Involvement of the Benzodiazepine Site in the Anticonvulsant Activity of Tapinanthus globiferus against Pentylenetetrazole-induced Seizures in Mice

Planta Medica ◽  
2020 ◽  
Vol 86 (16) ◽  
pp. 1204-1215
Author(s):  
Christianah A. Elusiyan ◽  
Ana Luiza Gonçalves Faria ◽  
Ane Emanuelle Queiroga Mendes ◽  
Iransé Oliveira Silva ◽  
José Luis Rodrigues Martins ◽  
...  

Abstract Tapinanthus globiferus is often referred to as an all-purpose herb for the treatment of stroke and epilepsy. The present study investigates the anticonvulsant effect of methanolic leaf extract, active fractions, and lupeol (isolate) of Tapinanthus globiferus in mice as well as the underlying mechanisms. Following phytochemical studies of T. globiferus, preliminary assays were performed to evaluate MLE-induced toxic effect and behavioral changes. The pentylenetetrazol (70 mg/kg, i. p.)-induced seizure was evaluated in mice that were pretreated orally with vehicle 10 mL/kg, MLE (4, 20, or 100 mg/kg), fractions (F1 to F6), lupeol 10 mg/kg or diazepam (3 mg/kg). Methanolic leaf extract preserved neuron viability as well as the relative organ weight, and hematological and biochemical parameters. The behavioral endpoints, neuromuscular coordination, and sensory response parameters revealed a dose-dependent effect of methanolic leaf extract. This extract, active fractions, lupeol, and diazepam potentiated the hypno-sedative effect of the barbiturate and attenuated PTZ-induced acute seizure. This antiseizure effect was completely reversed by flumazenil 2 mg/kg (benzodiazepine site antagonist). Altogether, the benzodiazepine site-mediated anticonvulsant effects of methanolic leaf extract, active fractions, and lupeol corroborate traditional application of T. globiferus against epilepsy.

Author(s):  
R. C. Agrawal

The phytochemical  screening, and anti-bacterial activities of the hydro-methanolic leaves extract of Psidium guajava   using standard screening methods such as disc diffusion methods. The secondary metabolites such as alkaloids, phenols , saponins, and tannins were present  in Psidium guava  extract in phytochemical screening, It also showed dose dependent  antibacterial activities against almost all the test organisms.  Results denote the antibacterial activity of Psidium guajava leaves extract


2019 ◽  
Vol 17 (4) ◽  
pp. 426-431
Author(s):  
Jin Xuezhu ◽  
Li Jitong ◽  
Nie Leigang ◽  
Xue Junlai

The main purpose of this study is to investigate the role of citrus leaf extract in carbon tetrachloride-induced hepatic injury and its potential molecular mechanism. Carbon tetrachloride was used to construct hepatic injury animal model. To this end, rats were randomly divided into 4 groups: control, carbon tetrachloride-treated, and two carbon tetrachloride + citrus leaf extract-treated groups. The results show that citrus leaf extract treatment significantly reversed the effects of carbon tetrachloride on the body weight changes and liver index. Besides, treatment with citrus leaf extract also reduced the levels of serum liver enzymes and oxidative stress in a dose-dependent manner. H&E staining and western blotting suggested that citrus leaf extract could repair liver histological damage by regulating AMPK and Nrf-2.


2019 ◽  
Vol 18 (1) ◽  
pp. 34-38
Author(s):  
Chen Lei ◽  
Pan Xiang ◽  
Shen Yonggang ◽  
Song Kai ◽  
Zhong Xingguo ◽  
...  

The aim of this study was to determine whether polydatin, a glucoside of resveratrol isolated from the root of Polygonum cuspidatum, warranted development as a potential therapeutic for ameliorating the pain originating from gallbladder spasm disorders and the underlying mechanisms. Guinea pig gallbladder smooth muscles were treated with polydatin and specific inhibitors to explore the mechanisms underpinning polydatin-induced relaxation of carbachol-precontracted guinea pig gallbladder. Our results shown that polydatin relaxed carbachol-induced contraction in a dose-dependent manner through the nitric oxide/cyclic guanosine monophosphate/protein kinase G and the cyclic adenosine monophosphate/protein kinase A signaling pathways as well as the myosin light chain kinase and potassium channels. Our findings suggested that there was value in further exploring the potential therapeutic use of polydatin in gallbladder spasm disorders.


Entropy ◽  
2021 ◽  
Vol 23 (5) ◽  
pp. 592
Author(s):  
Maria Rubega ◽  
Emanuela Formaggio ◽  
Franco Molteni ◽  
Eleonora Guanziroli ◽  
Roberto Di Marco ◽  
...  

Stroke is the commonest cause of disability. Novel treatments require an improved understanding of the underlying mechanisms of recovery. Fractal approaches have demonstrated that a single metric can describe the complexity of seemingly random fluctuations of physiological signals. We hypothesize that fractal algorithms applied to electroencephalographic (EEG) signals may track brain impairment after stroke. Sixteen stroke survivors were studied in the hyperacute (<48 h) and in the acute phase (∼1 week after stroke), and 35 stroke survivors during the early subacute phase (from 8 days to 32 days and after ∼2 months after stroke): We compared resting-state EEG fractal changes using fractal measures (i.e., Higuchi Index, Tortuosity) with 11 healthy controls. Both Higuchi index and Tortuosity values were significantly lower after a stroke throughout the acute and early subacute stage compared to healthy subjects, reflecting a brain activity which is significantly less complex. These indices may be promising metrics to track behavioral changes in the very early stage after stroke. Our findings might contribute to the neurorehabilitation quest in identifying reliable biomarkers for a better tailoring of rehabilitation pathways.


2021 ◽  
Vol 22 (15) ◽  
pp. 7932
Author(s):  
Sourav Panja ◽  
John T. Benjamin ◽  
Bibhash C. Paria

Maternal infection-induced early pregnancy complications arise from perturbation of the immune environment at the uterine early blastocyst implantation site (EBIS), yet the underlying mechanisms remain unclear. Here, we demonstrated in a mouse model that the progression of normal pregnancy from days 4 to 6 induced steady migration of leukocytes away from the uterine decidual stromal zone (DSZ) that surrounds the implanted blastocyst. Uterine macrophages were found to be CD206+ M2-polarized. While monocytes were nearly absent in the DSZ, DSZ cells were found to express monocyte marker protein Ly6C. Systemic endotoxic lipopolysaccharide (LPS) exposure on day 5 of pregnancy led to: (1) rapid (at 2 h) induction of neutrophil chemoattractants that promoted huge neutrophil infiltrations at the EBISs by 24 h; (2) rapid (at 2 h) elevation of mRNA levels of MyD88, but not Trif, modulated cytokines at the EBISs; and (3) dose-dependent EBIS defects by day 7 of pregnancy. Yet, elimination of maternal neutrophils using anti-Ly6G antibody prior to LPS exposure failed to avert LPS-induced EBIS defects allowing us to suggest that activation of Tlr4-MyD88 dependent inflammatory pathway is involved in LPS-induced defects at EBISs. Thus, blocking the activation of the Tlr4-MyD88 signaling pathway may be an interesting approach to prevent infection-induced pathology at EBISs.


2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Alian Désiré Afagnigni ◽  
Maximilienne Ascension Nyegue ◽  
Chantal Florentine Ndoye Foe ◽  
Youchahou Njankouo Ndam ◽  
Frédéric Nico Njayou ◽  
...  

The present work was undertaken to evaluate antidiarrheal activity of ethanolic leaf extract of Dissotis multiflora (Sm) Triana (D. multiflora) on Shigella flexneri-induced diarrhea in Wistar rats and its subacute toxicity. Diarrhea was induced by oral administration of 1.2 × 109 cells/mL S. flexneri to rats. Antidiarrheal activity was investigated in rats with the doses of 111.42 mg/kg, 222.84 mg/kg, and 445.68 mg/kg. The level of biochemical parameters was assessed and organs histology examined by 14 days’ subacute toxicity. S. flexneri stool load decreased significantly in dose-dependent manner. The level of ALT increased (p<0.05) in male rats treated with the dose of 445.68 mg/kg while creatinine level increased in rats treated with both doses. In female rats, a significant decrease (p<0.05) of the level of AST and creatinine was noted in rats treated with the dose of 222.84 mg/kg of D. multiflora. Histological exams of kidney and liver of treated rats showed architectural modifications at the dose of 445.68 mg/kg. This finding suggests that D. multiflora leaf extract is efficient against diarrhea caused by S. flexneri but the treatment with doses lower than 222.84 mg/kg is recommended while further study is required to define the exact efficient nontoxic dose.


2017 ◽  
Vol 15 (2) ◽  
pp. 151-156
Author(s):  
Somrudee NAKINCHAT ◽  
Voravuth SOMSAK

The emergence and spread of antimalarial drug resistance of Plasmodium parasites, as well as hypoglycemia, during malaria infection, and subsequent death, are critical problems in malaria-endemic areas. Hence, finding new compounds, especially plant extracts having antimalarial and anti-hypoglycemic activities, are urgently needed. The present study aimed to investigate the antimalarial and anti-hypoglycemic effects of Moringa oleifera leaf extract in Plasmodium berghei infection in mice. Aqueous crude extract of M. oleifera leaves was freshly prepared and used for an efficacy test in vivo. Groups of ICR mice (5 mice in each) were infected with 1´107 infected red blood cells of P. berghei ANKA by intraperitoneal injection and given the extract orally with doses of 100, 500, and 1000 mg/kg for 4 consecutive days. Parasitemia and plasma glucose levels were subsequently measured. The results showed that M. oleifera leaf extract presented significant (p < 0.001) inhibition of parasitemia in a dose-dependent manner. Moreover, this extract exerted anti-hypoglycemia effects in infected mice in a dose-dependent manner. The highest degrees of activity were found at a dose of 1000 mg/kg of the extract. Additionally, no effect on plasma glucose was found in normal mice treated with this extract. It can be concluded that aqueous crude extract of M. oleifera leaves exerted antimalarial and anti-hypoglycemic effects in P. berghei infection in mice.


2018 ◽  
Vol 7 (5) ◽  
pp. 419-424
Author(s):  
Abiodun Olusoji Owoade ◽  
◽  
Adewale Adetutu ◽  
Augustine Ikhueoya Airaodion ◽  
Olufemi Ogundeji Ogundipe ◽  
...  

This study evaluated the acute and subacute toxicity effects of Bridelia ferrugelia leaf extract. Observation of the acute group showed that LD50 of the extract is greater than 2000 mg/kg. The subacute investigation was determined by administering 200 mg/kg, 400 mg/kg and 600 mg/kg of the methanolic leaf extract to male Wistar rats for 28 days with distilled water as a control. Haematological and biochemical parameters, as well as lipid levels of vital organs, were examined. Toxicological evaluation of the extract did not produce any significant change in haematological and biochemical parameters in rats. In addition, blood lipids levels were not significantly affected, while dyslipidaemia effect observed in some vital organs were found to be nonlipotoxic. Administration of Bridelia ferrugelia at a dose of 200, 400 and 600 mg/kg for 28 days resulted in reduction of cardiac cholesterol level by 37.16%, 39.36% and 17.64% respectively, reduction of pulmonary cholesterol by 22.17%, 28.08% and 6.24 % respectively and dose-dependent decrease in pulmonary triglyceride level by 16.17, 29.14 and 54.25% respectively. This study indicates that Bridelia ferrugelia extract administered at 200, 400 and 600 mg/kg did not show any toxic effect on the parameters investigated in rats. Thus, the extract can be considered safe when administered orally


Author(s):  
Ignacio Palacios-Huerta

This chapter is concerned with the implications of incentives. It studies an incentive change in a natural setting where both productive and sabotage activities can be directly observed: soccer. The analysis proceeds in four steps. First, it describes the basic behavioral changes that took place after the change to the three-point rule. Second, it uses the control matches in the cup tournament to estimate the effects caused by the change in rewards. Third, it tries to understand the underlying mechanisms through which these changes took place and the reason they neutralized each other in terms of goal scoring by examining the way the behavior of teams changed during the match. Finally, it shows that this change represented undesirable sabotage rather than, say, desirable greater intensity in the games.


Author(s):  
Prashith Kekuda T. R. ◽  
Raghavendra H. L. ◽  
Shilpa M. ◽  
Pushpavathi D. ◽  
Tejaswini Petkar ◽  
...  

Objective: The present study was carried out to investigate antimicrobial, antiradical and insecticidal potential of leaf and fruit of Gardenia gummifera L. f. (Rubiaceae).Methods: The leaf and fruits were shade dried, powdered and extracted by maceration process using methanol. Antibacterial activity was evaluated against Gram positive and Gram negative bacteria by Agar well diffusion assay. Antifungal activity was determined against six seed-borne fungi by Poisoned food technique. Antiradical activity of leaf and fruit extracts was evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2-azinobis 3-ethylbenzothiazoline 6-sulfonate (ABTS) radical scavenging assays. Insecticidal activity of leaf and fruit extracts, in terms of larvicidal and pupicidal activity, was assessed against larvae and pupae of Aedes aegypti.Results: Both the extracts inhibited all test bacteria. Marked antibacterial activity was displayed by fruit extract when compared to leaf extract. S. epidermidis and E. coli were inhibited to highest and least extent by both extracts respectively. Fruit extract was found to exhibit higher antifungal effect when compared to leaf extract. Leaf extract and fruit extract exhibited highest inhibitory activity against A. niger and A. flavus respectively. Leaf and fruit extracts scavenged DPPH radical’s dose dependently with an IC50 value of 49.01µg/ml and 2.53µg/ml respectively. The scavenging of ABTS by leaf and fruit extracts was dose dependent and the IC50 value for leaf and fruit extract was 2.58µg/ml and 2.31µg/ml respectively. Fruit extract was shown to exhibit marked antiradical activity when compared to leaf extract. Leaf and fruit extracts exhibited dose dependent insecticidal activity in terms of larvicidal and pupicidal activity and the susceptibility of larvae and pupae to extracts was in the order II instar larvae>IV instar larvae>pupae. Fruit extract displayed marked insecticidal potential when compared to leaf extract.Conclusion: Overall, fruit extract of G. gummifera exhibited marked antimicrobial, antiradical and insecticidal activity when compared to leaf extract. The plant can be used for developing agents/formulations effective against infectious microorganisms, oxidative stress and insect vectors that transmit dreadful diseases. The observed bioactivities could be ascribed to the presence of active principles which are to be isolated and characterized.


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