scholarly journals Inhibitory Effect of PlantManilkara subsericeaagainst Biological Activities ofLachesis mutaSnake Venom

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Eduardo Coriolano De Oliveira ◽  
Caio Pinho Fernandes ◽  
Eladio Flores Sanchez ◽  
Leandro Rocha ◽  
André Lopes Fuly

Snake venom is composed of a mixture of substances that caused in victims a variety of pathophysiological effects. Besides antivenom, literature has described plants able to inhibit injuries and lethal activities induced by snake venoms. This work describes the inhibitory potential of ethanol, hexane, ethyl acetate, or dichloromethane extracts and fractions from stem and leaves ofManilkara subsericeaagainstin vivo(hemorrhagic and edema) andin vitro(clotting, hemolysis, and proteolysis) activities caused byLachesis mutavenom. All the tested activities were totally or at least partially reduced byM. subsericea. However, whenL. mutavenom was injected into mice 15 min first or after the materials, hemorrhage and edema were not inhibited. Thus,M. subsericeacould be used as antivenom in snakebites ofL. muta. And, this work also highlights Brazilian flora as a rich source of molecules with antivenom properties.

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Thaisa F. S. Domingos ◽  
Laura de A. Moura ◽  
Carla Carvalho ◽  
Vinícius R. Campos ◽  
Alessandro K. Jordão ◽  
...  

Snake venoms are complex mixtures of proteins of both enzymes and nonenzymes, which are responsible for producing several biological effects. Human envenomation by snake bites particularly those of the viperid family induces a complex pathophysiological picture characterized by spectacular changes in hemostasis and frequently hemorrhage is also seen. The present work reports the ability of six of a series of 1,2,3-triazole derivatives to inhibit some pharmacological effects caused by the venoms ofBothrops jararacaandLachesis muta.In vitroassays showed that these compounds were impaired in a concentration-dependent manner, the fibrinogen or plasma clotting, hemolysis, and proteolysis produced by both venoms. Moreover, these compounds inhibited biological effectsin vivoas well. Mice treated with these compounds were fully protected from hemorrhagic lesions caused by such venoms. But, only theB. jararacaedema-inducing activity was neutralized by the triazoles. So the inhibitory effect of triazoles derivatives against somein vitroandin vivobiological assays of snake venoms points to promising aspects that may indicate them as molecular models to improve the production of effective antivenom or to complement antivenom neutralization, especially the local pathological effects, which are partially neutralized by antivenoms.


2018 ◽  
Vol 2018 ◽  
pp. 1-14 ◽  
Author(s):  
Ameur Ben Younes ◽  
Maryem Ben Salem ◽  
Hanen El Abed ◽  
Raoudha Jarraya

Background. This study investigates the biological activities ofAnthyllis henonianaflowers extracts.Materials and Methods. Antioxidant activity and thein vitroinhibitory effect of key digesting enzymes related to postprandial hyperglycemia were determined. Diabetic rats were orally and daily given the best extract from flowers ofAnthyllis henonianaat a dose of acarbose for one month.Results. Among the extracts, the ethyl acetate one displayed remarkable antioxidant activity including DPPH (IC50= 2.34 mg/mL) and was more effective in inhibitingα-glucosidase (IC50= 17μg/mL) thanα-amylase (IC50= 920μg /mL) activities.In vivo, the results proved that ethyl acetate extract at doses of 400 mg/kg bw decreased significantly the blood glucose level and lipid profile levels and increased the activities of antioxidant enzymes. These protective impacts ofAnthyllis henonianaethyl acetate flowers extract were confirmed by histological results.Conclusion. This study demonstrates, for the first time, thatAnthyllis henonianaflowers ethyl acetate extract is effective in inhibiting hyperglycemia and oxidative stress caused by diabetes.


2021 ◽  
Vol 16 (10) ◽  
pp. 1934578X2110559
Author(s):  
Le Minh Ha ◽  
Ngo Thi Phuong ◽  
Nguyen Thi Thu Hien ◽  
Pham Thi Tam ◽  
Do Thi Thao ◽  
...  

In this study, we aimed at evaluating in vitro and in vivo anti-inflammatory activity of various extracts of the rhizomes of Globba pendula Roxb. Three extracts ( n-hexane, ethyl acetate, and water) were screened for their inhibitory effect on NO production by lipopolysaccharide-stimulated RAW 264.7 macrophages. The ethyl acetate extract of G. pendula rhizomes (EGP) showed a potential effect with an IC50 value of 32.45 µg/mL. For in vivo study, the ethyl acetate extract was further investigated for its anti-inflammatory effect using collagen antibody-induced arthritic mice (CAIA). The level of arthritis in experimental mice significantly reduced ( P < .05) after treatment with EGP at a dose of 500 mg/kg body weight (b.w.). This study also revealed that EGP is orally non-toxic. Ethyl p-methoxy cinamate was identified as the main constituent of EGP, which may result in its anti-inflammatory effect.


1997 ◽  
Vol 273 (6) ◽  
pp. E1127-E1132 ◽  
Author(s):  
Pascal Fragner ◽  
Olivier Presset ◽  
Nicole Bernad ◽  
Jean Martinez ◽  
Claude Roze ◽  
...  

The tripeptide pyro-Glu-His-Pro-NH2[thyrotropin-releasing hormone (TRH)] was isolated from the hypothalamus as a thyrotropin-releasing factor. It has a broad spectrum of central nervous system-mediated actions, including the stimulation of exocrine pancreatic secretion. TRH is also synthesized in the endocrine pancreas and found in the systemic circulation. Enzymatic degradation of TRH in vivo produces other bioactive peptides such as cyclo(His-Pro). Because of the short half-life of TRH and the stability of cyclo(His-Pro) in vivo, we postulated that at least part of the peripheral TRH effects on the exocrine pancreatic secretion may be attributed to cyclo(His-Pro), which has been shown to have other biological activities. This study determines in parallel the peripheral effects of TRH and cyclo(His-Pro) as well as the putative contribution of other TRH-related peptides on exocrine pancreatic secretion in rats. TRH and its metabolite cyclo(His-Pro) dose dependently inhibited 2-deoxy-d-glucose (2-DG)-stimulated pancreatic secretion. TRH and all the related peptides tested had no effect on the basal and cholecystokinin-stimulated amylase release from pancreatic acinar cells in vitro. These data indicate that cyclo(His-Pro) mimics the peripheral inhibitory effect of TRH on 2-DG-stimulated exocrine pancreatic secretion. This effect is not detected on isolated pancreatic acini. Our findings provide a new biological contribution for cyclo(His-Pro) with potential experimental and clinical applications.


2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Neuza Mariko Aymoto Hassimotto ◽  
Vanessa Moreira ◽  
Neide Galvão do Nascimento ◽  
Pollyana Cristina Maggio de Castro Souto ◽  
Catarina Teixeira ◽  
...  

Anthocyanins are flavonoids which demonstrated biological activities inin vivoandin vitromodels. Here in the anti-inflammatory properties of an anthocyanin-enriched fraction (AF) extracted from wild mulberry and the cyanidin-3-glucoside (C3G), the most abundant anthocyanin in diet, were studied in two acute inflammation experimental models, in the peritonitis and in the paw oedema assays, both of which were induced by carrageenan (cg) in mice. In each trial, AF and C3G (4 mg/100 g/animal) were orally administered in two distinct protocols: 30 min before and 1 h after cg stimulus. The administration of both AF and C3G suppresses the paw oedema in both administration times (P<0.05). In the peritonitis, AF and C3G reduced the polymorphonuclear leukocytes (PMN) influx in the peritoneal exudates when administered 1 h after cg injection. AF was more efficient reducing the PMN when administered 30 min before cg. Both AF and C3G were found to suppress mRNA as well as protein levels of COX-2 upregulated by cg in both protocols, but the inhibitory effect on PGE2production in the peritoneal exudates was observed when administered 30 min before cg (P<0.05). Our findings suggest that AF and C3G minimize acute inflammation and they present positive contributions as dietary supplements.


2021 ◽  
Vol 10 (1) ◽  
pp. 230-245
Author(s):  
Fahad A. Alhumaydhi ◽  
Ibrahim Khan ◽  
Abdur Rauf ◽  
Muhammad Nasimullah Qureshi ◽  
Abdullah S. M. Aljohani ◽  
...  

Abstract Currently, nanotechnology is gaining massive attention compared to conventional methods as the biosynthesis of plant-based nanoparticles is considered safe, effective, and ecofriendly. Therefore, keeping in view the importance of nanotechnology, the present study was designed to synthesize, characterize, and evaluate the biological effectiveness of saffron stigma-based gold nanoparticles (SS-AuNPs) for their in vitro and in vivo biological properties. These gold nanoparticles were characterized by UV–Vis spectroscopy, Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), energy-dispersive X-ray spectroscopy (EDX), and X-ray diffraction (XRD). The highest antibacterial effect was observed by the saffron extract against Escherichia coli (22 mm). SS-AuNPs significantly inhibited the activity of enzyme urease (54.98%) and CA-II (64.29%). However, the nonsignificant inhibitory effect was observed in the case of α-chymotrypsin. Maximum analgesic (84.98%) and antiinflammatory (88.98%) effects were observed for SS-AuNPs (10 mg/kg). Similarly, SS-AuNPs demonstrated a significant (P < 0.01) sedative effect at all tested doses.


Author(s):  
Ibrahim Sani ◽  
Rabi’u Aliyu Umar ◽  
Sanusi Wara Hassan ◽  
Umar Zaki Faruq ◽  
Fatima Bello ◽  
...  

Snake venom enzymes are the key substances involved in snake venom toxicity. Thus, inactivating these enzymes is generally considered to be the fundamental step in the management of snakebite. Conventionally, snakebite envenomation is treated parenterally with serum-based antivenins, and adjuvants to these antivenins are required for maximum protection of victims. Hence, this research was aimed at evaluating the inhibitory effect of Azadirachta indica leaf extracts on Naja nigricollis Reinhardt venom enzymes and screens for their antivenom adjuvant effects. A. indica leaf was collected, authenticated and extracted using 95% methanol followed by fractionation using hexane and ethyl acetate. The venom enzymes inhibition assays was evaluated using in vitro methods, while, adjuvant effect was screened using Albino rats. The results revealed that both the hexane and the ethyl acetate fractions showed capability of inhibiting the venom enzymes significantly (P<0.05) when compared with the venom controls in varying degrees of efficacies. For the adjuvant effect, no significant effect (P>0.05) of the venom at the administered dose was observed on bleeding time, clotting time, defibrinogenating and haemorrhagic effects compared to the normal control. However, the size of necrotic lesion and the percentage haemolysis were significantly (P<0.05) higher in the venom control rats. Both the hexane and the ethyl acetate fractions significantly mitigated these effects in the treated animals. The degree of protection was about 3 folds more than when the antivenin was used alone. Finally, these findings would be of importance in the area of drug development with a view to actualizing the substitution or enhancing the effect of conventional snakebite therapeutic options.


2021 ◽  
Author(s):  
Ziyan Xu ◽  
Liru Huang ◽  
Tiantian Zhang ◽  
Yuwei Liu ◽  
Mei Gong ◽  
...  

Abstract Cervical cancer is one of the most common female cancers worldwide, and it is one of the most lethal malignancies of the female reproductive system. Shikonin, a natural pigment of theophyllin, has a variety of biological activities and has shown significant inhibitory effects on a variety of tumours in vitro and in vivo. However, there are few studies on Shikonin in cervical cancer. In the present study, we found that Shikonin inhibited not only the proliferation but also the migration of cervical cancer cells. Our data showed that Shikonin inhibited the proliferation of HeLa and SiHa cells in a concentration- and time-dependent manner. In cervical cancer cells, Shikonin not only inhibited the phosphorylation of FAK, AKT and GSK3β but also inhibited the phosphorylation of FAK, AKT and GSK3β induced by EGF. Further exploring the mechanism, we found that Shikonin could inhibit the proliferation of cervical cancer cells by regulating the phosphorylation of the FAK/AKT/GSK3β pathway. In addition, Shikonin significantly inhibited cell migration and reduced the expression of proteins such as MTA1, TGFβ1 and VEGF. In conclusion, our study elucidated that Shikonin has an inhibitory effect on the proliferation and migration of cervical cancer cells, which may be mediated by the FAK/AKT/GSK3β signalling pathway. Our results suggest that Shikonin has the potential to become a clinical treatment for cervical cancer.


Biomolecules ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 758
Author(s):  
Tiyyaba Furqan ◽  
Sidra Batool ◽  
Rabia Habib ◽  
Mamoona Shah ◽  
Huba Kalasz ◽  
...  

The study documented here was aimed to find the molecular interactions of some of the cannabinoid constituents of cannabis with acetylcholinesterase (AChE). Molecular docking and LogP determination were performed to predict the AChE inhibitory effect and lipophilicity. AChE enzyme activity was measured in the blood of cannabis addicted human subjects. Further, genetic predisposition to cannabis addiction was investigated by association analysis of cannabinoid receptor 1 (CNR1) single nucleotide polymorphism (SNP) rs806368 and ACHE rs17228602 using restriction fragment length polymorphism (RFLP) method. All the understudied cannabis constituents showed promising binding affinities with AChE and are lipophilic in nature. The AChE activity was observed to be indifferent in cannabis addicted and non-addicted healthy controls. There was no significant association with CNR1 SNP rs806368 and ACHE rs17228602. The study concludes that in silico prediction for individual biomolecules of cannabis is different from in vivo physiological action in human subjects when all are present together. However, for a deeper mechanistic insight into these interactions and association, multi-population studies are suggested. Further studies to explore the inhibitory potential of different cannabis constituents for intended AChE inhibitor-based drug are warranted.


Toxins ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 240
Author(s):  
Christoffer V. Sørensen ◽  
Cecilie Knudsen ◽  
Ulrich auf dem Keller ◽  
Konstantinos Kalogeropoulos ◽  
Cristina Gutiérrez-Jiménez ◽  
...  

Antibiotics are often administered with antivenom following snakebite envenomings in order to avoid secondary bacterial infections. However, to this date, no studies have evaluated whether antibiotics may have undesirable potentiating effects on snake venom. Herein, we demonstrate that four commonly used antibiotics affect the enzymatic activities of proteolytic snake venom toxins in two different in vitro assays. Similar findings in vivo could have clinical implications for snakebite management and require further examination.


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