scholarly journals In vitro tracheospasmolytic effect and acute toxicity screening of Coptosapelta flavescens Korth root ’s water extract

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 949-954
Author(s):  
Khemasili Kosala ◽  
Sjarif Ismail ◽  
Ika Fikriah ◽  
Yovita Gunawan

There are no data available regarding the bronchospasmolytic activity and toxicity of water extract of Coptosapelta flavescens Korth root (WECFR). Therefore, this study aimed to determine: a. the in vitro tracheospasmolytic effect of WECFR; b. safety of WECFR using the brine shrimp lethality test (BSLT) and immobilization of Daphnia magna larvae (IDL). In study, a guinea pig tracheal ring was contracted with methacholine and cumulative doses of WECFR solution were administered. A dose-response curve (DRC) was plotted of the percentage of the tracheal ring relaxation response. To test whether the relaxation mechanism occured through stimulation of beta2-adrenergic receptors, the tracheal ring was incubated with propranolol. Data analyzed using analysis of variance, showed that the DRC of WECFR was obtained with p < 0.05 compared to the DRC of control, indicating that WECFR had a tracheospasmolytic effect. The DRC for propranolol-blocked WECFR did not shift to the right compared to the DRC of WECFR, confirming that the relaxation mechanism did not occur through the beta2-adrenergic receptors. Study b. assessed safety using BSLT and IDL. After exposing the larvae to WECFR and control for 24 and 48 h, respectively, the number of dead larvae was counted. Data analyzed using Probit program, showed that the lethal dose 50 of WECFR towards Artemia salina and Daphnia magna larvae was > 1000 ppm, which means that it was not toxic. This studies demonstrate that WECFR exhibits tracheospasmolitic effect, but not through beta2-adrenergic receptors; WECFR is safe for Artemia salina and Daphnia magna larvae.

2021 ◽  
Author(s):  
Jéssica Alves Cavalcantea ◽  
Luiz da Silva Maia Neto ◽  
Anna Lígia de Castro Figueiredo ◽  
Weslley Oliveira ◽  
José Roberto Pimentel Cabral de Seixas ◽  
...  

<i>Rhipsalis baccifera</i> (Sol.) Stearn is a typical cactus from tropical regions with wide geographic distribution, and its therapeutic potential is not yet fully understood, such as antitumoral property. Thus, this study evaluated the cytotoxic ethanolic extract of <i>R. baccifera</i> (EERB) and its antitumor activity against Erlich's tumor in mice. The EERB was obtained, and its phytochemical profile was filed by thin-layer chromatography. The toxicity was evaluated in vitro and in vivo using the microcrustacean<i> Artemia salina</i> Leach and mice. The lethal dose was determined after implantation of a tumor cell suspension, with subsequent treatment with EERB (200 mg/kg and 100 mg/kg) 48h after implantation. These values represent the tenth part of the DL<sub>50</sub> and CL<sub>50</sub>, respectively. The presence of phenols, tannins and triterpenes were demonstrated in the phytochemical results. Toxicity was dose-dependent, and the tumor inhibition was 84.1% and 75.8% at doses of 200 mg/kg and 100 mg/kg, respectively. We can highlight that the growth of Erlich's carcinoma suffered inhibitory effects against the EERB. EERB was found to have low acute toxicity and a high potential for use in antitumor therapy. Thus, new studies involving pre-clinical and clinical analyses of the extract are essential to determine the safe dose.


Molecules ◽  
2021 ◽  
Vol 26 (22) ◽  
pp. 6915
Author(s):  
Mustanir Yahya ◽  
Binawati Ginting ◽  
Nurdin Saidi

Increasing production of cocoa (Theobroma cacao L.) leads to a higher environmental burden due to its solid waste generation. Cocoa pod husk, one of the major solid wastes of cocoa production, contains rich bioactive compounds unveiling its valorization potential. With that in mind, our research aimed to explore the biological and antioxidant activities of aqueous extracts from cocoa pod husks. In this present work, cocoa pod husk was extracted using water and subsequentially partitioned using n-hexane, ethyl acetate, and methanol. The antimicrobial investigation revealed that the ethyl acetate solubles were active against the Staphylococcus aureus, Escherichia coli, and Candida albicans, where at a 20% w/v concentration, the inhibition diameters were 6.62 ± 0.10, 6.52 ± 0.02, and 11.72 ± 0.36 mm, respectively. The extracts were found non-toxic proven by brine shrimp lethality tests against Artemia salina with LC50 scores ranging from 74.1 to 19,054.6 μg/mL. The total phenolic content and total flavonoid content were obtained in the range of 47.44 to 570.44 mg/g GAE and 1.96 to 4.34 mg/g QE, respectively. Antioxidant activities of the obtained extracts were revealed by 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) assay with EC50 reached as low as 9.61 μg/mL by the ethyl acetate soluble. Phytochemical screening based on gas chromatography—mass spectroscopy analysis on the sample with the highest antioxidant activities revealed the dominant presence of three phytosterols, namely gamma-sitosterol, stigmasterol, and campesterol.


Author(s):  
Meruyert Akhmetova ◽  
◽  
Razina Ramazanovna Nigmatullina ◽  
Farida Anvarovna Mindubaуeva ◽  
Gulmira Tykezhanova ◽  
...  

In recent years progress has been evident in studies of the importance of serotonin in the physiological and pathological processes of the body and its mechanisms. The role of the serotonin system in the development of diseases such as atherosclerosis, arterial hypertension, and ischemic heart disease is largely discussed. In the myocardium of mammals and humans two types of serotonin receptors (5-HT2 and 5-HT4) have been identified. The activity of the heart is also controlled by the action of catecholamines on the adrenergic receptors of cardiomyocytes. In the implementation of the contraction of cardiomyocytes in the hearts of humans and animals there is also activation of adrenergic receptors, such as β1, β4 and α1A. Serotonin and adrenaline are regulators and modulators of physiological processes in organism, which, under pathological conditions, turn into factors contributing to the development of the disease. In studies on myocardial contractility in vitro in adult rats we found that with an increase in each concentration of serotonin, depending on the dose, a positive inotropic response to the right ventricular myocardium was observed. The effect of serotonin at the last dose on the force of contraction of the right ventricle compared with the first dose increased by 48.3 %. However, with an increase in the dose of epinephrine, the positive inotropic response weakened. At the maximum concentration of 10.0 mM epinephrine, a negative inotropic effect of 10.4 % was observed compared to the previous concentration. Thus, despite the fact that the distribution and functional role of serotonergic receptors in the heart repeats the role of adrenergic receptors, the inotropic response of cardiomyocytes to serotonin and adrenaline is different.


1974 ◽  
Vol 52 (1) ◽  
pp. 74-83 ◽  
Author(s):  
G. W. Higgs ◽  
A. H. Moawad

In order to investigate the phenomenon of "tubal locking" of ova, the in vitro contractility of circular rings from the rabbit oviductal isthmus was examined in different hormonal states. Both alpha and beta adrenergic receptors were found to be present in this preparation with predominance of the alpha receptors when the tissues were from either estrogen- or progesterone-dominant animals.Progesterone treatment of estrogen-primed, immature females influenced the dose–response curve of the circular oviductal muscle to norepinephrine, significantly shifting it to the right, in comparison with tissues from animals that had been treated with estrogen only. There was less of a shift when dose–response relations were determined for phenylephrine after beta receptor blocked with propranolol, suggesting that progesterone enhanced the responses of beta compared with alpha receptors. However, there was still a small difference between responses of estrogen- and progesterone-dominated tissue, at least at low concentrations. Since beta receptor activity had been effectively eliminated, this tendency suggests that progesterone's effect on the response to norepinephrine is not completely due to a modification in beta receptor activity.The spontaneous contractility of tissues from estrogen-treated animals was characterized by a series of rapid spike-like contractions with fairly consistent shape and frequency. Additional treatment with progesterone modified the pattern to an irregular one. Moreover, the total spontaneous activity of muscle from estrogen-dominant animals (as measured by the area under the contractility curve) was significantly reduced, and the rate of tension increase was considerably slower than that from animals with progesterone as the dominant hormone. This indicated a form of antagonism to estrogen by progesterone not involving adrenergic receptors.Maximal excitation of the strips with nonspecific agents or adrenergic agonists resulted in significantly less activity in tissues from progesterone-treated animals. The mechanism of action of progesterone to produce this effect probably involves a step or steps in the excitation–contraction process beyond the adrenergic receptors.


2017 ◽  
Vol 80 (2) ◽  
pp. 245-250 ◽  
Author(s):  
Dalmuri Han ◽  
Hyung Tae Lee ◽  
June Bong Lee ◽  
Yongbaek Kim ◽  
Sang Jong Lee ◽  
...  

ABSTRACT Our previous studies demonstrated that a bioprocessed polysaccharide (BPP) isolated from Lentinus edodes mushroom mycelia cultures supplemented with black rice bran can protect mice against Salmonella lipopolysaccharide–induced endotoxemia and reduce the mortality from Salmonella Typhimurium infection through upregulated T-helper 1 immunity. Here, we report that a BPP from L. edodes mushroom mycelia liquid cultures supplemented with turmeric (referred to as BPP-turmeric) alters chicken macrophage responses against avian-adapted Salmonella Gallinarum and protects chicks against a lethal challenge from Salmonella Gallinarum. In vitro analyses revealed that the water extract of BPP-turmeric (i) changed the protein expression or secretion profile of Salmonella Gallinarum, although it was not bactericidal, (ii) reduced the phagocytic activity of the chicken-derived macrophage cell line HD-11 when infected with Salmonella Gallinarum, and (iii) significantly activated the transcription expression of interleukin (IL)-1β, IL-10, tumor necrosis factor α, and inducible nitric oxide synthase in response to various Salmonella infections, whereas it repressed that of IL-4, IL-6, interferon-β, and interferon-γ. We also found that BPP-turmeric (0.1 g/kg of feed) as a feed additive provided significant protection to 1-day-old chicks infected with a lethal dose of Salmonella Gallinarum. Collectively, these results imply that BPP-turmeric contains biologically active component(s) that protect chicks against Salmonella Gallinarum infection, possibly by regulating macrophage immune responses. Further studies are needed to evaluate the potential efficacy of BPP-turmeric as a livestock feed additive for the preharvest control of fowl typhoid or foodborne salmonellosis.


Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
YC Oh ◽  
YH Jeong ◽  
WK Cho ◽  
SJ Lee ◽  
JY Ma

1991 ◽  
Vol 30 (01) ◽  
pp. 35-39 ◽  
Author(s):  
H. S. Durak ◽  
M. Kitapgi ◽  
B. E. Caner ◽  
R. Senekowitsch ◽  
M. T. Ercan

Vitamin K4 was labelled with 99mTc with an efficiency higher than 97%. The compound was stable up to 24 h at room temperature, and its biodistribution in NMRI mice indicated its in vivo stability. Blood radioactivity levels were high over a wide range. 10% of the injected activity remained in blood after 24 h. Excretion was mostly via kidneys. Only the liver and kidneys concentrated appreciable amounts of radioactivity. Testis/soft tissue ratios were 1.4 and 1.57 at 6 and 24 h, respectively. Testis/blood ratios were lower than 1. In vitro studies with mouse blood indicated that 33.9 ±9.6% of the radioactivity was associated with RBCs; it was washed out almost completely with saline. Protein binding was 28.7 ±6.3% as determined by TCA precipitation. Blood clearance of 99mTc-l<4 in normal subjects showed a slow decrease of radioactivity, reaching a plateau after 16 h at 20% of the injected activity. In scintigraphic images in men the testes could be well visualized. The right/left testis ratio was 1.08 ±0.13. Testis/soft tissue and testis/blood activity ratios were highest at 3 h. These ratios were higher than those obtained with pertechnetate at 20 min post injection.99mTc-l<4 appears to be a promising radiopharmaceutical for the scintigraphic visualization of testes.


1997 ◽  
Vol 77 (02) ◽  
pp. 376-382 ◽  
Author(s):  
Bruce Lages ◽  
Harvey J Weiss

SummaryThe possible involvement of secreted platelet substances in agonist- induced [Ca2+]i increases was investigated by comparing these increases in aspirin-treated, fura-2-loaded normal platelets and platelets from patients with storage pool deficiencies (SPD). In the presence and absence of extracellular calcium, the [Ca2+]i response induced by 10 µM ADP, but not those induced by 0.1 unit/ml thrombin, 3.3 µM U46619, or 20 µM serotonin, was significantly greater in SPD platelets than in normal platelets, and was increased to the greatest extent in SPD patients with Hermansky-Pudlak syndrome (HPS), in whom the dense granule deficiencies are the most severe. Pre-incubation of SPD-HPS and normal platelets with 0.005-5 µM ADP produced a dose-dependent inhibition of the [Ca2+]i response induced by 10 µ M ADP, but did not alter the [Ca2+]i increases induced by thrombin or U46619. Within a limited range of ADP concentrations, the dose-inhibition curve of the [Ca2+]i response to 10 µM ADP was significantly shifted to the right in SPD-HPS platelets, indicating that pre-incubation with greater amounts of ADP were required to achieve the same extent of inhibition as in normal platelets. These results are consistent with a hypothesis that the smaller ADP-induced [Ca2+]i increases seen in normal platelets may result from prior interactions of dense granule ADP, released via leakage or low levels of activation, with membrane ADP receptors, causing receptor desensitization. Addition of apyrase to platelet-rich plasma prior to fura-2 loading increased the ADP-induced [Ca2+]i response in both normal and SPD-HPS platelets, suggesting that some release of ADP derived from both dense granule and non-granular sources occurs during in vitro fura-2 loading and platelet washing procedures. However, this [Ca2+]i response was also greater in SPD-HPS platelets when blood was collected with minimal manipulation directly into anticoagulant containing apyrase, raising the possibility that release of dense granule ADP resulting in receptor desensitization may also occur in vivo. Thus, in addition to enhancing platelet activation, dense granule ADP could also act to limit the ADP-mediated reactivity of platelets exposed in vivo to low levels of stimulation.


Author(s):  
Nurgozhin T. ◽  
Sergazy S. H. ◽  
Adilgozhina G. ◽  
Gulyayev A. ◽  
Shulgau Z. ◽  
...  

Objective:This study investigates the hepatoprotective effect and the antioxidant role of polyphenol concentrate in the experimental model of carbon tetrachloride (CCl4) induced toxicity. Methods: Antioxidant activity of Cabernet Sauvignon grape polyphenol were evaluated by radical scavenging of 1,1-diphenyl-2-picryl hydrazyl radical (DPPH), 2,2’-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS.+). In addition, the effects of polyphenol concentrate on the survival of Wistar rats in the toxicity model, was also investigated. The polyphenol concentrate was administered for 5 five days prior to injection of carbon tetrachloride in a sub-lethal dose of 300 mg/kg of animal body weight in order to perform histological examinations of the liver and kidney, and detect the levels of AST, ALT and bilirubin. Results: Administration of polyphenol concentrate increased animal survival in the experimental model. Moreover, the intragastric administration of polyphenol concentrate prior to the initiation of the experimental model of toxicity, which was caused by a sub-lethal CCl4 dose, reduced morphological injuries in the liver and kidney, decreased the AST and ALT levels of the blood serum. Discussion and conclusion: Our data demonstrate that polyphenol concentrate possesses an antioxidant potential both in vitro and in vivo by reducing antioxidant stress that was caused by CCl4 administration into rats.


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