scholarly journals The Gastrointestinal Irritation of Polygala Saponins and Its Potential Mechanism In Vitro and In Vivo

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Li Wen ◽  
Nan Xia ◽  
PeiPei Tang ◽  
Yi Hong ◽  
ZiZhen Wang ◽  
...  
Keyword(s):  
Pharmacological Activity ◽  
Gastrointestinal Toxicity ◽  
Potential Mechanism ◽  
Gut Motility ◽  
Sleeping Time ◽  
Sedative Activity

Processing alters the pharmacological activity and reduces the gastrointestinal toxicity of the polygalae. To investigate the effect of processing, different glycosyl substituent products were tested. Hypnotic and subhypnotic doses of pentobarbital-induced sleep tests on mice were used to evaluate the sedative activity of polygala saponins with different glycosyl substituents; isolated gut motility experiment was employed to study excitatory effects of different polygala saponins; the gastrointestinal irritation effects of different polygala saponins were compared by measuring the levels of gastric PGE2 and intestinal TNF-αon mice. When compared with control, Onjisaponin B (OJB) and tenuifolin (TEN), but not senegenin (SNG), significantly increased the number of sleeping mice and prolonged the sleeping time (P<0.05); 80, 40, and 20 mg/L of OJB and 80 mg/L of TEN, but not SNG, obviously changed the amplitude and frequency of isolated jejunum (P<0.05); all the three compounds significantly decreased the level of gastric PGE2 but had no obvious influences on the reduction of intestinal TNF-αlevel. For sedative and hypnotic effects, OJB > TEN > SNG; for the protection form gastrointestinal irritation and damages, OJB > TEN > SNG. Therefore, in processing Polygala, glycosyl breaking may be related to the decline of pharmacological activity and gastrointestinal toxicity of polygala saponins.

scholarly journals Active Substances from Callicarpa nudiflora Exert Anti-Cervicitis Effects and Regulate NLRP3-Associated Inflammation

Molecules ◽  
2021 ◽  
Vol 26 (20) ◽  
pp. 6217
Author(s):  
Tianchi Liu ◽  
Ruiqi Wang ◽  
Chenpeng Liu ◽  
Jiahong Lu ◽  
Yitao Wang ◽  
...  
Keyword(s):  
Chinese Medicine ◽  
Ethanol Extract ◽  
Inflammatory Factor ◽  
Potential Mechanism ◽  
Active Components ◽  
New Agents ◽  
Scientific Support ◽  
Active Substances

Luohuazizhu suppository is a Traditional Chinese Medicine used in clinic to treat cervicitis, which is prepared from Callicarpa nudiflora Hook. et Arn (C. nudiflora), an herbal Chinese medicine named Luohuazizhu. This study aimed to figure out the active constituents of C. nudiflora and the potential mechanism for its anti-cervicitis effect. The ethanol extract in C. nudiflora (CNE) and the different fractions of CNE extracted by petroleum ether (CNE-p), dichloromethane (CNE-d), and n-butanol (CNE-b) were tested in vivo for their anti-cervicitis effects. Then the isolated compounds from the CNE-p were tested in vitro for their anti-inflammatory activities. The results displayed that CNE-p, CNE-d, and CNE-b exhibited adequate anti-cervicitis effects, with CNE-p showing the highest efficacy. Further experiment demonstrated that CNE-p could significantly inhibit the expression of NLRP3 in vitro. Six diterpenoids obtained from the CNE-p showed the ability to regulate inflammatory factor levels in vitro. Among these compounds, compounds 1 (callicarpic acid A) and 2 (syn-3,4-seco-12S-hydroxy-15,16-epoxy-4(18),8(17),3(16),14(15)-labdatetraen-3-oic acid) were the most effective agents, and they also inhibited the expression level of NLRP3 in vitro. The results confirmed that C. nudiflora has significant anti-cervicitis effects and the diterpenoids were most likely to be its active components. These data provide scientific support for the clinic usage of Luohuazizhu suppository and the development of new agents in treating cervicitis.

scholarly journals Evaluation of In vitro Antioxidant and In vivo Pharmacological Activity of Leaf Extracts of Hoya parasitica (Wall.)

2016 ◽  
pp. 163-170
Author(s):  
Ummee Tania ◽  
Md Hassan ◽  
Nusrat Eshita ◽  
Rumana Akhter ◽  
Mohammad Shahriar
Keyword(s):  
Pharmacological Activity ◽  
Leaf Extracts

scholarly journals Garcinoic Acid Improves Cardiac Function and Enhances Angiogenesis Following Myocardial Infarction

2021 ◽  
Author(s):  
Hongyao Hu ◽  
Wei Li ◽  
Yanzhao Wei ◽  
Hui Zhao ◽  
Zhenzhong Wu ◽  
...  
Keyword(s):  
Myocardial Infarction ◽  
Cardiac Function ◽  
Ventricular Remodeling ◽  
Vehicle Group ◽  
Potential Mechanism ◽  
Garcinia Kola ◽  
Angiogenic Proteins

Abstract Cardiac ischemia impairs angiogenesis in response to hypoxia, resulting in ventricular remodeling. Garcinoic acid (GA), the extraction from the plant garcinia kola, is validated to attenuate inflammatory response. However, the role of GA in heart failure (HF) and neovascularization after myocardial infarction (MI) is incompletely understood. The present study is striving to explore the role of GA and the potential mechanism of which in cardiac function after MI. SD rats were randomized into sham group, MI+vehicle group, and MI+GA group in vivo. Human umbilical endothelial cells (HUVECs) were cultured in vehicle or GA, and then additionally exposed to 2% hypoxia environment in vitro. MI rats displayed a dramatically reduced myocardial injury, cardiac function and vessel density in the peri-infarcted areas. GA delivery markedly improved cardiac performance and promoted angiogenesis. In addition, GA significantly enhanced tube formation in HUVECs under hypoxia condition. Furthermore, the expressions of pro-angiogenic factors HIF-1α, VEGF-A and bFGF, and pro-angiogenic proteins phospho-VEGFR2Tyr1175 and VEGFR2, as well as phosphorylation levels of Akt and eNOS were increased by GA treatment. In conclusion, GA preserved cardiac function after MI probably via promoting neovascularization. And the potential mechanism may be partially through upregulating the expressions of HIF-1α, VEGF-A, bFGF, phospho-VEGFR2Tyr1175 and VEGFR2 and activating the phosphorylations of Akt and eNOS.

CircRNA_0092516 regulates chondrocyte proliferation and apoptosis in osteoarthritis through the miR-337-3p/PTEN axis

2020 ◽  
Author(s):  
Zhihui Huang ◽  
Wenming Ma ◽  
Jinhuai Xiao ◽  
Xiaoyu Dai ◽  
Weiqi Ling
Keyword(s):  
Cell Apoptosis ◽  
Luciferase Reporter ◽  
Circular Rnas ◽  
Mechanism Analysis ◽  
Potential Mechanism ◽  
Luciferase Reporter Gene ◽  
Chondrocyte Proliferation ◽  
In Vivo Experiments

Abstract The dysregulation of circular RNAs (circRNAs) has been identified in various human diseases. Here, we probed into the potential mechanism of circRNA_0092516 in osteoarthritis (OA). The expression of circRNA_0092516 was tested by quantitative real-time PCR. MTT, flow cytometry and western blot were applied to confirm the functions of circRNA_0092516 in vitro. Besides, RNA pull-down and dual-luciferase reporter gene experiments were applied to probe into the mechanism. circRNA_0092516 was raised in the tissues of OA patients and chondrocytes stimulated by IL-1β. The potential mechanism analysis expounded that circRNA_0092516 bound to miR-337-3p, and the interference with circRNA_0092516 boosted chondrocyte proliferation and restrained cell apoptosis through the miR-337-3p/phosphatase and tensin homolog (PTEN) axis, thereby improving OA. In-vivo experiments expounded that circRNA_0092516 regulated cartilage production through miR-337-3p. Overall, our data expounded that the interference with circRNA_0092516 boosted chondrocyte proliferation and restrained cell apoptosis through the miR-337-3p/PTEN axis, eventually slowed down the progress of OA.

scholarly journals In vitro and in vivo antineoplastic activity of a novel bromopyrrole and its potential mechanism of action

2010 ◽  
Vol 159 (4) ◽  
pp. 909-918 ◽  
Author(s):  
Sheng Xiong ◽  
Hui-dan Pang ◽  
Jun Fan ◽  
Feng Ge ◽  
Xiao-xia Yang ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Antineoplastic Activity ◽  
Potential Mechanism

The in vivo and in vitro study of polysaccharides from a two-herb formula on ulcerative colitis and potential mechanism of action

2014 ◽  
Vol 153 (1) ◽  
pp. 151-159 ◽  
Author(s):  
Linjing Zhao ◽  
Hongbing Wu ◽  
Aihua Zhao ◽  
Huili Lu ◽  
Wei Sun ◽  
...  
Keyword(s):  
Ulcerative Colitis ◽  
Mechanism Of Action ◽  
In Vitro Study ◽  
Vitro Study ◽  
Potential Mechanism

scholarly journals Inhibitory Effects of Apigenin on Tumor Carcinogenesis by Altering the Gut Microbiota

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Shichang Bian ◽  
Hongjuan Wan ◽  
Xinyan Liao ◽  
Weisheng Wang
Keyword(s):  
Colon Cancer ◽  
Treatment Group ◽  
16S Rrna ◽  
Gut Microbiota ◽  
High Throughput Sequencing ◽  
Potential Mechanism ◽  
Inhibitory Effects ◽  
Antitumor Effects

The flavonoid apigenin is common to many plants. Although the responsible mechanisms have yet to be elucidated, apigenin demonstrates tumor suppression in vitro and in vivo. This study uses an azoxymethane (AOM)/dextran sodium sulfate- (DSS-) induced colon cancer mouse model to investigate apigenin’s potential mechanism of action exerted through its effects upon gut microbiota. The size and quantity of tumors were reduced significantly in the apigenin treatment group. Using 16S rRNA high-throughput sequencing of fecal samples, the composition of gut microbiota was significantly affected by apigenin. Further experiments in which gut microbiota were reduced and feces were transplanted provided further evidence of apigenin-modulated gut microbiota exerting antitumor effects. Apigenin was unable to reduce the number or size of tumors when gut microbiota were depleted. Moreover, tumor inhibition effects were initiated following the transplant of feces from mice treated with apigenin. Our findings suggest that the effect of apigenin on the composition of gut microbiota can suppress tumors.

Inhibitory effects of H2-receptor antagonists on cytochrome P450 in male ICR mice

1995 ◽  
Vol 14 (8) ◽  
pp. 623-629 ◽  
Author(s):  
DH Kim ◽  
EJ Kim ◽  
SS Han ◽  
JK Roh ◽  
TC Jeong ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Liver Microsomes ◽  
Receptor Antagonists ◽  
Sleeping Time ◽  
Icr Mice ◽  
In Vitro Effects ◽  
Hexobarbital Metabolism ◽  
Dose Dependent

1 The present study was undertaken to examine the effects of H2-receptor antagonists including newly developed mifentidine derivatives, IY-80843 and IY-80845, on cytochrome P450(P450) in vitro and in vivo. 2 Initially, 3-methylcholanthrene-, phenobarbital-, ethanol- and dexamethasone-induced liver microsomes were prepared from male ICR mice to study in vitro effects of above chemicals on ethoxyresorufin O- deethylase(EROD), pentoxyresorufin O-dealkylase(PROD), p-nitrophenol hydroxylase and erythromycin N-demethy lase(ERDM) activities, respectively. It was found that hist amine, cimetidine and famotidine were not inhibitory to four enzyme activities. Meanwhile, mifentidine slightly inhibited EROD and PROD activities and its derivatives IY-80843 and IY-80845 strongly inhibited PROD, EROD and ERDM activities. 3 Prolongation of hexobarbital-induced sleeping time was determined in male ICR mice to confirm in vitro inhibito ry effects of mifentidine and its derivatives in vivo. It was observed that cimetidine, mifentidine, IY-80843 and IY- 80845 caused dose-dependent increases in the sleeping time, indicating the inhibition of P450 responsible for hexobarbital metabolism. 4 It was concluded that mifentidine and its derivatives are P450 inhibitors and that our newly synthesized IY-80843 is most inhibitory. 5 The present results indicate that mifentidine and its derivatives not only antagonise the H 2-receptor but also inhibit P450 enzymes.

A Study of the Effect of Ovex on Parathion Toxicity in Rats

1973 ◽  
Vol 51 (9) ◽  
pp. 682-685 ◽  
Author(s):  
W. D. Black ◽  
A. E. Wade ◽  
R. B. Talbot
Keyword(s):  
Oral Administration ◽  
Liver Size ◽  
Sleeping Time ◽  
Hexobarbital Sleeping Time ◽  
Organophosphate Toxicity ◽  
Naphthyl Acetate

Oral administration (100 mg/kg) of the miticide ovex (p-chlorophenyl p-chlorobenzene-sulfonate) caused a decrease in the hexobarbital sleeping time of rats. Administration of this same dosage of ovex resulted in a significant decrease in the toxicity of orally administered parathion (100 mg/kg) to rats.The changes in rats noted in conjunction with the increased resistance to organophosphate toxicity in vivo were an increased liver size, an increased rate of in vitro α-naphthyl acetate hydrolysis by the 9000 × g liver supernatant.The hexane-extractable organophosphate detected in the liver of the ovex-pretreated rats was significantly lower than the hexane extractable organophosphate found in the liver of the control rats.

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