tannins and Pain

Fadolmidine (MPV-2426) is a novel alpha2 -adrenoceptor (alpha2) -AR) agonist developed for spinal analgesia. It is highly selective for alpha2 -ARs, but it lacks subtype selectivity. Due to its pharmacokinetic properties, it only poorly penetrates blood-brain barrier or spreads from the site of injection within the central nervous system. By intrathecal (i.t.) administration to laboratory animals, fadolmidine produces dose-dependent antinociception in healthy controls and in models of inflammatory, postoperative and neuropathic pain. Fadolmidine has been effective against various submodalities of pain such as heat pain, mechanical pain, and visceral pain. In general, the antinociceptive potency of fadolmidine, i.t., was equal to that of dexmedetomidine. At antinociceptive i.t. doses fadolmidine did not suppress motoneurons or responses to innocuous stimulation. It produced no hemodynamic depression and considerably less sedation than dexmedetomidine. By peripheral administration fadolmidine had no or only a weak antinociceptive action, except following nerve injury, particularly that of the postganglionic sympathetic nerve fibers. Together these experimental animal studies indicate that i.t. administration of fadolmidine provides a segmentally restricted treatment of somatic and visceral pain, with only minor cardiovascular and sedative side effects. Additionally, peripheral administration of fadolmidine might provide a selective treatment for some hypersensitivity states that involve dysfunction of the sympathetic nervous system.

Topics: Adrenergic Agonists; Adrenergic alpha-2 Receptor Agonists; Analgesics; Animals; Dose-Response Relationship, Drug; Humans; Hydrolyzable Tannins; Imidazoles; Indans; Injections, Spinal; Pain; Rats; Tannins

To assess the efficacy of thrice daily topical 4Jointz utilizing Acteev technology (a combination of a standardized comfrey extract and a pharmaceutical grade tannic acid, 3.5 g/day) on osteoarthritic knee pain, markers of inflammation and cartilage breakdown over 12 weeks.. Adults aged 50-80 years (n = 133) with clinical knee OA were randomised to receive 4Jointz or placebo in addition to existing medications. Pain and function were measured using a visual analogue scale (VAS) and the Knee Injury and Osteoarthritis Outcome Score (KOOS) scale at baseline, 4, 8 and 12 weeks. Inflammation was measured analysing IL-6 expression and CTX-2 presence as representative for cartilage breakdown using ELISA, at baseline and 12 weeks.. Pain scores significantly reduced in the group who received 4Jointz compared to the group who received placebo after 12 weeks using both the VAS (-9.9 mm, P = 0.034) and the KOOS pain scale (+5.7, P = 0.047). Changes in IL-6 and CTX-2 were not significant (-0.04, P = 0.5; -0.01, P = 0.68). Post-hoc analyses suggested that treatment may be most effective in women (VAS -16.8 mm, P = 0.008) and those with milder radiographic osteoarthritis (OA) (VAS -16.1 mm, P = 0.009). Rates of adverse events were similar in both groups, excepting local rash that was more common amongst participants receiving 4Jointz (21% vs 1.6%, IRR 13.2, P = 0.013), but only 26% (n = 4) of participants with rashes discontinued treatment. There were no changes in systemic blood results.. Topical treatment using 4Jointz reduced pain but had no effect on inflammation or cartilage breakdown over 12 weeks of treatment.. Australia and New Zealand Clinical Trials registry ACTRN12610000877088.

Topics: Administration, Topical; Aged; Aged, 80 and over; Analgesics; Comfrey; Double-Blind Method; Drug Combinations; Female; Humans; Knee Joint; Male; Middle Aged; Osteoarthritis, Knee; Pain; Pain Management; Pain Measurement; Plant Extracts; Recovery of Function; Tannins; Treatment Outcome

Medicinal plants belonging to the genus Mimosa, such as Mimosa tenuiflora, M. caesalpinifolia, and M. verrucosa are known for their popular use for asthma, bronchitis and fever. Ethnopharmacological studies report that Mimosa acutistipula is used to treat alopecia and pharyngitis, conditions that can be related to oxidative stress, inflammatory processes and painful limitations. However, there is no studies on its efficacy and mechanism of action.. To elucidate the antioxidant, anti-inflammatory, analgesic and antipyretic activity of M. acutistipula leaves.. Phytochemical profile of M. acutistipula extracts was evaluated by several reaction-specific methods. Secondary metabolites such as tannins, phenols and flavonoids were quantified with colorimetric assays. In vitro antioxidant potential was evaluated using DPPH and ABTS + as free radical scavenging tests, FRAP and phosphomolybdenum as oxide-reduction assays, and anti-hemolytic for lipid peroxidation evaluation. In vivo anti-inflammatory evaluation was performed by paw edema, and peritonitis induced by carrageenan. Analgesic effect and its possible mechanisms were determined by acetic acid-induced abdominal writhing and the formalin test. Antipyretic activity was evaluated by yeast-induced fever.. M. acutistipula leaves ethyl acetate extract showed expressive concentrations of phenolic compounds and antioxidant activity. It also exhibited anti-inflammatory and analgesic activity, besides its antipyretic effect. Thus, these results provide information regarding its popular use and might help future therapeutics involving this specimen.

Topics: Analgesics; Anti-Inflammatory Agents; Antioxidants; Antipyretics; Edema; Flavonoids; Methanol; Mimosa; Pain; Peritonitis; Phenols; Plant Extracts; Tannins

Moringa oleifera Lam (Moringaceae) is a highly valued plant, distributed in many countries of the tropics and subtropics. It has an impressive range of medicinal uses with high nutritional value.. The commercially processed M. oleifera was extracted using methanol as its solvent. Phytochemical analysis as well as the anti-oxidant properties of this supplement were also investigated. Acute toxicity was carried out in fasted mice. Carrageenan and histamine tests were used to assess anti-inflammatory effects in rats, while analgesic activities were assessed using the acetic acid-induced writhing test and formalin-induced paw lick test in mice. In the anti-oxidant tests, 1,1-diphenyl-2-picrylhydrazyl, ferrous reducing activity power, 2,21-azinobis-(3-ethylbenthialozine)-6-sulphonic acid and total polyphenolic (TPP) assays were deployed at concentrations of 10 mg/mL and 20 mg/mL.. The phytochemical analysis showed that the extract contained flavonoids, terpenoids, glycosides, tannins and saponins. In the acetic acid-induced writhing test, the extract significantly reduced the number of writhes at 100 and 200 mg/kg but not so much at 50 mg/kg. In the formalin-induced paw lick test, the effect was similar to that of the acetic writhing test. The analgesic effects were comparable to that of indomethacin used at 10 mg/kg. In the anti-inflammatory test, the extract reduced the formation of oedema especially at a dose of 200 mg/kg. In the anti-oxidant test, the extract was found to possess a free radical-scavenging property and is concentration related.. The use of this extract for medicinal and nutritional purposes may have thus been justified; however, caution must be exercised in its use to prevent the toxic effect.

Topics: Analgesics; Animals; Animals, Laboratory; Anti-Inflammatory Agents; Antioxidants; Edema; Female; Flavonoids; Glycosides; Inflammation; Methanol; Mice; Moringa oleifera; Pain; Phytochemicals; Plant Extracts; Plant Leaves; Rats; Rats, Wistar; Saponins; Tannins; Terpenes

Oxidative stress and analgesia are connected with different pathological conditions. The drug candidates from synthetic sources are associated with various side effects; therefore, researchers are giving priority to find novel, effective and safe phytomedicines. Teucrium species possesses antioxidant, analgesic, anti-inflammatory and hepatoprotective activities. The essential oils of Teucrium stocksianum have shown strong antinociceptive potential. Our current study is designed to embark total phenolic content (TPC), antioxidant and antinociceptive potential of the methanolic extract of Teucrium stocksianum (METS).. Phytochemical composition was determined by using standard methods. Free radical scavenging potential and TPC of METS were assessed by using 2, 2-diphenyl-1-picryl-hydrazyl (DPPH) and Folin-Ciocalteu Reagent (FCR) respectively. Antinociceptive potential was determined by acetic acid induced abdominal writhing, formalin induced paw licking and tail immersion tests. Different test dose 50, 100 and 150 mg/kg body weight of METS were administered intra peritonealy (i.p) to various groups of mice for the evaluation of analgesic potential.. Phytochemical screening confirmed the presence of flavonoids, tannins, saponins, anthraquinone, steroid, phlobatannin, terpenoid, glycoside and reducing sugars. METS was found safe at a dose of 1000 mg/kg body weight. A concentration dependent free radical scavenging effect was observed with methanolic aerial parts extract of Teucrium stocksianum (MAPETS) and methanolic roots extracts of Teucrium stocksianum (MRETS). MAPETS and MRETS have shown highest antioxidant activity 91.72% and 86.19% respectively at 100 μg/ml. MAPETS was found more rich (115.32 mg of GAE/g of dry material) in TPC as compared to MAPETS (105.41 mg of GAE/g). METS demonstrated a dose dependent antinociceptive potential in different pain models, like in acetic acid, formalin and tail immersion showing 83.103%, 80.872% and 67.58% at a dose of 150 mg/kg, similar to acetylsalicylic acid (74.79%, 82.87%, 100 mg/kg) and TramadolR (74%, 30 mg/kg) respectively.. Strong antioxidant potential and high TPCs are residing in the methanolic extract of T. stocksianum. METS showed analgesic potential in all models of nociception implying that both peripheral and central pathways of analgesia are involved. This might be due to the presence of various classes of phytochemicals in the plant extract.

Topics: Analgesics; Animals; Antioxidants; Flavonoids; Male; Methanol; Mice; Models, Animal; Oxidative Stress; Pain; Phenols; Random Allocation; Saponins; Tannins; Teucrium

The analgesic and anti-inflammatory activities of Zea mays husk extract (25, 50, 100, and 200 mg/kg of body weight) were investigated in rats. The hot plate and formalin-induced paw licking models were used to assess analgesic effects of the extract, whereas the carrageenan and cotton pellet models were used for the evaluation of anti-inflammatory activity. The extract at 25, 50, 100, and 200 mg/kg body weight significantly (P < .05) reduced pain stimuli and inflammatory activity when compared with the control group. The reductions in paw licking time and granuloma weight in the formalin and cotton pellet models were both dose dependent. Also, the 200 mg/kg doses of the extract produced higher effects compared with indomethacin (5 mg/kg body of weight) in all the tests. These observations suggest that Z. mays husk extract may have analgesic and anti-inflammatory effects that may be due to its tannins and polyphenolic constituents. These results provide scientific validation for the use of Z. mays husk decoction for the treatment of pain and inflammatory conditions in Nigerian folk medicine.

Topics: Analgesics; Animals; Anti-Inflammatory Agents; Behavior, Animal; Dose-Response Relationship, Drug; Flavonoids; Granuloma; Indomethacin; Inflammation; Male; Medicine, African Traditional; Pain; Phenols; Phytotherapy; Plant Extracts; Plant Leaves; Polyphenols; Rats; Rats, Wistar; Tannins; Zea mays

Gynandropsis gynandra (Capparidaceae) leaves are traditionally used in the treatment of pain. In order to evaluate the scientific validity of this, leaves were extracted successively to produce various extracts. These extracts were screened for antinociceptive activity using the hot plate test and acetic acid-induced writhing test in mice at a dose of 100 mg kg(-1), intraperitoneally. Ethanol and aqueous extracts were found most active in both the tests. The action was blocked by naloxone (1 mg kg(-1), s.c.) in the hot plate test, which suggests involvement of opioid receptors in the action. Flavonoids and tannins were observed in the active extracts, so we can say that they may responsible for the antinociceptive activity.

Topics: Acetic Acid; Analgesics; Animals; Cleome; Flavonoids; Injections, Intraperitoneal; Male; Mice; Naloxone; Pain; Plant Extracts; Plant Leaves; Tannins

Myracrodruon urundeuva Allemão is a plant utilized in Northeast Brazil as an antiinflammatory, wound healing and in gynecological illnesses. The objectives of the present study were to evaluate the antiinflammatory and antiulcer properties of the tannin-enriched fraction (TEF) isolated from the stem bark of M. urundeuva, in the formalin test, in mice, and in carrageenan-induced paw edema and gastric ulcer models, in rats. The results showed that TEF dose-dependently inhibited both phases of the formalin test. However, the effect was predominant in the 2nd phase of the response where inhibitions of 47%, 76% and 85% were observed, with doses of 5, 10 and 50 mg/kg, i.p. In the carrageenan-induced paw edema, significant inhibitions were observed at 3 h (44%) and 4 h (28%), with a dose of 10 mg/kg, i.p. TEF also significantly decreased by 37%, 43% and 57% gastric ulceration induced by indomethacin, at doses of 10, 20 and 50 mg/kg p.o. In the ethanol-induced gastric ulcer model, TEF was less effective, and significant inhibitions (42% to 46%) were observed only with doses of 100 and 200 mg/kg, p.o., respectively. In conclusion, it was shown that TEF presents antiinflammatory and antiulcer effects, partly due to its antioxidant action, known to be present in polyphenols, including tannins.

Topics: Administration, Oral; Anacardiaceae; Animals; Anti-Inflammatory Agents, Non-Steroidal; Anti-Ulcer Agents; Carrageenan; Dose-Response Relationship, Drug; Edema; Female; Formaldehyde; Humans; Injections, Intraperitoneal; Male; Mice; Pain; Phytotherapy; Plant Bark; Plant Extracts; Rats; Stomach Ulcer; Tannins

Topics: Analgesics; Animals; Droperidol; Hot Temperature; Male; Mice; Pain; Sensory Thresholds; Tannins