: The extracts and the compounds isolated from Phyllanthus amarus Schumm and Thonn (Family: Euphorbiaceae) have shown a wide spectrum of pharmacological activities including antiviral, antibacterial, antiplasmodial, antimalarial, antimicrobial, anticancer, antidiabetic, hypolipidemic, antioxidant, hepatoprotective, nephroprotective and diurectic properties. Background: This investigation was aimed at exploring the anxiolytic potential of Phyllanthus amarus standardized extracts and predict probable role of marker phyto constitutents. Objective and Methods: Three standardized extracts of Phyllanthus amarus plant viz. standardized aqueous extract of Phyllanthus amarus whole plant (PAAE), standardized methanolic extract of P. amarus leaf (PAME) and the standardized hydro-methanolic extract of P. amarus leaf (PAHME) were tested in the classical animal models of anxiety: Elevated plus-maze model and Light & Dark Exploration test. Results: The lower doses of the tannin rich extract (PAHME) of the P. amarus possess significant anxiolytic activity compared to lignin rich (PAME) and aqueous extracts (PAAE), while at a higher dose (400mg/kg) the results of all three extracts appears to be potentially sedative. While the molecular docking studies support these probable anxiolytic, the sedative effects of the Phyllanthus amarus extracts could be due to the interaction of tannins and lignans with the GABAbenzodiazepine receptor complex. Conclusion: The results of the present study indicate that the tannin-rich extract of the P. amarus may have potential clinical applications in the management of anxiety. It can be further studied for optimum dosage to be used as a future of anti-anxiety drug development or as a standardized Phytomedicine.
Context:Alocasia indica Schott (Araceae) is used in several regions of India, especially in rural communities, by traditional medicine practitioners to treat diarrhea. However, no scientific data are available to justify the traditional potentials of the plant species in gastrointestinal disorders. Objective: To evaluate the antidiarrheal and in vitro antiprotozoal activities of extracts of leaves of Alocasia indica using various pharmacological models. Materials and methods:In vitro antidiarrheal activity of aqueous and ethanol extracts of Alocasia indica was evaluated against Escherichia coli, Salmonella typhimurium, Shigella flexneri and Staphylococcus aureus by agar well diffusion method. In vivo antidiarrheal activity of the extracts was studied against recinolic acid-induced diarrhea and magnesium sulfate-induced diarrhea. The effect of the extracts on normal intestinal transit, recinolic acid-induced intestinal transit, recinolic acid-induced intestinal fluid accumulation (enteropooling) and gastric emptying was assessed. In vitro antiprotozoal activity of aqueous and ethanol extracts of Alocasia indica was studied against Entamoeba histolytica and Giardia intestinalis. Results: The aqueous and ethanol extracts exhibited significant in vitro antidiarrheal activity compared to the standard drug ciprofloxacine (10 µg/mL). The plant extracts showed significant (P <0.05) and dose-dependent antidiarrheal activity comparable to that of the reference drug, loperamide (10 mg/kg). The plant extracts exhibited significant in vitro antiprotozoal activity against both protozoa compared to the standard amebicidal and giardicidal drugs, metronidazole and emetine. Discussion and conclusion: The results showed that the extracts of Alocasia indica have significant antidiarrheal and in vitro antiprotozoal activities which support its use in traditional herbal medicine practice.
11 November 2020 in Natural Products and Bioprospecting
Anxiety is an unpleasant state, which can critically decrease the quality of life is often accompanied by nervous behaviour and rumination. Niranthin is a lignan isolated from various Phyllanthus sources. The literature survey on niranthin highlights wide ranges of the therapeutic potentials. In a present study, based on our previous investigations, we evaluated pure, isolated and characterized niranthin as an anxiolytic agent. The niranthin [6-[(2R,3R)-3-[(3,4-dimethoxyphenyl)methyl]-4-methoxy-2-(methoxymethyl)butyl]-4-methoxy-1,3-benzodioxole] was purchased from commercial source and further subjected for assessment of its anxiolytic potentials using popular animal models including Elevated plus-maze model/test (EPM) and Light & Dark Exploration test (L&D). GABA-A receptor mediation was evaluated by pretreating the mice with the GABA-A receptor antagonist Flumazenil before the EPM task. Molecular docking simulation studies (pdb id: 4COF) carried out by Vlife QSAR software showed that niranthin (docking score: − 62.1714 kcal/mol) have shown comparatively best docking score compared to the standard drug Diazepam (docking score: − 63.1568 kcal/mol). To conclude, Niranthin has probable potential in the management of anxiety disorder. Our in-silico and in-vivo analysis (indirectly) indicated the plausible role of GABA mediation for anxiolytic activity. Although, these studies are preliminary, future in depth experimental explorations will be required to use Niranthin as anti-anxiety drug in near future.
Background: The standardized extracts of P. fraternus were previously reported by us for its anti-inflammatory, analgesic, and anti-arthritic biological potentials. However, we have not reported for a consequence of P. fraternus on chronic inflammatory muscle hyperalgesia. Herein, we have demonstrated chronic pain modulating effect of standardized extracts of P. fraternus. Materials and Methods: Firstly, we have collected various parts of P. fraternus plant including the dried stems, leaves, and roots. In order to produce chronic inflammations, we further allowed injection to the left gastrocnemius muscle belly of rats with a freshly prepared solution of 3% carrageenan in normal saline (100µL). Thermal/heat hyperalgesia, mechanical hyperalgesia and muscle circumferences were determined in the current experimental model. In order to estimate, chronic pain modulating potential of P. fraternus, we have also studied histopathological studies and measurement of prostaglandin E-2 (PGE2). Results: After administration of 3% carrageenan intramuscular injection, we investigated the chronic thermal and mechanical hypersensitivity of aforementioned test sample i.e. standardized extracts of P. fraternus in terms of adopting 2 gradual dosings of 200 and 400 mg/kg (administered intraperitoneally) from day 14th to 22nd. From our study, we observed significant antihyperalgesic activity; when we allowed administering standardized extracts of P. fraternus intraperitoneally. Conclusion: To conclude, we have investigated the antihyperalgesic and anti-inflammatory potentials of standardized extracts of P. fraternus. These effects might be having mediation via supraspinal or spinal neuronal mechanisms, and mainly observed due to evidence of PGE2 inhibitions.
1 May 2022 in Recent Advances in Inflammation & Allergy Drug Discovery
The main objectives of the present work are to determine the clinical effect of niranthin on visceral or somatic inflammatory pain. The study was performed to determine the effects of niranthin on visceral or somatic inflammatory hypersensitivity of adult Swiss albino mice by using complete Freund’s adjuvant (CFA) induced pain model. The effect of CFA injection was determined after 24 hours of injection by using an aesthesiometer such as Von Frey filaments to evaluate tactile acetone-evoked cooling and thermal sensitivity. We used a digital Plethysmometer to measure paw edema. Single dose of niranthin intraperitoneal injection (5 and 10 mg/kg) was injected into mice having CFA-induced mechanical hypersensitivity and after 30 minutes of administration, reduced mechanical hypersensitivity was observed. In addition, niranthin also reduced acetone- evoked hypersensitivity within 4 hours. Compared to DMSO, niranthin was most highly active to reduce CFA-induced paw edema. To reduce mechanical hypersensitivity, multiple doses of niranthin (bis in die (b.i.d.)) from 1st - 5th day and b.i.d. day 9th and 10th) were given and remarkable results were observed such as did not cause tolerance in multiple dosing and significantly reduced in CFA induced hypersensitivity. This work reported niranthin having antinociceptive activity and indicated that niranthin is conventionally active in the management of persistent pain.
Fibromyalgia is a chronic disorder marked by widespread musculoskeletal pain and increased sensitivity to stimuli. The acid-sensing ion channel 3 (ASIC3) is believed to play a key role in its pathogenesis, making it a potential therapeutic target. Artemisinin, a natural compound from Artemisia annua, has shown promise as a pain modulator. This study examined Artemisinin’s effect on ASIC3 using both in vivo and in silico approaches in a rat model of fibromyalgia. Fibromyalgia-like symptoms were induced in rats, and pain behaviors were assessed. Artemisinin was then administered to evaluate its impact on pain sensitivity. Results showed a significant reduction in pain responses following reduction in pain responses following Artemisinin treatment. In parallel, molecular docking studies revealed that Artemisinin binds to specific regions of ASIC3, potentially affecting its function. Furthermore, analysis suggests that Artemisinin may downregulate ASIC3 expression, providing a potential mechanism for its analgesic effect. These findings indicate that Artemisinin modulates ASIC3 activity and reduces pain sensitivity in fibromyalgia, offering a promising therapeutic avenue. Both behavioral and molecular data support this interaction, highlighting the potential of Artemisinin in fibromyalgia management. Further studies are needed to fully understand its mechanism and to validate its clinical applicability in human fibromyalgia treatment.