Pharmacognostical Standardization, Isolation of Phytoconstituents (β-sitosterol), HPTLC analysis of extracts of Operculina turpethum (Linn.) roots and evaluation of cytotoxic, in vitro & in vivo anti-inflammatory activities

2021 ◽  
Vol 18 ◽  
Author(s):  
Akash Ved ◽  
Shweta Gupta ◽  
Namrata Singh ◽  
Karuna S. Shukla ◽  
Om Prakash ◽  
...  

Background: Operculina turpethum (Linn.) Silva Manso, family- convolvulaceae, is an important plant in Indian conventional system of medicine which is extensively employed by different tribes in many countries to cure edema and painful conditions like arthritis, back pain; hyperlipidemia, diabetes mellitus, liver disorders, skin disorders and to regulate bowel functions. Objective: The roots of O. turpethum (Linn.) was subjected to physicochemical, phytochemical standardization, the chromatographic separation which was accomplished by column chromatography, TLC, and HPTLC, further, the acute toxicity, cytotoxic and anti-inflammatory activities of Operculina turpethum roots were estimated by in vivo and in vitro models. Materials and Methods: This study includes percentage yield of extraction, organoleptic evaluation along with the analysis of its physicochemical investigations & preliminary phytochemical estimation. The isolation of active phytoconstituents was done by column chromatography, and the isolated compound was then exposed to TLC and HPTLC analysis. Cytotoxic activity was tested by WST-1 based cell viability assay on HepG2 cells. Anti-inflammatory activity of methanol extract (ME) was evaluated against inflammation occur by both in vitro and in vivo method. Results: The methanolic extract exhibited the presence of most of the phytoconstituents out of all the extracts, the phytoconstituent phytosterol, i.e., β-sitosterol was isolated by column chromatography, identified and quantified by TLC and HPTLC, which is liable for anti-inflammatory activity. The amount of β-sitosterol was estimated to be 14.09 µg in 10.00 mg fraction of MEOT. MEOT is devoid of toxicity up to 2000 mg/kg in Wistar albino rats. It was analysed that in vitro anti-inflammatory activity of MEOT by egg albumin denaturation method exhibited a incredible decrement in turbidity and increasing the percentage inhibition of albumin denaturation (60.52%) in MEOT treated group as compared with control group. In egg albumin-induced edema in rats, MEOT at the dose of 400 mg/kg reduced the edema formation (3.03 ± 0.02) induced by egg albumin at 4th h. In cotton pellet-induced granuloma in rats, MEOT at the dose of 400 mg/kg displayed maximum granuloma inhibition (51.06%) which is similar to that of indomethacin. Conclusion: From the obtained findings it is confirmed that O. turpethum contains β-sitosterol which is responsible for potent anti-inflammatory activity without causing cytotoxicity to the plant. The results suggested that ME of O. turpethum roots had high potential for application as an anti-inflammatory agent. The recognization and confirmation of the plant can be obtaineded from the study and will present data which is aidful in determining the quality and purity of a crude drug which further helps in preventing its adulteration.

2020 ◽  
Vol 11 (4) ◽  
pp. 7317-7322
Author(s):  
Sebastin V ◽  
Gopalakrishnan G ◽  
Sreejith M ◽  
Anoob Kumar K I

Plants of the genus Argyreia have ethnomedicinal importance, and several pharmacological activities are also reported. In this study, the anti-inflammatory activity of different extracts of Argyreia imbricata was evaluated by in vitro and in vivo methods. In both evaluations, standard, Diclofenac sodium was used for comparative evaluation. In this study, extraction of powdered whole plant material was done with different solvents viz., petroleum ether, chloroform, ethyl acetate and methanol by soxhelation. In vitro anti-inflammatory activity of all the prepared extracts was evaluated by stabilization of human red blood cell (HRBC) membrane in different temperature and tonicity conditions. Among the six different concentrations of four tested extracts, the ethyl acetate and methanol extracts (1000μg/ml) showed significant activity in the in vitro evaluation. They were selected for the in vivo evaluation on the paw oedema induced by carrageenan on Wistar albino rats. Two doses, 200mg.kg-1 and 400mg.kg-1 of the test extracts were subjected to evaluation. Both the tested extracts showed the activity, particularly, the methanol extract in the dose of 400mg.kg-1 showed significant activity. Results of this study strongly supported the anti-inflammatory activity of the tested extracts. Further, studies on toxicity, identification, isolation of the active constituents may give useful results.


Author(s):  
Priya Mohan B. N. ◽  
Suma Jayaram ◽  
Sanitha Kuriachan

Background: Inflammation is part of the complex biological response of vascular tissues to harmful stimuli. Though there are standard anti-inflammatory drugs like aspirin, diclofenac, etc., these are not free of side effects. This has led to an increase in demand for natural products with anti-inflammatory activity having less side effects. Hence the study was conducted to evaluate the anti-inflammatory activity of ethanolic extract of Ficus racemose (EEFR) in albino rats.Methods: Healthy albino rats of either sex were divided into 4 groups of 6 animals each. Group1-control, group 2-diclofenac sodium 2 mg/kg and group 3 and 4 EEFR (200 and 400 mg/kg respectively), anti-inflammatory activity was evaluated by Carrageenan induced paw oedema: formalin induced-peritonitis and cotton pellet induced granuloma model for in vivo activity and protein denaturation test for in vitro activity.Results: EEFR exhibited significant in vitro (p<0.001) anti-inflammatory effect at the dose of 200 and 400 mg/kg. EEFR produced 61.37% inhibition at the dose of 400 mg/kg and diclofenac (standard drug) produced 62.95% of inhibition after 3 hours of drug treatment in carrageenan induced paw oedema. The exudate volume was decreased in formalin induced peritonitis by EEFR and diclofenac significantly (p<0.001). In cotton pellet induced granuloma EEFR (400 mg/kg) and diclofenac showed decreased formation of granuloma by 28.36% and 28.00% (p<0.001) respectively.Conclusions: EEFR has significant anti-inflammatory activity in both acute and chronic model in a dose dependant manner in comparison with standard drug.


2020 ◽  
Vol 17 (3) ◽  
pp. 195-206
Author(s):  
Teerasak Damrongrungruang ◽  
Panjaree Panpitakkul ◽  
Jirachaya Somudorn ◽  
Pimpitchaya Sangchart ◽  
Pramote Mahakunakorn ◽  
...  

Background: Glutaryl melatonin, which is synthesized from melatonin and is a pineal glandderived neurohormone with anti-inflammatory and anti-oxidant properties, was comparatively investigated for its potential use as a topical anti-inflammatory agent. Objective: Glutaryl melatonin, synthesized and screened for in vitro anti-candidiasis and in vitro and in vivo anti-inflammatory activities, was formulated as a niosome gel for topical oral evaluation in 5- fluorouracil-induced oral mucositis in mice. Methods: In vitro anti-fungal activity in Candida albicans, in vitro anti-inflammatory activity in Escherichia coli liposaccharide-induced RAW cells and in vivo anti-inflammatory activity using a croton oilinduced ear edema model in ICR mice were investigated. Mucositis in mice (n= 6/group, 10-week-old mice) was induced by intraperitoneal injections of 5-fluorouracil, and the mice were subjected to a topical oral application of niosome gel containing melatonin (2% w/w) or glutaryl melatonin (2% w/w) and were compared with mice subjected to blank, fluocinolone acetonide (0.5% w/w) and control conditions. Results: Glutaryl melatonin, at a 14.2 mM concentration, showed the highest fungicidal effect on C. albicans using the broth dilution method, indicating a nonsignificant difference from 1 μM of nystatin (p = 0.05). Nitric oxide, interleukin-6 and tumor necrosis factors were analyzed by ELISA. Liposaccharide-induced RAW cells were significantly reduced by glutaryl melatonin (p < 0.01). Ear edema inhibition of glutaryl melatonin was significant 1 h after application compared with that of melatonin (p = 0.03). Food consumption and body weight of the 5-fluorouracil-treated mice were significantly lower than those of the normal mice before all treatments (p < 0.05). Differences in the amount of licking behavior, which were observed in the control group for 5 min, were noticeable in the 5- fluorouracil-treated mice but not in the mice treated with the glutaryl melatonin niosome gel. Conclusion: Glutaryl melatonin exhibited mild anti-candidiasis and anti-inflammatory properties. The incorporation of glutaryl melatonin in a niosome gel formulation, demonstrated the potential for topical oral applications to reduce oral discomfort caused by 5-fluorouracil treatment in mice.


Author(s):  
SUMATHI RAJAMANI ◽  
GOBINATH KALYANA SUNDARAM ◽  
TAMIZHARASI SENGODAN ◽  
SIVAKUMAR THANGAVELU ◽  
NIKHITHA K SHANMUKHAN ◽  
...  

Objective: Naringenin (NAR) a flavonoid, exhibits extensive pharmacological action, fails to attain a significance in application due to low aqueous solubility (~ 0.214 mg/mL) which results in low bioavailability (5.8%). Nanosuspension of NAR (NARNS) was prepared in our previous studies using high-pressure homogenization employing various polymers. All these formulations were characterized and as a continuation of our work formulations was further evaluated for their anti-inflammatory activity by in vitro and in vivo methods. Methods: Denaturation of protein method and membrane stabilization methods was chosen for in vitro evaluation. In vivo studies performed were acute inflammatory studies (carrageenan-induced paw edema) and chronic inflammatory studies (cotton pellet granuloma) on Wistar albino rats. Results: The studies demonstrated that the NAR and NARNS at a dose of 50mg/kg P.O. have a potent activity compared to the standard drug diclofenac. Conclusion: The percentage of protection against inflammation exhibited by NARNS was highly significant compared to NAR.


Author(s):  
Shiva Murthy N. ◽  
Srinivas V. ◽  
Shanthi M.

Background: NSAIDS are associated with side effects and research should continue for developing safer drugs. This study aims to evaluate newer thiazolidine-4-ones for their anti-inflammatory and ulcerogenic activities in wister rats.Methods: Five groups of wister rats, 6 in each were used.  Anti-inflammatory and ulcerogenic activities of diclofenac (30mg/kg), nimesulide (50mg/kg), thia-1 (50mg/kg) and thia-2 (50mg/kg) are compared with control group (4% Gum Acacia). Carrageenin-induced paw edema, formaline induced acute peritonitis and cotton pellet-induced granulomatous tissue formation models were used for evaluating anti-inflammatory activity. After removing cotton pellets with granuloma on 8th day gastric ulcerogenicity was assessed by using macroscopic and microscopic scoring of ulcers.Results: Diclofenac, nimesulide and thia 2 reduced both paw edema and peritoneal exudate volume significantly (p <0.01). Wet weight of cotton pellets reduced significantly (p <0.01) by diclofenac, nimesulide and thia 2. Diclofenac (p <0.01) and thia 2 (p <0.05) reduced dry weight of cotton pellets significantly. nimesulide and thia-1 reduced it by 19.14% and 2.68% respectively and was considered statistically not significant (p>0.05). Nimesulide, thia-1 and thia-2 did not increase gastric ulcer score significantly (p >0.05). Diclofenac increased ulcer score significantly (p <0.01).Conclusions: Thia-2 demonstrated significant anti-inflammatory activity in acute and chronic models. In addition to inhibition of cyclooxygenase pathway, PPAR agonistic activity may be involved in its anti-inflammatory activity.  No significant ulcerogenicity was observed on comparing with nimesulide and control. Further in-vitro and in-vivo studies are recommended to confirm the results of this study.


Author(s):  
O. V. Ikpeazu ◽  
M. I. Ezeja ◽  
K. K. Igwe

Aims: To investigate the anti-inflammatory activity of Picralima nitida stem bark methanol extract (PNSBE). Study Design: The study was carried out using in vivo (carrageenan-induced paw oedema and egg albumin-induced paw oedema) and in vitro (Human red blood cell (HRBC) membrane stabilization assay) models in rat. Place and Duration of Study: Department of Veterinary Physiology and Pharmacology, Michael Okpara University of Agriculture, Umudike, Abia State, Nigeria from March to July, 2020. Methodology: The extract was used at the doses of 100, 200 and 400 mg/kg while diclofenac (20 mg/kg) was used as the standard reference drug for the in vivo study (carrageenan-induced paw oedema and egg albumin). For the in vitro study (red blood cell haemolysis), the extract was used at the concentrations of 25, 50, 100, 200 and 400 µg/ml while diclofenac 250 µg/ml was used. Results: In the carrageenan-induced paw oedema model, the extract at the doses used and the reference drug significantly (p < 0.05) reduced the paw edema in the rats at 1 hour in a dose dependent manner. Also, in the egg albumin model, the paw oedema of treated rats was significantly (P < 0.05) reduced by PNSBE dose dependently reducing the mean rat paw oedema from 0.99 ± 0.12 to 0.61 ± 0.06 at the first hour. There was also a concentration dependent inhibition of red blood cell haemolysis by the extract in the HRBC membrane stabilization assay. Conclusion: Picralma nitida demonstrated a significant anti-inflammatory activity in this study.


Author(s):  
Thriveni Vasanth Kumar ◽  
Manjunatha H. ◽  
Rajesh Kp

Objective: Dietary curcumin and capsaicin are well known for their health beneficial potencies. The current study was done to assess the anti-inflammatory activity of curcumin, capsaicin and their combination by employing in vitro and in vivo models.Methods: We investigated the protective effect of curcumin, capsaicin and their combination using in vitro heat induced human red blood cell (HRBC) membrane stabilisation, in vivo 3% agar induced leukocyte mobilisation and acetic acid induced vascular permeability assay.Results: Curcumin, capsaicin and their combination exhibited concentration dependent protective effect against heat-induced HRBC membrane destabilisation, while combined curcumin and capsaicin restored 87.0±0.64 % membrane stability and it is found to be better than curcumin, capsaicin and diclofenac sodium (75.0±0.25. 72±0.9 and 80.0±0.31 %) protective effect. In agar suspension induced leukocyte mobilization assay, the combined curcumin and capsaicin had shown 39.5±1.58 % of inhibition compared to individual curcumin and capsaicin, which showed moderate inhibition of 16.0±3.14 and 21.6±2.17 % respectively. Besides, the combined curcumin and capsaicin had shown highly significant inhibition of acetic acid-induced vascular permeability in rats (62.0±3.14 %), whereas individual curcumin and capsaicin showed moderate inhibition of vascular permeability with 36.0±2.41 and 43.0±1.92 % respectively.Conclusion: This study demonstrates the significant anti-inflammatory property of combined curcumin and capsaicin at half of the individual concentration of curcumin and capsaicin.


2005 ◽  
Vol 317 (1) ◽  
pp. 53-60 ◽  
Author(s):  
Xiaohua Xue ◽  
Kuei-Tai A. Lai ◽  
Jing-Feng Huang ◽  
Yin Gu ◽  
Lars Karlsson ◽  
...  

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