scholarly journals Identification of the Anti-sickling Activity of Anogeissus leiocarpus and In Silico Investigation of Some of Its Phytochemicals

2020 ◽  
Vol 8 (1) ◽  
pp. 1-14
Author(s):  
Taiwo O. Elufioye ◽  
Babatunde M. Williams ◽  
Mojisola C. Cyrl-Olutayo

Background: The anti-sickling activity of Anogeissus leiocarpus, a plant used for managing sickle cell disease (SCD), has been previously proven. Objectives: This study investigated the anti-sickling mechanism of A. leiocarpus by probing its effects on Gardos channel (KCNN4), erythropoietin (EPO), erythropoietin receptor (EPOR), catalase (CAT), G6pD, D-type cyclins and cyclin-dependent kinase inhibitors (p21) gene expression as well as assessing in silico drug-likeness of reported compounds as EPOR agonist. Methods: A total of 18 rats (45-76 g) were selected and divided into 6 groups (n=3). The control group was given water ad libitum, standard group was given 0.1 mL/kg of Ciklavit® and experimental group was given daily oral doses of 50-100 mg/kg body weight of crude methanol extract or ethyl acetate fraction (EA-PF). Haematological parameters were analyzed while histopathological and molecular studies of kidney and bone marrow were carried out, followed by RT-PCR analysis of KCNN4, EPO, EPOR, CAT, G6pD, p21, and cyclin-dependent kinase inhibitors. Docking studies of the reported compounds were also done. Results: EA-PF had an insignificant (P>0.05) effect on haematological parameters compared to the basal group. While CAT and p21 acted in a positive feedback loop, G6pD was downregulated in the experimental groups. KCNN4 acted in a negative-feedback mechanism and the upregulation of EPO and EPOR was followed by increased reticulocytes. Kaempferol, quercetin, and catechin showed non-violation of Lipinski’s rule and high binding affinities of 6.5 kcal/mol, 6.7 kcal/mol, and 6.7 kcal/mol, respectively, for EPOR pocket compared to the co-crystallized ligand. Conclusion: Results suggest that ethyl acetate fraction of Anogeissus leiocarpus achieved a steady state level of the Gardos channel and stimulation of EPO expression via EPOR agonist.

Author(s):  
Hendrika Andriana Silitonga ◽  
◽  
Gontar Alamsyah Siregar ◽  
Rosita Juwita Sembiring ◽  
Marline Nainggolan ◽  
...  

ABSTRACT Background: Recent studies showed that Interleukin-8 (IL-8), activated cytokine immune response which plays an important role in the development of acute and chronic gastritis. Harmless anti-inflammatory therapeutic alternatives have been proposed, for example, the consumption of Sechium Edule Jacq. Swartz (chayote). Antioxidant (flavonoid) and cell regeneration (alkaloid) agents were found in chayote. This study aimed to determine the effect of chayote Sechium Edule Jacq. Swartz extracts on the level of IL-8 in Wistar rats with aspirin- induced gastritis. Subjects and Method: This was a randomized controlled trial (RCT) conducted at the laboratory of Mathematics and Natural Science, Universitas Sumatra Utara from January to February 2020. A total of 35 male Wistar rats was selected for this study and randomly allocated into 7 groups: (1) Negative control; (2) Positive control; (3) 100 mg/ kg BW chayote ethanol extract ; (4) 200 mg/kg BW chayote ethanol extract; (5) 100 mg/ kg BW chayote ethyl acetate fraction; (6) 200 mg/kg BW chayote ethyl acetate fraction; and (7) 20 mg omeprazole. The rats in positive control and treatment groups were induced with aspirin (200mg/ kg BW). The negative control group received no intervention. The dependent variable was level of IL-8 measured by ELISA. The independent variables were treatment status. The data were analyzed by One Way Anova and post hoc test. Results: The mean differences of IL-8 level were not statistically significant between study groups (p= 0.327). Mean of IL-8 level was higher in positive control group (Mean= 160.80; SD= 6.90) than in negative control group (Mean= 141.20; SD= 10.98). The lowest IL-8 level was in 100mg/ kg BW chayote ethanol extract group (Mean= 149.94; SD= 40.4), followed by 200mg/ kg BW (Mean= 152.4; SD= 30.73) and 100mg/ kg BW (Mean= 164.60; SD= 25.04) chayote ethyl acetate fraction groups, 20 mg omeprazole group (Mean= 170.60; SD= 21.58), and 200 mg/ kg BW chayote ethanol extract group (Mean= 176.80; SD= 10.98). Conclusion: The low dose (100mg/ kg BW) chayote ethanol extract has the most potential antiinflammation effect on in vitro gastritis with the lowest IL-8 level of all doses of chayote ethanol extract, chayote ethyl acetate fraction, and omeprazole. Keywords: antiinflammation, IL-8, chayote ethanol extract, ethyl acetate fraction, omeprazole, aspirin induced gastritis Correspondence: Hendrika Andriana Silitonga. Department of Histology, Faculty of Medicine, Universitas Methodist Indonesia. Email: [email protected]. Mobile: +6281361430688. DOI: https://doi.org/10.26911/the7thicph.05.35


2018 ◽  
Vol 51 (4) ◽  
pp. 164
Author(s):  
K. Khairiah ◽  
Irham Taufiqurrahman ◽  
Deby Kania Tri Putri

Background: Binjai (Mangifera caesia) is a herb derived from South Kalimantan possessing antioxidant properties which promote wound healing inhibiting oxidation radicals. The natural antioxidants present in binjai leaves can be extracted by fractionation. Purpose: This study aimed to analyze the antioxidant activity of ethyl acetate fraction in 96% ethanol extract of binjai leaf. Methods: The study constituted a pure experimental study incorporating a post-test design with only random sampling technique consisting of two groups, namely; an ethyl acetate fraction as the treatment group and ascorbic acid as the positive control group. The leaves were treated in accordance with the soxhlet method and subsequently fractionated to extract ethyl acetate fraction. This was used to measure antioxidant activity with DPPH radical damping method using a UV-Vis spectrophotometer. A linear regression calculation was performed with a standard curve to quantify the IC50 value, before the ethyl acetate fraction underwent a qualitative test of secondary metabolite. Results: An independent t-test indicated significant differences between groups, an average value of IC50 in ascorbic acid of 13.812 ppm with 0.996 linearity and a fraction of ethyl acetate 38.526 ppm with a linearity of 0.999. In contrast, at this linearity value ascorbic acid and ethyl fraction acetate demonstrate a very high linear connection between concentration and inhibition. A secondary metabolite test conducted on the ethyl acetate fraction produced positive results for flavonoid, tannins, and phenol. Conclusion: Based on the IC50 parameters, the fraction of ethyl acetate in 96% ethanol extract of binjai leaf produces very strong antioxidant activity in the content of the compounds in the fraction, namely: flavonoid, tannins and phenol.


Author(s):  
Soumya Prakash Rout ◽  
Durga Madhab Kar ◽  
Laxmidhar Maharana

<p>ABSTRACT<br />Context: Several species of the genus Annona were reported to have hypoglycemic properties and this makes Annona reticulata Linn. (Annonaceae)<br />an interesting plant for investigating its anti-hyperglycemic potential.<br />Objective: Different fractions prepared from hydro-alcoholic extract of A. reticulata leave were investigated for their blood glucose lowering effect on<br />Streptozotocin (STZ) induced hyperglycemic rats.<br />Methods: Ethyl acetate, methanol, and residual fractions (at dose level of 100 mg/kg by oral route) prepared from the hydro-alcoholic extract of<br />A. reticulata leave were administered for 14 consecutive days to STZ induced hyperglycemic rats for evaluation of their anti-hyperglycemic potential.<br />Anti-hyperglycemic potential was assessed by observation of a decrease in fasting blood glucose level.<br />Results: The studies revealed that ethyl acetate fraction decreased the blood glucose level of hyperglycemic rats from 447.67 to 234.17 mg/dL and is<br />significant (p&lt;0.001) when compared with diabetic control group. The residual fraction and methanolic fraction decreased blood glucose level from<br />417.83 to 402.50 mg/dL and 432.33 to 371.67 mg/dL respectively but not significant when compared with the diabetic control group. Standard drug<br />metformin (dose 300 mg/kg) reduced the blood glucose level from 447.33 to 219.50 mg/dL.<br />Discussion: Ethyl acetate fraction at tested dose level was capable not only to control the elevated blood glucose level but also able to attenuate<br />certain secondary parameters associated with STZ induced hyperglycemia.<br />Conclusion: This study suggested that the ethyl acetate fraction prepared from hydro-alcoholic extract of A. reticulata leave exhibit potential antihyperglycemic<br />property<br />in the tested<br />experimental<br />models and should be investigated<br />further.<br />Keywords: Streptozotocin, Diabetes, Dyslipidemia.</p>


2016 ◽  
Vol 9 (1) ◽  
pp. 204
Author(s):  
Amanda O. Andrade ◽  
Maria A. P. Da Silva ◽  
Alison H. De Oliveira ◽  
Marcos Aurelio F. Dos Santos ◽  
Lilian C. S. Vandesmet ◽  
...  

The effects of aqueous and ethanol extracts and leaf fractions of <em>Psychotria viridis</em> Ruiz &amp; Pavon (chacrona) at different concentrations on the germination and initial growth of <em>Lactuca sativa</em> L. were tested, and the phenolic and flavonoid compounds of these extracts and fractions were assessed. The bioassays consisted of the following treatments: crude aqueous extract (CAE) at 25, 50, 75 and 100% concentration, crude ethanol extract (CEE) and ethyl acetate, dichloromethane and methanol fractions at 6.25, 12.5, 25, 50 and 100% concentration and a control group. All treatments consisted of five replicates. The CAE, CEE and the ethyl acetate fraction of <em>P. viridis</em> caused both positive and negative effects on the seeds and seedlings of <em>L. sativa</em>.<em> </em>By contrast, the dichloromethane and methanol fractions only caused negative effects on <em>L. sativa</em>. The following compounds were identified in the extracts and fractions: gallic acid, chlorogenic acid, caffeic acid, ellagic acid, catechin, orientin, vitexin, quercetin, apigenin, rutin and luteolin, and the presence of the alkaloid N,N-dimethyltryptamine (DMT) has also been reported in the literature. <em>P. viridis</em> had allelopathic effects in all types of plant extracts and fractions tested, and one of these compounds or their combined action may account for these effects.


Author(s):  
Diniatik Diniatik ◽  
Suwijiyo Pramono ◽  
Sugeng Riyanto

Objective: The research was conducted by in silico analysis of xanthine oxidase inhibitors of volatile compounds from ethyl acetate fraction of ethanolic extract of Stelechocarpus burahol (Bl.) Hook f. and Th. leaves. The objective of the research was to determine the active compounds as a potential inhibitor of xanthine oxidase by using in silico screening method.Methods: The research was conducted using volatile compounds that were obtained by using gas chromatography of ethyl acetate fraction of ethanolic extract of S. burahol leaves and models of xanthine oxidase inhibitor downloaded via Protein Data Bank (PDB) with code 3BDJ, then performed docking process using the PyRx program, and then evaluated of the free energy (ΔG) as docking process results.Results: Volatile compounds in the ethyl acetate fraction of ethanolic extract were 3 heptene, 2,2,4,6,6-pentamethyl (2.15%),  methyl hexadecanoate (4.16%), ethyl tridecanoate (34.63%), methyl octadecanoate (7.26%), ethyl hexadecanoate (51.8%). The result showed that three of the chemical compounds have the lower free energy value as xanthine oxidase inhibitors than oxypurinol.Conclusion: They were ethyl tridecanoate, methyl octadecanoate, ethyl hexadecanoate with free energy (ΔG) -10.7, -7.6, -7.1 kcal / mol.Keywords: Stelechocarpus burahol (Bl.) Hook f. and Th., xanthine oxsidase, in silico analysis.


2021 ◽  
Vol 5 (2) ◽  
pp. 228-233
Author(s):  
Lusia Hayati ◽  
Joko Marwoto ◽  
Septi Purnamasari ◽  
Yuni Fitriayanti

A B S T R A C TBackground. The use of plants as anti-fertility in men has been done to reduce sideeffects. The Gendola plant is one of the Basellaceae family plants, which is a naturalmedicinal plant in Indonesia. Gendola leaves contain phenol compounds, flavonoids,tannins, steroids and triterpenoids which can have cytotoxic activity. This studyaims to determine the in vitro anti sperm activity of the ethyl acetate fraction ofGendola leaves on male spermatozoa. Methods. This study is an experimentallaboratory in vitro study using male sperm preparations. The sample used was 20men for each group, both the group was given the gondola leaf fraction and thecontrol group. The treatment group was given ethyl acetate fraction of Gendola leaves(Basella rubra Linn.) With a concentration of 0.05% for 5, 10 and 15 minutes, theviability and motility of sperm were calculated. Data analysis was performed usingthe Mann Whitney test (p <0.05) using SPSS release for Windows software. Results.The results showed that the ethyl acetate fraction affected the motility and viabilityof spermatozoa. When compared with the control group, the motility treatment groupobtained was classified as non-progressive. In the treatment group, the viability ofspermatozoa was significantly different at minute 5, minute 10 and minuted 15 (p<0.05). Conclusion. Ethyl acetate fraction has potential as an anti sperm inreducing sperm motility and viability.


Author(s):  
PRISKA ERNESTINA TENDA ◽  
ELEONORA MARYETA TOYO ◽  
ARBA PRAMUNDITA RAMADANI

Objectives: To evaluate the effect of extract and its fraction (n-hexane, ethyl acetate, and water) of the mulberry leaf (Morus australis Poir.) in reducing triglyceride and total cholesterol levels on HFD and PTU induced rats. Methods: In this study, mulberry leaves were collected from East Nusa Tenggara-Indonesia, extracted using maceration method, and fractionated with various solvents. The thin layer chromatography with silica gel 60 F254 was utilized to identify the active compound on both extract and fraction. Furthermore, using a quasi-experimental with control group design, this study employed 40 healthy male Wistar rats and divided into 8 groups, namely: normal and negative control, positive controls (simvastatin and gemfibrozil), ethanolic extract, and fractions (n-hexane, ethyl acetate, and water). All groups were fed with a high cholesterol diet and 0.01% PTU, except for the normal group. During the study, the blood was drawn at day 0, 28, 35, and 42. The triglyceride level was observed using Glycerophosphate-Oxidase Phenol Aminoantipyrine (GPO-PAP) method, while the total cholesterol was measured by Cholesterol Oxidase Phenol Aminoantipyrine (CHOD-PAP). Results: On the 42nd day, ethyl fraction of mulberry leaf (Morus australis Poir.) showed the most significant result of reducing the level of triglyceride and total cholesterol compared to the high-fat diet and PTU induced rat on day 0: triglyceride of 104.89±2.70 mg/dl vs 64.76±1.97 mg/dl and total cholesterol of 96.70±2.45 vs 88.02±1.38 mg/dl. Ethyl acetate fraction was similar to simvastatin in lowering the level of total cholesterol. TLC identification also showed that mulberry leaf contains flavonoids and polyphenols that act as anti-hyperlipidemic. Conclusion: Ethyl acetate fraction of mulberry leaf (Morus australis Poir.) showed best activity on lowering both triglyceride and total cholesterol.


2021 ◽  
Vol 18 (5) ◽  
pp. 1089-1094
Author(s):  
Hongling Zhang ◽  
Hairong Zeng ◽  
Ling Wang ◽  
Yi Qin ◽  
Qinwan Huang ◽  
...  

Purpose: To study the effect of solvent fractions of the crude extract of liushenqu on gastrointestinal motility in guinea pigs, and the mechanism of action. Methods: The effects of solvent fractions of crude extract of liushenqu (LSQ) on receptors in guinea pig isolated small intestinal cells were determined by treatment with different receptor blockers, including diphenhydramine (0.067 mg/mL), atropine sulfate (0.064 mg/mL), propranolol hydrochloride (0.033mg/mL), phentolamine mesylate (0.04mg/mL) and ondansetron hydrochloride (0.048mg/mL), to investigate the possible pharmacological mechanism of action. Results: There was no significant change in the maximum amplitude of muscle tension before and after administration in the control group, petroleum ether fraction group, and dichlormethane fraction group, while muscle tension in the 95 % ethanol and n-butanol fractions significantly increased (p < 0.01). The mean changes in tension were significantly different from that of control group (p < 0.01), but ethyl acetate fraction showed significant intestinal muscle inhibition (p < 0.01). Addition of LSQ did not alleviate the inhibition caused by diphenhydramine, but it significantly reversed the inhibition caused by blockers of cholinergic muscarinic receptor, adrenergic alpha- and beta- receptors, and 5-HT receptor (p < 0.01). Conclusion: These results indicate that n-butanol fraction is the most effective bioactive fraction of LSQ, while ethyl acetate fraction has the opposite effect. In addition, its mechanism of action is related to increase in the amplitude of small intestine smooth muscle contraction and acceleration of small intestine peristalsis.


2017 ◽  
Vol 2 (1) ◽  
pp. 1
Author(s):  
Verawati Verawati ◽  
Mimi Aria ◽  
Iyun Julia Ningsih

<p>Hypercholesterolemia is a risk factor for atherosclerosis and vascular diseases. Medicinal plants with different content of secondary metabolites such as polyphenols and flavonoids are natural sources to cope hypercholesterolemia. This study aimed to determine the effect of ethyl acetate fraction of piladang leaves (<em>Solenostemon scutellarioides</em> (L) Codd) on serum cholesterol levels in hypercholesterolemic male rats. Rats were divided into 6 groups, each consisting of 6 animals: group I (negative control), group II (positive control), group III, IV and V were each given fraction of ethyl acetate doses respectively 100, 250 and 500 mg/kg and group VI (simvastatin as a comparator). Measurement of serum cholesterol levels were conducted with CHOD-PAP method using a photometer 5010. Result showed ethyl acetate fraction affects cholesterol levels of experimental animals with a lower value than the positive control. According to statistics of one way ANOVA followed by the Duncan test method SPSS 17 showed no significant differences (p&gt; 0.05) on cholesterol levels in all given doses of ethyl acetate fraction. Group III(a dose of 100 mg / kg) was probably the most effective in lowering the blood cholesterol levels of experimental animals.</p>


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