scholarly journals Aktivitas Analgetik Ekstrak dan Fraksi-fraksi Akar Pakis Tangkur (Polypodium feei., METT) Dari Gunung Talaga Bodas Secara In Vivo

2021 ◽  
Vol 8 (1) ◽  
pp. 52
Author(s):  
Deden Winda Suwandi ◽  
Tina Rostinawati ◽  
Muchtaridi Muchtaridi ◽  
Anas Subarnas
Keyword(s):  
Hot Plate

<p>Pakis tangkur merupakan tanaman obat tradisional yang sering dimanfaatkan oleh masyarakat untuk mengobati penyakit reumatik. Tanaman ini tumbuh di area pegunungan talaga bodas, Garut. Penelitian sebelumnya, melaporkan bahwa senyawa Shellegueain A yang terkandung dalam akar pakis tangkur yang berasal dari pegunungan Tangkuban Perahu efektif sebagai analgetik. Namun, dalam bentuk sediaan ekstrak yang secara umum merupakan sediaan yang paling banyak digunakan secara tradisional oleh masyarakat belum dilaporkan. Penelitian ini bertujuan untuk mengetahui aktivitas analgetik ekstrak etanol dosis 100, 200 dan 400 mg/kg serta fraksi n-heksan, etil asetat dan air dosis 50, 100 dan 200 mg/kg dengan metode geliat (siegmund) dan metode panas (hot plate). Hasilnya menunjukkan bahwa ekstrak etanol menghasilkan jumlah geliat hewan sebesar 85,5; 68,45 dan 77,35 kali dengan nilai persen proteksi 71,78; 77,4 dan 74,5 %. Sediaan fraksi n-heksan sebesar 90,45; 78,7 dan 85,95 kali (nilai persen proteksi 70,14; 74,03 dan 71,63 %); fraksi etil asetat sebesar 58,5; 102,5 dan 55,5 kali (nilai persen proteksi 80,05; 66,17 dan 79,68 %) serta fraksi air sebesar 205,2; 65,2 dan 60,5 kali (nilai persen proteksi sebesar 32,28; 78,48 dan 80,03 %). Aktivitas analgetik kuat hanya ditunjukkan oleh fraksi etil asetat dengan lama waktu respon 136,5; 147,5 dan 128,75 detik (nilai persen peningkatan 59,01; 55,4 dan 74,3 %) serta fraksi air sebesar 153; 144,75 dan 146 detik (persen peningkatan 57,39; 66,77 dan 71,47 %). Fraksi yang terbaik sebagai obat pereda nyeri adalah fraksi etil asetat terutama dosis 200 mg/kgbb.   </p>

Synthesis of 8-alkoxy-1,3-dimethyl-2, 6-dioxopurin-7-yl-substituted acetohydrazides and butanehydrazides as analgesic and anti-inflammatory agents

2015 ◽  
Vol 21 (5) ◽  
pp. 273-278 ◽  
Author(s):  
Grażyna Chłoń-Rzepa ◽  
Agnieszka W. Jankowska ◽  
Małgorzata Zygmunt ◽  
Krzysztof Pociecha ◽  
Elżbieta Wyska
Keyword(s):  
Analgesic Activity ◽  
Structural Element ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Peripheral Mechanism ◽  
Anti Inflammatory ◽  
Factor Α ◽  
Necrosis Factor ◽  
Inhibit Tumor Necrosis Factor

AbstractA series of new 8-alkoxy-1,3-dimethyl-2,6-dioxopurin-7-yl-substituted acetohydrazides and butanehydrazides 6–12 was synthesized and evaluated for the analgesic activity in two in vivo models: the writhing syndrome and the hot-plate tests. Among the investigated derivatives, compounds with N′-arylidenehydrazide moiety 9–12 show analgesic activity significantly higher than that of acetylsalicylic acid, which may indicate the importance of this structural element for analgesic properties. The lack of the activity in the hot-plate test may suggest that the analgesic activity of the newly synthesized compounds is mediated by a peripheral mechanism. The selected compounds 7 and 12 inhibit tumor necrosis factor α production in a rat model of lipopolysaccharide-induced endotoxemia, similarly to theophylline, which may confirm their anti-inflammatory properties.

scholarly journals Analgesic Effects of Vigna unguiculata subsepecies dekindtiana in Mice

2020 ◽  
pp. 10-22
Author(s):  
Adekunle T. Adegbuyi ◽  
Moses A. Akanmu ◽  
G. Olayiwola ◽  
Abayomi O. Sijuade
Keyword(s):  
Acetic Acid ◽  
Receptor Antagonist ◽  
Vigna Unguiculata ◽  
Analgesic Effect ◽  
Methanol Extract ◽  
Positive Control ◽  
Hot Plate ◽  
Thermal Tests ◽  
Writhing Test

In the present study, we investigated the antinociceptive effects of the plant Vigna unguiculata spp dekindtiana using chemical and thermal tests in mice. The peripheral and the central analgesic activities of the methanol extract and its fractions were investigated in-vivo in albino mice using acetic acid induced-writhing test and hot plate models respectively. The result of the central analgesic effect showed that the methanol extract (VUME) at 400 mg/kg produced a significant (p<0.05) delay in reaction time in mice on hot plate compared to the control. Various fractions of the extract showed more potency compared to the crude extract. In acetic writhing model, the extract and the fractions demonstrated dose dependent reduction in writhing reaction induced by acetic acid in mice. The reduction was significant when compared to control which was suggestive of the analgesic effect of the plant. It was also seen that the extract and fractions showed an improved analgesic effect compared to diclofenac used as positive control in this model. Yohimbine (alpha adrenergic receptor antagonist) and cyproheptadine (serotonergic receptor antagonist) reversed the antinociceptic effect of the fractions in the hot plate model demonstrating the possibility of adrenergic and serotonergic involvement in eliciting the analgesic effect. Naloxone on the other hand, caused a reversal only in the butanol fraction meaning that this fraction may contain active principles that may mediate their analgesic effect through the opioid mechanism. In the writhing test, yohimbine abolished the analgesic effect of both hexane and butanol fractions. This may therefore, suggest that the analgesic effect of these fractions may be mediated through adrenergic pathway. In conclusion, the plant V. unguiculata subspecies dekindtiana possesses active principles with potential analgesic activity, establishing the folkloric use of the plant in managing pain.

scholarly journals Enrichment of Eucalyptus oil nanoemulsion by micellar nanotechnology: transdermal analgesic activity using hot plate test in rats’ assay

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Zarith Asyikin Abdul Aziz ◽  
Hasmida Mohd Nasir ◽  
Akil Ahmad ◽  
Siti Hamidah Mohd Setapar ◽  
Hafandi Ahmad ◽  
...  
Keyword(s):  
Particle Size ◽  
Analgesic Activity ◽  
Eucalyptus Globulus ◽  
Ph Value ◽  
Activity Assay ◽  
Hot Plate ◽  
Spontaneous Emulsification ◽  
Grape Seed Oil ◽  
Tween 40

Abstract Eucalyptus globulus is an aromatic medicinal plant which known for its 1,8-cineole main pharmacological constituent exhibits as natural analgesic agent. Eucalyptus globulus-loaded micellar nanoparticle was developed via spontaneous emulsification technique and further evaluation for its analgesic efficacy study, in vivo analgesic activity assay in rats. The nanoemulsion system containing Eucalyptus-micelles was optimized at different surfactant types (Tween 40, 60 and 80) and concentrations (3.0, 6.0, 9.0, 12.0, 15.0, and 18.0 wt. %). These formulations were characterized by thermodynamically stability, viscosity, micelles particle size, pH, and morphology structure. The spontaneous emulsification technique offered a greener micelles formation in nanoemulsion system by slowly titrated of organic phase, containing Eucalyptus globulus (active compound), grape seed oil (carrier oil) and hydrophilic surfactant into aqueous phase, and continuously stirred for 30 min to form a homogeneity solution. The characterizations evaluation revealed an optimized formulation with Tween 40 surfactant type at 9.0 wt. % of surfactant concentration promoted the most thermodynamic stability, smaller micelles particle size (d = 17.13 ± 0.035 nm) formed with spherical shape morphological structure, and suitable in viscosity (≈2.3 cP) and pH value (6.57) for transdermal purpose. The in vivo analgesic activity assay of optimized emulsion showed that the transdermal administration of micellar nanoparticle of Eucalyptus globulus on fore and hind limb of rats, possessed the central and peripheral analgesic effects by prolonged the rats pain responses towards the heat stimulus after being put on top of hot plate (55 °C), with longest time responses, 40.75 s at 60 min after treatment administration. Thus, this study demonstrated that micellar nanoparticle of Eucalyptus globulus formed in nanoemulsion system could be promising as an efficient transdermal nanocarrier for the analgesic therapy alternative.

scholarly journals In vivo and in silico evaluation of analgesic activity of Lippia alba

2019 ◽  
Vol 5 (1) ◽  
Author(s):  
Md. Abdullah Aziz ◽  
Manna Mehedi ◽  
Mst. Irin Akter ◽  
Sadiur Rahman Sajon ◽  
Kishor Mazumder ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Analgesic Activity ◽  
In Silico ◽  
Cyclooxygenase 2 ◽  
Latency Time ◽  
Hot Plate ◽  
Standard Drug ◽  
Lippia Alba ◽  
Tail Immersion

Abstract Background This study was conducted to evaluate the analgesic activity of different extracts of Lippia alba (L. alba) along with in silico evaluation of analgesic activity of the isolated compounds from L. alba against cyclooxygenase-2 enzyme and ADME/T analysis of isolated compounds. Method In vivo analgesic activity of different extracts of L. alba was evaluated by acetic acid-induced writhing, tail immersion and hot plate on Swiss albino mice of either sex. In silico activity of the isolated compounds and ADME/T analysis were performed by Schrödinger-Maestro (Version 10.1) and OSIRIS Data warrior (version 4.6.1) softwares. Results Three different extracts (Methanolic extract: ME; Petroleum ether extract: PEE; Dichloromethane extract: DCME) of 250 mg/kg and 500 mg/kg doses were used in the experiments to evaluate analgesic activity. In acetic acid-induced writhing test, significant results were seen for PEE (500 mg/kg) and DCME (500 mg/kg), which were 53.09 ± 2.87 & 50.09 ± 4.24%, respectively. In tail immersion test, the best latency time was found at + 60 min for PEE (500 mg/kg) which is (5.65 ± 0.25) sec. For hot plate test, DCME at a dose 500 mg/kg showed the highest increase in latency time, which was 13.48 ± 0.33 s. In the case of in silico evaluation of analgesic activity, the compounds such as geranial, neral, (E)-caryophyllene, caryophyllene oxide, mussaenide, and 8-epi-loganin meet the condition of Lipinski’s rule of five. Among these safe compounds, 8-epi-loganin showed the best docking score of − 8.17 kcal/mol against cyclooxygenase-2 enzyme (PDB ID: 6COX), which was almost similar to that of the standard drug, Celecoxib (− 11.11 kcal/mol). Conclusion In conclusion, L. alba can be a potent source of analgesic medicine and further modification and simulation studies are required to establish the effectiveness of 8-epi-loganin.

scholarly journals Antioxidant, Anti-Inflammatory, and Analgesic Activities ofAgrimonia eupatoriaL. Infusion

2017 ◽  
Vol 2017 ◽  
pp. 1-13 ◽  
Author(s):  
Telmo N. Santos ◽  
Gustavo Costa ◽  
J. Pinto Ferreira ◽  
Joana Liberal ◽  
Vera Francisco ◽  
...  
Keyword(s):  
Antiradical Activity ◽  
Inflammatory Activity ◽  
No Production ◽  
Hot Plate ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
First Time

Agrimony (Agrimonia eupatoriaL.) (Ae) is used in traditional medicine to treat inflammatory and oxidative related diseases. Therefore, this study focuses on the anti-inflammatory and analgesic potential of Ae infusion (AeI). Phenolic compounds characterization was achieved by HPLC-PDA-ESI/MSn. To evaluate antioxidant potential, 2,2-diphenyl-1-picrylhydrazyl (DPPH), superoxide anion, hydroxyl radical, and SNAP assays were used. In vitro anti-inflammatory activity of AeI was investigated in LPS-stimulated macrophages by measuring the NO production. In vivo anti-inflammatory activity was validated using the mouse carrageenan-induced paw edema model. Peripheral and central analgesic potential was evaluated using the acetic acid-induced writhing and hot-plate tests, respectively, as well as the formalin assay to assess both activities. The safety profile was disclosed in vitro and in vivo, using MTT and hematoxylin assays, respectively. Vitexin, quercetinO-galloyl-hexoside, and kaempferolO-acetyl-hexosyl-rhamnoside were referred to in this species for the first time. AeI and mainly AePF (Ae polyphenolic fraction) showed a significant antiradical activity against all tested radicals. Both AeI and AePF decreased NO levels in vitro, AePF being more active than AeI. In vivo anti-inflammatory and analgesic activities were verified for both samples at concentrations devoid of toxicity. Agrimony infusion and, mainly, AePF are potential sources of antiradical and anti-inflammatory polyphenols.

scholarly journals Analgesic and Anti-Inflammatory Activities of Resveratrol through Classic Models in Mice and Rats

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Guangxi Wang ◽  
Zhiqiang Hu ◽  
Xu Song ◽  
Qiankun Cui ◽  
Qiuting Fu ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Biological Activities ◽  
Drug Candidate ◽  
Hot Plate ◽  
Sod Activity ◽  
Analgesic Effects ◽  
Mouse Ear ◽  
Anti Inflammatory ◽  
Ear Oedema

Background. Inflammation and pain are closely related to humans’ and animals’ health.Resveratrol(RSV) is a natural compound with various biological activities. The current study is aimed to evaluate the analgesic and anti-inflammatory activities of RSV in vivo. Materials and Methods. The analgesic effects were assessed by the acetic acid-induced writhing and hot plate tests. The anti-inflammatory effects were determined using the xylene-induced mouse ear oedema, the acetic acid-induced rat pleurisy, and carrageenan-induced rat synovitis tests, respectively.Results. The analgesic results showed that RSV could significantly inhibit the number of writhes and improve the time and pain threshold of mice standing on hot plate. The anti-inflammatory results showed that RSV could inhibit the ear oedema of mice. In acetic acid-induced pleurisy test, RSV could significantly inhibit the WBC and pleurisy exudates, could decrease the production of NO, and elevate the activity of SOD in serum. In carrageenan-induced synovitis test, RSV could reduce the content of MDA and elevate the T-SOD activity in serum; RSV could inhibit the expressions of TP, PGE2, NO, and MDA.Conclusion. Shortly, these results indicated that RSV had potent analgesic and anti-inflammatory activities and could be a potential new drug candidate for the treatment of inflammation and pain.

scholarly journals OPTIMASI EFEK ANALGESIK DAUN BINAHONG DENGAN PENAMBAHAN JAHE DAN KUNYIT SECARA IN VIVO

2019 ◽  
Vol 9 (2) ◽  
pp. 144-151
Author(s):  
Lusi Indriani ◽  
Oktaviana Zunnita ◽  
Muhammad Raifal Khairi
Keyword(s):  
Hot Plate

Penelitian menunjukkan daun binahong (Anredera cordifolia (Ten.) Steenis) dapat dimanfaatkan sebagai analgesik. Ekstrak etanol 70% daun binahong mempunyai daya analgesik sebesar 48,06% pada dosis 1g/kgBB dan 69,33% pada dosis 4g/kgBB pada mencit putih jantan. Jahe dan kunyit sudah terbukti berkhasiat sebagai analgesik. Penelitian ini bertujuan mengoptimasi efek analgesik ekstrak daun binahong dengan penambahan ekstrak jahe dan kunyit pada mencit putih jantan. Mencit putih dibagi menjadi 6 kelompok perlakuan yaitu kelompok dosis 1 (binahong dosis tunggal 20mg/20gBB), dosis 2 binahong:jahe:kunyit (20:1:3,5mg/20gBB), dosis 3 (10:2:3,5mg/20gBB), dosis 4 (10:1:7mg/20gBB), kontrol positif (Natrium diklofenak 0,182mg/20gBB) dan kontrol negatif (CMC Na 0,5%). Efek analgesik diuji menggunakan metode induksi nyeri dengan rangsangan panas. Semua mencit diuji pendahuluan dengan menempatkan mencit di atas hot plate bersuhu 55°C. Parameter yang diamati adalah respon mencit mengangkat kaki belakang atau melompat. Selanjutnya diberikan larutan uji secara oral sesuai dengan dosis yang telah ditentukan. Pengamatan dilakukan pada menit ke- 0, 10, 20, 30, 40, 50 dan 60 setelah pemberian dosis perlakuan. Hasil penelitian menunjukkan bahwa kelompok dosis kombinasi binahong-jahe-kunyit menunjukkan efek analgesik lebih baik dibanding binahong dosis tunggal, dengan daya analgesik lebih dari 50%. Daya analgesik paling tinggi ditunjukkan oleh dosis 4 yaitu kombinasi ekstrak binahong-jahe-kunyit (10 mg/20gBB: 1mg/20gBB:7mg/20gBB) yaitu sebesar 130,87% yang setara dengan Na diklofenak (137,50%).

scholarly journals In vivo Analgesic activity of methanolic extract of Helianthus annuus seeds

2016 ◽  
Vol 5 (4) ◽  
pp. 38-40 ◽  
Author(s):  
Rubab Tarannum Islam ◽  
Ahmed Tanjimul Islam ◽  
Mir Monir Hossain ◽  
Kishor Mazumder
Keyword(s):  
Body Weight ◽  
Acetic Acid ◽  
Helianthus Annuus ◽  
Analgesic Activity ◽  
Latency Period ◽  
Pharmaceutical Journal ◽  
Mice Model ◽  
Hot Plate ◽  
Writhing Test

The sunflower seed is the seed of the sunflower (Helianthus annuus). The methanol extract of seeds of Helianthus annuus were screened for analgesic activity in mice model to systematically explore the medicinal values of the plant. Acetic acid induced writhing and hot plate methods were used to confirm the central and peripheral analgesic action. In case of acetic acid-induced writhing test the extract showed significant (P <0.05) analgesic potential at doses 100 and 200 mg/kg body weight (50.35 and 57.85% inhibition, respectively). In the hot plate method, increase (p < 0.05) of latency period was also observed in comparison to standard aspirin. At 60 minutes, the latency period of two different doses (100 and 200 mg/kg body weight) was found at 13 ± 0.91 and 16.5 ± 1.55 second. The results obtained support the use of Helianthus annuus seeds in painful conditions acting both centrally and peripherally.Islam et al., International Current Pharmaceutical Journal, March 2016, 5(4): 38-40http://www.icpjonline.com/documents/Vol5Issue4/02.pdf

scholarly journals Antioxidant, Anti-Inflammatory, and Analgesic Activities of Aqueous Extract of Diploknema butyracea (Roxb.) H.J. Lam Bark

2020 ◽  
Vol 2020 ◽  
pp. 1-6
Author(s):  
Sumit Bahadur Baruwal Chhetri ◽  
Deepa Khatri ◽  
Kalpana Parajuli
Keyword(s):  
Antioxidant Activity ◽  
Phenolic Content ◽  
Radical Scavenging ◽  
Total Phenolic ◽  
Paw Edema ◽  
Hot Plate ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Radical Scavenging Assay

Diploknema butyracea (Roxb.) H.J. Lam is a multipurpose tree used by the Nepalese indigenous people for medicinal purposes such as rheumatism, asthma, and ulcer and other purposes such as cooking and lighting. However, there is no scientific evidence for the medicinal uses of this plant. The present study aimed to explore the phytochemical constituents, estimate the total phenolic content, evaluate antioxidant activity, and investigate the in vivo anti-inflammatory and analgesic activities of aqueous extract of Diploknema butyracea (Roxb.) H.J. Lam bark (ADBB). Phytochemical screening was performed using standard methods. The total phenolic content was determined using the Folin–Ciocalteu method. The in vitro antioxidant activity was determined using 2, 2-diphenyl-1-picrylhydrazyl radical scavenging assay and nitric oxide radical scavenging assay. For the in vivo studies, the plant extract was given in three different doses (50, 100, and 200 mg/kg body weight) to male albino Wistar rats. Anti-inflammatory and analgesic studies were carried out using the carrageenan-induced rat paw edema and the hot plate method, respectively. Results revealed the presence of different phytoconstituents such as flavonoids, tannins, glycosides, terpenoids, and carbohydrates together with a considerable amount of phenolic compounds. Antioxidant assays indicated the potent antioxidant activity of the plant extracts. The higher dose of D. butyracea (200 mg/kg) exhibited a maximum and significant inhibition (53.20%) of rat hind paw edema volume at 4 h and showed a greater increment in latency time (12.15 ± 1.81 sec) in the hot plate test at 120 min. The present study demonstrated the antioxidant, anti-inflammatory, and analgesic potential of ADBB, which supports its traditional medicinal use.

scholarly journals Synthesis and anаlgеsic activity 5-methyl-3-aryl[1,2,4]triazolo[4,3-a]pyrimidin-7-oles derivatives

2018 ◽  
pp. 55-61
Author(s):  
A. G. Ogorodnik ◽  
V. A. Yanchenko ◽  
L. S. Bobkova ◽  
N. M. Seredinska ◽  
A. M. Demchenko
Keyword(s):  
Analgesic Activity ◽  
1H Nmr Spectroscopy ◽  
The Body ◽  
Aryl Substituent ◽  
Hot Plate ◽  
Methyl Group ◽  
Structure Activity ◽  
Subsequent Cyclization ◽  
Fourth Position

Pain is a signal of inflammation and disruption of the body. It is the most important protective and adaptive mechanism that ensuring the safety of the individual. A strong and prolonged effect of "pain" irritant arising in injuries or after surgical manipulation transforms the protective reaction of the body to harmful factor that is the cause of secondary violations physiological processes. The aim of this work was the synthesis of substances in a series of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidine-7-ol and study the analgesic effect of the synthesized compounds. The objects of our research were selected derivatives of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidine-7-ol, which were synthesized by condensation and subsequent cyclization of 6-methyl-2-metylsulfanilpirymidyn-4-ol (1) with the corresponding substituted benzoic acid hydrazide The primary evaluation of analgesic activity conducted on thermal  stimulation models («hot plate»). A number of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol derivatives were synthesized, and their structure and purity were confirmed by 1H NMR spectroscopy. The analgesic activity of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol was investigated in order to reveal the structure-activity relationship. The screening for analgesic activity for 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol derivatives in in vivo experiments on hot plate models showed that the highest activity Was noted for the compound containing the methyl group in the fourth position of the aryl substituent, which is 184.28% of the change in the latent period of the reaction, which exceeds the action of the reference preparation of ketorolac by 71.57%. The introduction of halogens into the aryl moiety leads to a decrease in the analgesic activity of the compounds. A series of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidine-7-ol derivatives were synthesized by condensation and subsequent cyclization of 6-methyl-2-metylsulfanylpirymydyn-4-ol with relevant substituted hydrazide of benzoic acid. The structure and purity of obtained compounds were confirmed by 1H NMR spectroscopy. The analgesic activity of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol was investigated in order to reveal the structure-activity relationship. The screening of analgesic activity of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pirymidyn-7-ol derivatives in vivo models for «hot plate» shows that the highest activity was noted for compound containing methyl group in the fourth position of the aryl substituent, which is 184.28% change latent period reaction, that exceeds effect reference drug ketorolac at 71.57%. The introduction of halogens in the aryl fragment leads to a decrease analgesic activity of compounds.

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