Pharmacological Screening for CNS Depression, Analgesic and Anti-inflammatory Potentials of Sonneratia caseolaris (Linn.) Barks in Different Solvent Fraction

Aims: Bark of different fractions of Sonneratia caseolaris (Linn.) (Sonneratiaceae) were screened for its analgesic, anti-inflammatory and CNS activities. Study Design: For the purpose of these experiments the extracts were subjected to an in-vivo study. Place and Duration of Study: The study was carried out in August 2014 in the Department of Pharmacy, Southeast University, Dhaka, Bangladesh. Methodology: Ethanolic (ETF), ethyl acetate (EAF), chloroform(CLF) and pet ether (PTF) fractions of bark of S. caseolaris were used to evaluate the analgesic activity using Acetic acid induced writhing and Formalin test. The same fractions were evaluated for anti-inflammatory activity using Carrageenan induced hind paw edema model. The CNS depressant activity was evaluated by Hole cross method. Two doses of 150 mg/kg and 300 mg/kg were used. Results: The different fractions produced significant (p<0.05) writhing inhibition at both doses and reduced the number of linking induced by formalin. Among these fractions the most potent activity was found in ETF about 79.40% (300 mg/kg) that was almost similar to standard Diclofenac-Na 82.78% (10 mg/kg), then EAF 74.59% followed by CLF 59.03% and PTF 52.45% at dose 300 mg/kg). In formalin-induced paw licking model, all fractions of S. caseolaris showed superior result in the late phase compare to the early phase .The same fractions of extracts caused significant (p<0.05) inhibition of carrageenan induced paw edema in a dose dependent manner. A statistically significant (p<0.05) locomotor activity was also observed. Conclusion: Our result revealed that all the extractives of S. caseolaris have noticeable analgesic, anti-inflammatory and CNS depressant activities.

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Molecular Insight into the Anti-Inflammatory Effects of the Curcumin Ester Prodrug Curcumin Diglutaric Acid In Vitro and In Vivo

International Journal of Molecular Sciences ◽

10.3390/ijms21165700 ◽

2020 ◽

Vol 21 (16) ◽

pp. 5700 ◽

Cited By ~ 1

Author(s):

Rianthong Phumsuay ◽

Chawanphat Muangnoi ◽

Peththa Wadu Dasuni Wasana ◽

Hasriadi Hasriadi ◽

Opa Vajragupta ◽

...

Keyword(s):

Time Course ◽

Area Under The Curve ◽

Dependent Manner ◽

Paw Edema ◽

Inflammatory Agent ◽

Potent Inhibition ◽

Anti Inflammatory ◽

Ester Prodrug

Curcumin diglutaric acid (CurDG), an ester prodrug of curcumin, has the potential to be developed as an anti-inflammatory agent due to its improved solubility and stability. In this study, the anti-inflammatory effects of CurDG were evaluated. The effects of CurDG on inflammatory mediators were evaluated in LPS-stimulated RAW 264.7 macrophage cells. CurDG reduced the increased levels of NO, IL-6, and TNF- α, as well as iNOS and COX-2 expression in cells to a greater extent than those of curcumin, along with the potent inhibition of MAPK (ERK1/2, JNK, and p38) activity. The anti-inflammatory effects were assessed in vivo by employing a carrageenan-induced mouse paw edema model. Oral administration of CurDG demonstrated significant anti-inflammatory effects in a dose-dependent manner in mice. The effects were significantly higher compared to those of curcumin at the corresponding doses (p < 0.05). Moreover, 25 mg/kg curcumin did not exert a significant anti-inflammatory effect for the overall time course as indicated by the area under the curve data, while the equimolar dose of CurDG produced significant anti-inflammatory effects comparable with 50, 100, and 200 mg/kg curcumin (p < 0.05). Similarly, CurDG significantly reduced the proinflammatory cytokine expression in paw edema tissues compared to curcumin (p < 0.05). These results provide the first experimental evidence for CurDG as a promising anti-inflammatory agent.

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IN VITRO ANTIOXIDANT AND IN VIVO ANTI-INFLAMMATORY ACTIVITY OF THE AERIAL PART OF BLUMEA ERIANTHA DC

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2018v10i7.25588 ◽

2018 ◽

Vol 10 (7) ◽

pp. 75 ◽

Cited By ~ 1

Author(s):

Urmila U. Tambewagh ◽

Supada Rambhau Rojatkar

Keyword(s):

Antioxidant Activity ◽

Aerial Part ◽

Methanol Extract ◽

Reducing Power ◽

Dependent Manner ◽

Paw Edema ◽

Anti Inflammatory ◽

In Vitro Antioxidant Activity

Objective: Objective of the present study was to carry out in vivo anti-inflammatory and in vitro antioxidant activity of methanol extract of aerial part of the Blumea eriantha DC belonging to family Asteraceae.Methods: The shade dried aerial part of B. eriantha (0.5 kg) was powdered and extracted with methanol (1.5 x 3L) at room temperature (24h x 3). After filtration combined all the three extracts and were concentrated on rotary evaporator under reduced pressure at 40 °C, thereby providing crude methanol extract which was subsequently employed for further studies. Anti-inflammatory effect was studied by carrageenan-induced paw edema model in rats at dose level 100, 200, and 400 mg/kg. Acute oral toxicity study and in vitro antioxidant potential of the extract was also studied. The in vitro antioxidant activity of methanol extract of aerial part of Blumea eriantha DC was evaluated against 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydrogen peroxide (H2O2) and hydroxyl (OH) radicalscavenging and reducing power assays.Results: The results indicate that methanol extract of Blumea eriantha (BEME, 400 mg/kg) exhibited significant inhibition (p<0.001) of increase in paw edema at 5th h. IC50 value of BEME showed significant antioxidant activity. The extract exhibits promising free radical scavenging effect of DPPH, H2O2, OH and reducing power in a dose-dependent manner up to 100µg/ml concentration while the reference standard Ascorbic acid demonstrated more scavenging potential than the methanol extract of Blumea eriantha The methanol extract was found to be safe at the dose of 2000 mg/kg.Conclusion: The results of the experimental study confirmed that methanol extract of Blumea eriantha DC possesses significant anti-inflammatory and antioxidant activity.

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Analgesic and Anti-Inflammatory Activities of the Methanol Extract fromPogostemon cablin

Evidence-based Complementary and Alternative Medicine ◽

10.1093/ecam/nep183 ◽

2011 ◽

Vol 2011 ◽

pp. 1-9 ◽

Cited By ~ 17

Author(s):

Tsung-Chun Lu ◽

Jung-Chun Liao ◽

Tai-Hung Huang ◽

Ying-Chih Lin ◽

Chia-Yu Liu ◽

...

Keyword(s):

Acetic Acid ◽

Methanol Extract ◽

Second Phase ◽

Dependent Manner ◽

Paw Edema ◽

Pogostemon Cablin ◽

Anti Oxidant ◽

Anti Inflammatory ◽

Factor Α

Pogostemon cablin(PC) is a herbal medicine traditionally applied to treat not only common cold, nausea and diarrhea but also headache and fever. The aim of this study was to investigate the analgesic and anti-inflammatory properties of standardized PC methanol extract (PCMeOH)in vivo. Investigations were performed in mice with two analgesic models. One was acetic acid-induced writhing response and the other formalin-induced paw licking. The anti-inflammatory effect was tested by λ-carrageenan (Carr)-induced mice paw edema. These analgesic experimental results indicated that PCMeOH (1.0 g/kg) decreased the acetic acid-induced writhing responses and PCMeOH (0.5 and 1.0 g/kg) decreased the licking time in the second phase of the formalin test. Moreover, Carr-induced paw edema inflammation was significantly reduced in a dose-dependent manner when PCMeOH (0.5 and 1.0 g/kg) was administered 3 and 4 h after the Carr injection. Mechanistic studies showed that PCMeOH decreased the levels of malondialdehyde in the edema paw by increasing the activities of anti-oxidant enzymes, such as superoxide dismutase, glutathione peroxidase and glutathione reductase, in the liver and decreasing the cyclooxygenase 2 and tumor necrosis factor-α activities in the edema paw. This study has demonstrated the analgesic and anti-inflammatory effects of PCMeOH, thus verifying its popular use in traditional medicine.

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Evaluation of anti-inflammatory activity of Justicia secunda Vahl leaf extract using in vitro and in vivo inflammation models

Clinical Phytoscience ◽

10.1186/s40816-019-0137-8 ◽

2019 ◽

Vol 5 (1) ◽

Cited By ~ 1

Author(s):

Godswill Nduka Anyasor ◽

Azeezat Adenike Okanlawon ◽

Babafemi Ogunbiyi

Keyword(s):

Erythrocyte Membrane ◽

Diclofenac Sodium ◽

Inflammatory Activity ◽

Dependent Manner ◽

Paw Edema ◽

In Vivo Models ◽

In Vivo Inflammation ◽

Anti Inflammatory

Abstract Background Justicia secunda Vahl. is a medicinal plant used in ethnomedical practice as therapy to manage inflammation. Therefore, this study was designed to evaluate the anti-inflammatory activity of methanol extract of J. secunda leaves (MEJSL) using in vitro and in vivo inflammation models. Methods Seventy-percent MEJSL was prepared following standard procedure. In vitro anti-inflammatory assays were performed using heat-induced bovine serum albumin (BSA) denaturation and erythrocyte membrane stabilization assays. Carrageenan and formaldehyde induced inflammation in rat models were used to evaluate the anti-inflammatory activity of MEJSL in vivo. Diclofenac sodium was used as a reference drug. In addition, liver and kidney function assays and hematological analysis were carried out. Results Data revealed that varying concentrations of MEJSL significantly (P < 0.05) inhibited heat-induced BSA denaturation and stabilized erythrocyte membrane against hypotonicity-induced hemolysis when compared with diclofenac sodium in a concentration-dependent manner. In vivo study showed that 10 mg/kg body weight (b.w.) diclofenac sodium, 100 and 300 mg/kg b.w. MEJSL suppressed carrageenan-induced paw edema at the sixth hour by 71.14%, 83.08%, and 89.05%, respectively. Furthermore, 10 mg/kg b.w. diclofenac sodium, 100 and 300 mg/kg b.w. MEJSL inhibited formaldehyde-induced paw edema by 72.53%, 74.73%, and 76.48%, respectively. Animals treated with varying doses of MEJSL had reduced plasma aspartate aminotransferase and alanine aminotransferase activities; urea and creatinine concentrations; and modulated hematological parameters when compared with the untreated control group. Conclusions Findings from this study showed that MEJSL exhibited substantial anti-inflammatory actions in the in vitro and in vivo models. It also indicated that MEJSL anti-inflammatory mechanisms of action could be through interference with phase 2 inflammatory stressors, upregulation of cytoprotective genes, stabilization of inflammatory cell membranes and immunomodulatory activity.

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Coptis chinensisand Myrobalan (Terminalia chebula) Can Synergistically Inhibit Inflammatory Response In Vitro and In Vivo

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2014/510157 ◽

2014 ◽

Vol 2014 ◽

pp. 1-8 ◽

Cited By ~ 4

Author(s):

Enhui Cui ◽

Xiaoyan Zhi ◽

Ying Chen ◽

Yuanyuan Gao ◽

Yunpeng Fan ◽

...

Keyword(s):

Nitric Oxide ◽

Therapeutic Potential ◽

In Vitro Cytotoxicity ◽

High Dose ◽

Dependent Manner ◽

Paw Edema ◽

Coptis Chinensis ◽

Anti Inflammatory

Objectives. To investigate the anti-inflammatory effect ofCoptis chinensisplus myrobalan (CM) in vitro and in vivo.Methods. The inflammation in mouse peritoneal macrophages was induced by lipopolysaccharide (LPS). Animal models were established by using ear swelling and paw edema of mouse induced by xylene and formaldehyde, respectively. In vitro, cytotoxicity, the phagocytosis of macrophages, the levels of nitric oxide (NO), induced nitric oxide synthase (iNOS), tumor necrosis factor-α(TNF-α), and interleukin-6 (IL-6) in cell supernatant were detected. In vivo, swelling rate and edema inhibitory rate of ear and paw were observed using CM-treated mice.Results. At 150–18.75 μg·mL−1, CM had no cytotoxicity and could significantly promote the growth and the phagocytosis of macrophages and inhibit the overproduction of NO, iNOS, TNF-α, and IL-6 in macrophages induced by LPS. In vivo, pretreatment with CM, the ear swelling, and paw edema of mice could be significantly inhibited in a dose-dependent manner, and the antiedema effect of CM at high dose was better than dexamethasone.Conclusion. Our results demonstrated thatCoptis chinensisand myrobalan possessed synergistically anti-inflammatory activities in vitro and in vivo, which indicated that CM had therapeutic potential for the prevention and treatment of inflammation-mediated diseases.

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Evaluation of central nervous system depressant activity of methanolic and petroleum ether extract of Manilkara zapota leaves (in vivo)

International Journal of Phytomedicine ◽

10.5138/09750185.1896 ◽

2016 ◽

Vol 8 (3) ◽

pp. 308

Author(s):

Manirujjaman ◽

Trudi Collet

Keyword(s):

Central Nervous System ◽

Nervous System ◽

Locomotor Activity ◽

Petroleum Ether ◽

Open Field ◽

Dependent Manner ◽

Manilkara Zapota ◽

Cns Depressant ◽

Cns Depressant Activity

The purpose of this study was to examine the central nervous system (CNS) -depressant activity of methanolic and petroleum ether extracts of leaves obtained from Manilkara zapota (Sapotaceae) in vivo. CNS-depressant action was evaluated by observing the effects of plant extracts on both exploratory and spontaneous locomotor activity in mice using open field and hole cross tests respectively. The extracts were found to exhibit CNS-depressant activity in a dose-dependent manner. In the open field test, both the methanolic and petroleum ether extracts reduced the exploratory behavior of mice significantly (p<0.05). Although the extracts reduced locomotor activity in the hole cross test, the results were found to be insignificant. Overall, these findings indicate that both types of extracts derived from M. zapota leaves possess CNS-depressant activity.

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Cartilage protective and anti-analgesic effects of ALM16 on monosodium iodoacetate induced osteoarthritis in rats

BMC Complementary and Alternative Medicine ◽

10.1186/s12906-019-2746-7 ◽

2019 ◽

Vol 19 (1) ◽

Cited By ~ 4

Author(s):

Doo Jin Choi ◽

Soo-Im Choi ◽

Bo-Ram Choi ◽

Young-Seob Lee ◽

Dae Young Lee ◽

...

Keyword(s):

Joint Disease ◽

Control Group ◽

Dependent Manner ◽

Paw Edema ◽

In Vivo Models ◽

Age Related ◽

Monosodium Iodoacetate ◽

Anti Inflammatory

Abstract Background Osteoarthritis (OA) is an age-related joint disease with characteristics that involve the progressive degradation of articular cartilage and resulting chronic pain. Previously, we reported that Astragalus membranaceus and Lithospermum erythrorhizon showed significant anti-inflammatory and anti-osteoarthritis activities. The objective of this study was to examine the protective effects of ALM16, a new herbal mixture (7:3) of ethanol extracts of A. membranaceus and L. erythrorhizon, against OA in in vitro and in vivo models. Methods The levels of matrix metalloproteinase (MMP)-1, −3 and − 13 and glycosaminoglycan (GAG) in interleukin (IL)-1β or ALM16 treated SW1353 cells were determined using an enzyme-linked immunosorbent and quantitative kit, respectively. In vivo, the anti-analgesic and anti-inflammatory activities of ALM16 were assessed via the acetic acid-induced writhing response and in a carrageenan-induced paw edema model in ICR mice, respectively. In addition, the chondroprotective effects of ALM16 were analyzed using a single-intra-articular injection of monosodium iodoacetate (MIA) in the right knee joint of Wister/ST rat. All samples were orally administered daily for 2 weeks starting 1 week after the MIA injection. The paw withdrawal threshold (PWT) in MIA-injected rats was measured by the von Frey test using the up-down method. Histopathological changes of the cartilage in OA rats were analyzed by hematoxylin and eosin (H&E) staining. Results ALM16 remarkably reduced the GAG degradation and MMP levels in IL-1β treated SW1353 cells. ALM16 markedly decreased the thickness of the paw edema and writhing response in a dose-dependent manner in mice. In the MIA-induced OA rat model, ALM16 significantly reduced the PWT compared to the control group. In particular, from histological observations, ALM16 showed clear improvement of OA lesions, such as the loss of necrotic chondrocytes and cartilage erosion of more than 200 mg/kg b.w., comparable to or better than a positive drug control (JOINS™, 200 mg/kg) in the cartilage of MIA-OA rats. Conclusions Our results demonstrate that ALM16 has a strong chondroprotective effect against the OA model in vitro and in vivo, likely attributed to its anti-inflammatory activity and inhibition of MMP production.

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Decoding the temporal nature of brain GR activity in the NFκB signal transition leading to depressive-like behavior

Molecular Psychiatry ◽

10.1038/s41380-021-01016-1 ◽

2021 ◽

Author(s):

Young-Min Han ◽

Min Sun Kim ◽

Juyeong Jo ◽

Daiha Shin ◽

Seung-Hae Kwon ◽

...

Keyword(s):

Inhibitory Action ◽

Time Course ◽

Molecular Mechanisms ◽

Late Phase ◽

Fine Tuning ◽

Dependent Manner ◽

Middle Phase ◽

Temporal Shift

AbstractThe fine-tuning of neuroinflammation is crucial for brain homeostasis as well as its immune response. The transcription factor, nuclear factor-κ-B (NFκB) is a key inflammatory player that is antagonized via anti-inflammatory actions exerted by the glucocorticoid receptor (GR). However, technical limitations have restricted our understanding of how GR is involved in the dynamics of NFκB in vivo. In this study, we used an improved lentiviral-based reporter to elucidate the time course of NFκB and GR activities during behavioral changes from sickness to depression induced by a systemic lipopolysaccharide challenge. The trajectory of NFκB activity established a behavioral basis for the NFκB signal transition involved in three phases, sickness-early-phase, normal-middle-phase, and depressive-like-late-phase. The temporal shift in brain GR activity was differentially involved in the transition of NFκB signals during the normal and depressive-like phases. The middle-phase GR effectively inhibited NFκB in a glucocorticoid-dependent manner, but the late-phase GR had no inhibitory action. Furthermore, we revealed the cryptic role of basal GR activity in the early NFκB signal transition, as evidenced by the fact that blocking GR activity with RU486 led to early depressive-like episodes through the emergence of the brain NFκB activity. These results highlight the inhibitory action of GR on NFκB by the basal and activated hypothalamic-pituitary-adrenal (HPA)-axis during body-to-brain inflammatory spread, providing clues about molecular mechanisms underlying systemic inflammation caused by such as COVID-19 infection, leading to depression.

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The impact of indole-3-lactic acid on immature intestinal innate immunity and development: a transcriptomic analysis

Scientific Reports ◽

10.1038/s41598-021-87353-1 ◽

2021 ◽

Vol 11 (1) ◽

Author(s):

Wuyang Huang ◽

Ky Young Cho ◽

Di Meng ◽

W. Allan Walker

Keyword(s):

Lactic Acid ◽

Mechanistic Model ◽

Transcriptomic Analysis ◽

Dependent Manner ◽

Protective Effects ◽

Very Preterm Infants ◽

Anti Inflammatory ◽

The Impact

AbstractAn excessive intestinal inflammatory response may have a role in the pathogenesis of necrotizing enterocolitis (NEC) in very preterm infants. Indole-3-lactic acid (ILA) of breastmilk tryptophan was identified as the anti-inflammatory metabolite involved in probiotic conditioned media from Bifidobacteria longum subsp infantis. This study aimed to explore the molecular endocytic pathways involved in the protective ILA effect against inflammation. H4 cells, Caco-2 cells, C57BL/6 pup and adult mice were used to compare the anti-inflammatory mechanisms between immature and mature enterocytes in vitro and in vivo. The results show that ILA has pleiotropic protective effects on immature enterocytes including anti-inflammatory, anti-viral, and developmental regulatory potentials in a region-dependent and an age-dependent manner. Quantitative transcriptomic analysis revealed a new mechanistic model in which STAT1 pathways play an important role in IL-1β-induced inflammation and ILA has a regulatory effect on STAT1 pathways. These studies were validated by real-time RT-qPCR and STAT1 inhibitor experiments. Different protective reactions of ILA between immature and mature enterocytes indicated that ILA’s effects are developmentally regulated. These findings may be helpful in preventing NEC for premature infants.

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ANTIULCER AND ANTI-INFLAMMATORY ACTIVITIES OF HYDROALCOHOLIC EXTRACTS OF STEM BARK AND LEAF OF ANOGEISSUS PENDULA EDGEW

INDIAN DRUGS ◽

10.53879/id.58.01.11950 ◽

2021 ◽

Vol 58 (01) ◽

pp. 41-46

Author(s):

Deeksha Singh ◽

◽

Amit Nayak ◽

Rakesh Yadav ◽

Uttam Singh Baghel ◽

...

Keyword(s):

Phenolic Compounds ◽

Stem Bark ◽

Inflammatory Activity ◽

Antiulcer Activity ◽

Paw Edema ◽

Ulcer Index ◽

Pylorus Ligation ◽

Anti Inflammatory ◽

Anogeissus Pendula

Anogeissus pendula Edgew has been reported to be used in gastric disorder even though no attempt has been made to evaluate the same. The present study was designed to evaluate the hydroalcoholic extracts of stem bark and leaves for in vivo acute antiulcer and anti-inflammatory activities. Antiulcer activity was studied by pylorus ligation induced ulcers while anti-inflammatory activities was studied by carrageenan induced paw edema. The extract of stem bark at 200 and 400 mg/kg b. w., significantly (P<0.05) reduced ulcer index whereas extracts of both stem bark and leaves significantly (P<0.001) reduced paw diameter at the fifth hour. The hydroalcholic extract of stem bark of A. pendula possesses more significant antiulcer and anti-inflammatory activity than the hydroalcholic extract of leaves may be due to the presence of higher amount of phenolic compounds.

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