge for AyuFlex1 (P = 0.022) and AyuFlex2 (P = 0.043) relative to baseline, 5) improved 6-min walk performance distance covered (P = 0.047) and VAS discomfort (P = 0.026) post-6 min walk in AyuFlex1 + AyuFlex2 relative to baseline, 6) and tended to decrease COMP levels in AyuFlex1 + AyuFLex2 (P = 0.104) relative to baseline. All biomarkers of safety remained within normative limits during the study. Low back health tended to improve in the AyuFlex1 and AyuFlex2 group, but failed to reach significance relative to placebo group.Con...

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“…In a study to analyse the analgesic properties of the fruits of T. chebula (Kumar, Pokuri, & Pingali, 2015;Pokuri, Kumar, & Pingali, 2016). In another study using fruits of T. chebula (water extract) where pain was induced by 0.1% formalin in mice, it was documented that extract exhibit analgesic activity attributed to its inhibitory action on the synthesis and/or release of inflammatory factors (Sireeratawong, Jaijoy, Khonsung, & Soonthornchareonnon, 2014).…”

Section: Analgesic Effectmentioning

confidence: 99%

“…Moreover, CA also has been reported to restrain the proliferation/growth of retinoblastoma cells by modulating mitochondrial membrane permeabilization, induction of Cytochrome c release, activation of caspase 3 and imbalancing the Bax/Bcl 2 ratio towards cell death. Furthermore it also activates G1 cell cycle arrest by increasing the expression of p27, a CDK inhibitor (Kumar et al, 2015).…”

Section: Antitumour Antimutagenic and Radioprotective Activitiesmentioning

confidence: 99%

Fruits ofTerminalia chebulaRetz.: A review on traditional uses, bioactive chemical constituents and pharmacological activities

Nigam

Mishra

Adhikari‐Devkota

et al. 2020

Phytotherapy Research

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Fruits of Terminalia chebula Retz. (Combretaceae) are widely used as crude drugs in various traditional medicine systems. The aim of this article is to review the available scientific information regarding the traditional uses, bioactive chemical constituents and the pharmacological activities of T. chebula. Numerous researches conducted on T. chebula have confirmed the presence of wide range of the phytochemicals such as flavonoids, tannins, phenolic acids and other bioactive compounds. T. chebula is also widely studied regarding its pharmacological activities such as antioxidant, hepatoprotective, neuroprotective, cytotoxic, antidiabetic, anti-inflammatory activities among others. However, more in vivo and clinical studies for mechanism-based pharmacological evaluation should be conducted in future to provide stronger scientific evidences for their traditional uses.

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Evaluation of the Analgesic Activity of Standardized Aqueous Extract of Terminalia chebula in Healthy Human Participants Using Hot Air Pain Model

Cited by 15 publications

References 13 publications

Evaluation of the analgesic activity of single and multiple oral doses of teneligliptin (20 mg/day), using hot air analgesiometer in healthy human volunteers: a randomized, double blind, placebo controlled, cross over study

Evaluation of the analgesic activity of single and multiple oral doses of teneligliptin (20 mg/day), using hot air analgesiometer in healthy human volunteers: a randomized, double blind, placebo controlled, cross over study

Effects of dietary supplementation with a standardized aqueous extract of Terminalia chebula fruit (AyuFlex®) on joint mobility, comfort, and functional capacity in healthy overweight subjects: a randomized placebo-controlled clinical trial

Fruits ofTerminalia chebulaRetz.: A review on traditional uses, bioactive chemical constituents and pharmacological activities

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