Nephroprotective effects of Helianthus annuus seeds extract in gentamicin induced nephrotoxic male mice.

Acute kidney injury (AKI) causes a decrease in renal function which leads to failure in balancing electrolyte, fluid and acid-base homoeostasis. AKI is a damaging and life-threatening disorder, but it can be managed if identified earlier. This study aimed to investigate the possible nephroprotective effect of Helianthus annuus seeds extract against gentamicin (GM) induced nephrotoxicity in male mice. The control group (0.5 ml normal saline i.p.,), Gentamycin (GM) group (GM 100 mg/kg i.p), silymarin + GM group (silymarin 50 mg/kg and GM 100 mg/kg i.p.,), H. annuus extract (HAE) and GM, group (HAE 250 mg/kg and GM 100 mg/kg i.p), HAE2 + GM group (HAE2; 500 mg/kg and GM 100 mg/kg i.p) and H. annuus oil (HAO) + GM (HAO 2.5 ml/kg and GM 100 mg/kg i.p). Serum creatinine, urea and blood urea nitrogen (BUN) were significantly (P< 0.001) elevated in the GM group compared to the control group. The elevated level of serum creatinine, urea and BUN were decreased significantly (P<0.001) in groups treated with HAE and HAO extracts compared to the GM group. The kidney histopathological study from the GM group showed tubular necrosis, vacuolation and fibrosis. However, the animal that received HAE and HAO showed no tubular necrosis and vacuolation. Only mild inflammation was observed compared to the GM group. In conclusion, the extract caused marked radical scavenger and protected the kidney from oxidative damage of GM. H. annuus seeds contain strong antioxidant compounds, including flavonoids, phenolic acids, tocopherols and minerals, which could be responsible for the current show.

Alkaloids and Colon Cancer: Molecular Mechanisms and Therapeutic Implications for Cell Cycle Arrest.

Cancer is the second most fatal disease worldwide, with colon cancer being the third most prevalent and fatal form of cancer in several Western countries. The risk of acquisition of resistance to chemotherapy remains a significant hurdle in the management of various types of cancer, especially colon cancer. Therefore, it is essential to develop alternative treatment modalities. Naturally occurring alkaloids have been shown to regulate various mechanistic pathways linked to cell proliferation, cell cycle, and metastasis. This review aims to shed light on the potential of alkaloids as anti-colon-cancer chemotherapy agents that can modulate or arrest the cell cycle. Preclinical investigated alkaloids have shown anti-colon cancer activities and inhibition of cancer cell proliferation via cell cycle arrest at different stages, suggesting that alkaloids may have the potential to act as anticancer molecules.

In vivo antinociceptive and muscle relaxant activity of leaf and bark of Buddleja asiatica L.

The current study was designed to assess the antinociceptive and skeleton muscle relaxant effect of leaves and barks of Buddleja asiatica in animal models. In acetic acid induced writhing test, pretreatment of ethanolic extract of leaves and barks evoked marked dose dependent antinociceptive effect with maximum of 70% and 67% pain relief at 300mg/kg i.p. respectively. In chimney test, the ethanolic extract of leaves and barks evoked maximum of 66.66% and 53.33% muscle relaxant effect after 90min of treatment at 300mg/kg i.p respectively. In traction test, the ethanolic extract of leaves and barks caused maximum of 60% and 73.33% muscle relaxant effect after 90min of treatment at 300mg/kg i.p respectively. In short, both leaves and barks demonstrated profound antinociceptive and skeleton muscle relaxant effects and thus the study provided natural healing agents for the treatment of said disorders.

Antipyretic and antinociceptive potential of extract/fractions of Potentilla evestita and its isolated compound, acacetin.

BACKGROUND: Fever and pain management is a very challenging job for the clinician as the available synthetic agents are causing serious side effects. The present research article deals with the antipyretic and antinociceptive activity of extract/fractions of Potentilla evestita and acacetin isolated from the chloroform fraction of the plant. METHODS: Various chromatographic and spectroscopic techniques were used for the isolation and characterizion of compound. In-vivo yeast induced fibrile mice were used for antipyretic activity while acetic acid induced writhing and formalin tests were used for antinociceptive. RESULTS: The extract/fractions of P. evestita caused marked antipyretic effect during various assessment times in which chloroform was the most prominent followed by ethyl acetate. When acacetin was injected, it produced marked effect with maximum activity of 33.28% and 55.01% at 5 and 10 mg/kg i.p respectively. When studied in acetic acid induced writhing test, the extract/fractions evoked significant antinociceptive effect in which chloroform was the most effective fraction followed by ethyl acetate. Acacetin showed significant antinociceptive effect with 44.77% and 67.03% reduction in abdominal constriction at 5 and 10 mg/kg i.p., respectively. Similarly, it evoked significant dose dependent reduction in noxious stimulation with 42.07% and 64.57% pain attenuation at 5 and 10 mg/kg i.p., respectively in initial phase. In the late phase, it illustrated more dominant effect with 46.32% and 67.29% reduction of painful sensation. CONCLUSIONS: In conclusion, the extract/fractions of P. evestita as well as the isolated compound, acacetin showed strong antipyretic and antinociceptive activity in various animal models possibly mediated through both peripheral and central mechanism.

Antinociceptive and Anti-Inflammatory Like Effects of Berberis baluchistanica.

BACKGROUND: Numerous therapeutic agents are in clinical practice for the treatment of inflammatory and painful conditions, but their applications have been challenged by various side /toxic effects. Therefore, new effective and safe therapies are most warrant, for which medicinal plant could be a significant alternative. Berberis baluchistanica has traditionally been used as analgesic and anti-inflammatory without any scientific background. OBJECTIVE: The current study was designed to evaluate the analgesic and anti-inflammatory like effects of extract B. baluchistanica in animal models. METHODS: For the study of antinociceptive effect, an extractof B. baluchistanica (100, 200 and 300 mg/kg i.p.), was tested in acetic acid-induced writhing and formalin tests. While for the anti-inflammatory action, carrageenan-induced paw edema, cotton pellet induced granuloma and xylene induced ear edema tests were used. RESULTS: The results showed the significant dose-dependent antinociceptive effect of extract of B. baluchistanica in acetic acid-induced writhing and formalin-induced flinching behavior tests. However, the effect was strongly antagonized by the injection of naloxone, suggesting the expression via opioidergic receptors. Similarly, strong anti-inflammatory action was illustrated in carrageenan- induced paw edema, cotton pellet induced granuloma and xylene induced ear edema tests and thus provided evidence for the versatile phytochemical nature of its phytochemical. CONCLUSION: In short, it is concluded that the extract of B. baluchistanica exhibited significant antinociceptive and anti-inflammatory effects in animal models. Further detailed studies on the efficacy and safety as well as on the phytochemical investigation are required to ascertain its clinical uses.

Mechanisms Underlying Anti-hyperalgesic Properties of Kaempferol-3,7- di-O-α-L-rhamnopyranoside Isolated from Dryopteris cycadina.

BACKGROUND: The present study was designed to evaluate the anti-hyperalgesic effect of kaempferol-3,7-di-O-α-L-rhamnopyranoside isolated from the ethyl acetate soluble part of Dryopteris cycadina. Pretreatment of the compound at the doses of 2.5, 5, and 10 mg/kg caused a significant reduction in abdominal constrictions in acetic acid-induced writhing test with maximum effect of 63.03% (P < 0.001) at 10 mg/kg i.p. When subjected in formalin test, it evoked a marked antinociceptive effect in both phases in a dose-dependent manner. The maximum (p < 0.01) pain-inhibiting effects were 61.36% and 65.89% in 1st and 2nd phases at 10 mg/kg i.p., respectively. Administration of atropine (non-selective cholinergic receptor antagonist) significantly (p < 0.05) antagonized the antihyperalgesic effect of the compound, while glibenclamide and naloxone did not alter the induced antinociceptive effect and thus, antinociceptive activity of the compound is mediated, at least in part, through cholinergic system antagonism; independent of calcium channel and opioidergic receptor participation. Furthermore, docking studies underlined strong COX-2 inhibitory activity of the compound. RESULT: Our data concluded that overall analgesic activity of the compound seems to involve COX-2 inhibition and activation of cholinergic receptors. However, further detailed studies are required in this direction to confirm the analgesic effect of the compound for its possible clinical utility.

In vitro attenuation of thermal-induced protein denaturation by aerial parts of Artemisia scoparia.

The goal of this study was to explore the aerial parts of Artemisia scoparia (crude extract, total flavonoid contents, and aqueous fraction) for protein denaturation potential. The crude extract provoked marked attenuation of thermal-induced denatured protein in a concentration-dependent manner with maximum inhibition of 54.05 µg/mL at 500 µg/mL and IC50 of 449.66 µg/mL. When total flavonoid contents were studied, it illustrated most dominant activity concentration dependently with maximum amelioration of 62.16 µg/mL at 500 µg/mL and IC50 of 378.35 µg/mL. The aqueous fraction also exhibited significant activity with maximum of 56.75% inhibition at 500 µg/mL and IC50 of 445.10 µg/mL. It can be concluded on the basis of the results that the crude extract, flavonoid contents, and aqueous fraction of the plant possessed significant inhibition on thermal-induced denatured protein.

Suppression of inflammatory response by chrysin, a flavone isolated from Potentilla evestita Th. Wolf. In silico predictive study on its mechanistic effect.

Flavonoids are the most abundant natural polyphenols widely distributed in plants. Among them, chrysin has recently attracted the attention for its anti-tumor and anti-oxidant activities and also for its protective effects on allergic inflammation. Therefore, in this study, we set out to investigate and characterize the effects of chrysin in classical models of inflammation reasoning that this would expand our knowledge on the pharmacological properties of this flavone. To this aim we have firstly isolated chrysin from Potentilla evestita Th. Wolf. and successively evaluated its anti-inflammatory and analgesic potential on writhing and formalin test and also on carrageenan-induced paw oedema. Finally, the present study was planned to investigate, by the aim of docking analysis, the molecular interaction of this compound on the binding site of COX-1 and COX-2 enzymes. On writhing test, we observed a significant inhibition of writhings after the administration of chrysin at 5.0 and 10.0 mg/kg i.p. (25.00±9.22% and 55.67±7.62% respectively). On formalin test, the flavone at dose of 10.0 mg/kg i.p. displayed its maximum analgesic and anti-inflammatory effect on both early (35.67±7.88%) and late phase (50.57±5.36%) and similarly displayed at 4h a significant anti-inflammatory effect in carrageenan-induced paw oedema. Moreover, in silico analysis of receptor ligand complex shows that chrysin interacts weakly with COX-1 binding site whereas displayed a remarkable interaction with COX-2. These findings suggest that the flavone chrysin isolated from P. evestita Th. Wolf. possesses in vivo anti-inflammatory and anti-nociceptive potential, which are supported in silico by an interaction with COX-2 binding site.

In vivo antinociceptive and anti-inflammatory activities of umbelliferone isolated from Potentilla evestita.

This study was designed to evaluate the antinociceptive and anti-inflammatory activities of a compound, umbelliferone, isolated from the chloroform fraction of Potentilla evestita in animal models. When tested against acetic acid-induced noxious stimulus, it significantly prolonged pain threshold and provided 38.38% and 60.95% reduction in abdominal constriction at 5 and 10 mg/kg i.p., respectively. Post-umbelliferone injection evoked significant dose-dependent reduction in noxious stimulation with 33.65% and 58.89% pain attenuation at 5 and 10 mg/kg i.p., respectively, in the initial phase. In the late phase, it illustrated more dominant effect with 37.65% and 63.79% blockade of painful sensation. Similarly, it exhibited significant anti-inflammatory activity during various assessment times (1-5 h) with 46.28% and 66.13% amelioration after 4th of administration against induced oedema. In conclusion, umbelliferone possessed strong antinociceptive and anti-inflammatory activities by inhibiting both peripheral and centrally acting pain mediators.

Antipyretic activity of decoction of Joshanda and its saponin and sterol contents: validation in an animal-based model.

Joshanda is a polyherbal product that is commonly used in the treatment of cold and flu usually accompanied by fever. The present study was designed to scrutinize the antipyretic activity of a decoction of Joshanda and its total saponin and sterol contents in brewer's yeast induced febrile mice. The results revealed marked attenuation of induced pyrexia by the decoction and its saponin contents during various assessment times (1-5 hours) in a dose-dependent manner, which were not supported by sterol contents. The maximum antihyperthermic effect of the decoction and saponin contents were 75.38% and 81.32%, respectively, at 300 mg/kg i.p. This findings suggested that Joshanda extracts strongly ameliorated induced pyrexia and thus validated it as a useful household remedy for cold and flu accompanied by fever.