scholarly journals Uji Aktivitas Antimalaria dari Spons Xestospongia sp. Asal Pulau Yapen secara In Vivo

2021 ◽  
Vol 24 (2) ◽  
pp. 177-184
Author(s):  
Murtihapsari Murtihapsari ◽  
Mathelda K. Roreng ◽  
Apriani Parubak ◽  
Alif Rahman

It is generally admitted that marine sponge has rich of secondary metabolite as alkaloids, peptides and terpene. Those various compounds can be used for antimalarial drug.  This study aims to evaluate the in vivo antimalarial activity and to characterize the effectiveness of dose (ED50) of n-hexane extracted from Xestospongia sp. by using the Plasmodium berghei infected to mices. In the present study, we used Peter’s four day suppressive test, where the mice infected with Plasmodium berghei intra peritoneal with a suspension containing infected red blood cell origin from donor mice with parasitemia. Results of present study exhibited that the sponge Xestospongia sp. contains secondary metabolite including tritepenoid/steroid, alkaloid and saponin. Furthermore, an in vivo test revealed the affectivity dose (ED50) was 0.24 mg/kg of body weight. This finding is categorized a signifant decreasing level of parasitemia.   Secara umum, spons laut mempunyai kandungan metabolit sekunder seperti alkaloid, peptide dan terpena. Berbagai senyawa tersebut dapat dimanfaatkan sebagai obat antimalaria. Penelitian ini bertujuan untuk mengetahui kandungan kimia dan mengevaluasi aktivitas antimalarial secara in vivo untuk efektivitas dosis (ED50) ekstrak n-heksana dari spons Xestospongia sp. dengan menggunakan Plasmodium berghei yang diinfeksi ke tikus. Penelitian ini digunakan metode the 4-day Supresive Test, dimana mencit yang diinfeksi Plasmodium berghei secara intra peritoneal dengan suspensi yang mengandung sel darah merah terinfeksi yang berasal dari mencit donor. Hasil penelitian ini menunjukkan adanya kandungan metabolit sekunder diantaranya tritepenoid/steroid, alkaloid dan saponin. Selanjutnya, uji in vivo diperoleh nilai ED50 sebesar 0,24 mg/kg BB dikelompokan sangat baik, yang dapat menurunkan tingkat parasitemia secara signifikan. Dengan demikian, spons laut asal pulau Yapen dapat dijadikan sebagai sumber metabolit potensial untuk obat antimalaria.

2020 ◽  
Author(s):  
Abebe Basazn Mekuria ◽  
Mestayet Geta ◽  
Eshetie Melese Birru ◽  
Desalegn Asmelashe Gelayee

Abstract Background: Due to drug resistance and inefficient eradication techniques, malaria continues to be a major public health issue in countries with low- and middle-income. The seeds of Schinus molle are used in the Ethiopian folklore medicine for the treatment of malaria. However, this claim is not yet supported with scientific researches. Hence, the current study aims to investigate in vivo, antimalarial activity of hydro-alcoholic crude extract and subsequent solvent fraction of Schinus molle seeds on Plasmodium berghe infected mice.Methods: A hydro-alcoholic crude extract and solvent fractions (ethyl acetate, chloroform and aqueous) of Schinus molle seeds were tested at different doses (100, 200 and 400 mg/kg respectively ) to evaluate in vivo antimalarial activity of extracts in a 4-day suppressive, curative, and prophylaxis antimalarial test models. The parasitemia level, packed cell volume, survival of date, body weight, and body temperature were used to evaluate the anti-plasmodia activity of the extracts. One way ANOVA was employed to analyze these data, followed by post hoc Tukey’s HSD multiple comparison test.Results: The chemo-suppressive activities produced by the highest dose (400mg/kg) of crude extract and the aqueous fraction of Schinus molle seeds in the four-day suppressive test were 76.03% and 73.82%(p<0.001), respectively. In the curative test, the highest dose of crude and the aqueous fraction of Schinus molle seeds had 82.12% and 84.30% (p<0.001) suppression activity, respectively. The percentage of suppression in the prophylactic activities test of the aqueous fraction was 79.78% (p<0.001) at 400mg/kg compared to the negative control group. The studied plant extracts were likely anticipated to show rapid rectal temperature reduction and weight loss significantly. Among the extracts, only chloroform fraction has prevented the reduction of packed cell volume, due to the absence of saponin in the fraction. The mice which were treated with crude extract and aqueous fraction survived longer and gained net body weight as compared to vehicle-treated mice (p<0.001).Conclusion: The crude extract and aqueous fraction of Schinus molle seeds possessed significant antimalarial activity. These results collectively indicate that the plant has promising anti-plasmodial activity against Plasmodium berghei. However, further confirmatory studies followed by isolation and characterization of the active antimalarial compound are recommended.


2021 ◽  
Vol 49 (1) ◽  
Author(s):  
Kantarakorn Kaewdana ◽  
Prapaporn Chaniad ◽  
Pitchanee Jariyapong ◽  
Arisara Phuwajaroanpong ◽  
Chuchard Punsawad

Abstract Background Sophora exigua Craib. is commonly used in Thailand to reduce fever and increase postpartum breast milk production in women who have hypogalactia. However, there has been no report on the antioxidant and antimalarial properties of this plant. This study aimed to investigate the antioxidant and antimalarial activities of S. exigua root extract and to evaluate its acute toxicity in mice to confirm its safety. Methods The in vitro antioxidant activities were determined using 2,2-diphenyl-1-picrylhydrazyl (DPPH), superoxide radical, and hydroxyl radical scavenging assays. The in vivo antioxidant activities were determined by detecting the malondialdehyde (MDA) content and superoxide dismutase (SOD) activity in the livers of malaria-infected mice. The in vivo antimalarial activity was determined by Peters’ 4-day suppressive test in mice infected with Plasmodium berghei ANKA and orally administered S. exigua root aqueous and ethanolic extracts at different doses (200, 400, and 600 mg/kg body weight). In addition, the acute oral toxicity of the plant extracts was assessed in mice at a dose of 2000 mg/kg body weight. Results The ethanolic extract of S. exigua root exhibited inhibition of DPPH radicals, superoxide anions, and hydroxyl radicals, with half maximal inhibitory concentration (IC50) values of 24.63 ± 1.78, 129.78 ± 0.65, and 30.58 ± 1.19 μg/ml, respectively. Similarly, research on the in vivo antioxidant activity indicated that the ethanolic extract of S. exigua root exerted a stronger effect than the aqueous extract. The aqueous extract at doses of 200, 400, and 600 mg/kg had stronger antimalarial activity than the ethanolic extract. The aqueous extract at 600 mg/kg exhibited 60.46% suppression of parasitemia. Increased levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), and alkaline phosphatase (ALP) and blood urea nitrogen (BUN) were detected in the mice treated with 2000 mg/kg ethanolic extract, which was related to the results of histopathological analysis of liver tissue, showing ballooning degeneration of hepatocytes, diffuse hepatic hemorrhage, and infiltration of inflammatory cells. Conclusions This study demonstrated that the ethanolic S. exigua root extract possessed antioxidant properties, and the aqueous extract also had antimalarial activity. Therefore, this plant is an alternative source of new antioxidant and antimalarial agents.


1977 ◽  
Vol 16 (01) ◽  
pp. 26-29 ◽  
Author(s):  
D. D. Greenberg ◽  
P. Som ◽  
G. E. Meinken ◽  
D. F. Sacker ◽  
H. L. Atkins ◽  
...  

Summary 99mTc-pertechnetate distribution studies were performed in rabbits and mice following pretreatment between 5—336 hours with various routinely used stannous complexes (HSA, MAA, GHT, DTPA, PYPs) containing different amounts of Sn++ (0.17 —15.0 μ mg/kg). Beyond a concentration of 0.26 mg/kg of Sn++ an alteration in 99mTc-pertechnetate distribution was observed. The red blood cell was found to be the most prominent target. An in-vivo reduction of 99mTc-pertechnetate apparently occurred by the presence of stannous ion within the red blood cell. Preloading time period between 5—24 hours did not alter the uptake of RBC/plasma ratio. Beyond that period it decreased slowly and still persisted up to 2 weeks following pretreatment. RBC/ plasma ratio of 99mTcO4 - increased with increased Sn++ content of various commercially available pharmaceutical kits.


Author(s):  
Shannon L. McArdel ◽  
Anne-Sophie Dugast ◽  
Maegan E. Hoover ◽  
Arjun Bollampalli ◽  
Enping Hong ◽  
...  

AbstractRecombinant agonists that activate co-stimulatory and cytokine receptors have shown limited clinical anticancer utility, potentially due to narrow therapeutic windows, the need for coordinated activation of co-stimulatory and cytokine pathways and the failure of agonistic antibodies to recapitulate signaling by endogenous ligands. RTX-240 is a genetically engineered red blood cell expressing 4-1BBL and IL-15/IL-15Rα fusion (IL-15TP). RTX-240 is designed to potently and simultaneously stimulate the 4-1BB and IL-15 pathways, thereby activating and expanding T cells and NK cells, while potentially offering an improved safety profile through restricted biodistribution. We assessed the ability of RTX-240 to expand and activate T cells and NK cells and evaluated the in vivo efficacy, pharmacodynamics and tolerability using murine models. Treatment of PBMCs with RTX-240 induced T cell and NK cell activation and proliferation. In vivo studies using mRBC-240, a mouse surrogate for RTX-240, revealed biodistribution predominantly to the red pulp of the spleen, leading to CD8 + T cell and NK cell expansion. mRBC-240 was efficacious in a B16-F10 melanoma model and led to increased NK cell infiltration into the lungs. mRBC-240 significantly inhibited CT26 tumor growth, in association with an increase in tumor-infiltrating proliferating and cytotoxic CD8 + T cells. mRBC-240 was tolerated and showed no evidence of hepatic injury at the highest feasible dose, compared with a 4-1BB agonistic antibody. RTX-240 promotes T cell and NK cell activity in preclinical models and shows efficacy and an improved safety profile. Based on these data, RTX-240 is now being evaluated in a clinical trial.


Pathogens ◽  
2021 ◽  
Vol 10 (5) ◽  
pp. 532
Author(s):  
Hae-Soo Yun ◽  
Sylvatrie-Danne Dinzouna-Boutamba ◽  
Sanghyun Lee ◽  
Zin Moon ◽  
Dongmi Kwak ◽  
...  

In traditional Chinese medicine, Ranunculus japonicus has been used to treat various diseases, including malaria, and the young stem of R. japonicus is consumed as a food in the Republic of Korea. However, experimental evidence of the antimalarial effect of R. japonicus has not been evaluated. Therefore, the antimalarial activity of the extract of the young stem of R. japonicus was evaluated in vitro using both chloroquine-sensitive (3D7) and chloroquine-resistant (Dd2) strains; in vivo activity was evaluated in Plasmodium berghei-infected mice via oral administration followed by a four-day suppressive test focused on biochemical and hematological parameters. Exposure to extracts of R. japonicus resulted in significant inhibition of both chloroquine-sensitive (3D7) and resistant (Dd2) strains of P. falciparum, with IC50 values of 6.29 ± 2.78 and 5.36 ± 4.93 μg/mL, respectively. Administration of R. japonicus also resulted in potent antimalarial activity against P. berghei in infected mice with no associated toxicity; treatment also resulted in improved hepatic, renal, and hematologic parameters. These results demonstrate the antimalarial effects of R. japonicus both in vitro and in vivo with no apparent toxicity.


PLoS ONE ◽  
2015 ◽  
Vol 10 (8) ◽  
pp. e0136885 ◽  
Author(s):  
Stéphane Kerbrat ◽  
Benoit Vingert ◽  
Marie-Pierre Junier ◽  
Flavia Castellano ◽  
François Renault-Mihara ◽  
...  

1997 ◽  
Vol 272 (5) ◽  
pp. H2107-H2114 ◽  
Author(s):  
D. C. Poole ◽  
T. I. Musch ◽  
C. A. Kindig

As muscles are stretched, blood flow and oxygen delivery are compromised, and consequently muscle function is impaired. We tested the hypothesis that the structural microvascular sequellae associated with muscle extension in vivo would impair capillary red blood cell hemodynamics. We developed an intravital spinotrapezius preparation that facilitated direct on-line measurement and alteration of sarcomere length simultaneously with determination of capillary geometry and red blood cell flow dynamics. The range of spinotrapezius sarcomere lengths achievable in vivo was 2.17 +/- 0.05 to 3.13 +/- 0.11 microns. Capillary tortuosity decreased systematically with increases of sarcomere length up to 2.6 microns, at which point most capillaries appeared to be highly oriented along the fiber longitudinal axis. Further increases in sarcomere length above this value reduced mean capillary diameter from 5.61 +/- 0.03 microns at 2.4-2.6 microns sarcomere length to 4.12 +/- 0.05 microns at 3.2-3.4 microns sarcomere length. Over the range of physiological sarcomere lengths, bulk blood flow (radioactive microspheres) decreased approximately 40% from 24.3 +/- 7.5 to 14.5 +/- 4.6 ml.100 g-1.min-1. The proportion of continuously perfused capillaries, i.e., those with continuous flow throughout the 60-s observation period, decreased from 95.9 +/- 0.6% at the shortest sarcomere lengths to 56.5 +/- 0.7% at the longest sarcomere lengths and was correlated significantly with the reduced capillary diameter (r = 0.711, P < 0.01; n = 18). We conclude that alterations in capillary geometry and luminal diameter consequent to increased muscle sarcomere length are associated with a reduction in mean capillary red blood cell velocity and a greater proportion of capillaries in which red blood cell flow is stopped or intermittent. Thus not only does muscle stretching reduce bulk blood (and oxygen) delivery, it also alters capillary red blood cell flow dynamics, which may further impair blood-tissue oxygen exchange.


1999 ◽  
Vol 277 (2) ◽  
pp. H508-H514 ◽  
Author(s):  
Charmaine B. S. Henry ◽  
Brian R. Duling

The endothelial cell glycocalyx influences blood flow and presents a selective barrier to movement of macromolecules from plasma to the endothelial surface. In the hamster cremaster microcirculation, FITC-labeled Dextran 70 and larger molecules are excluded from a region extending almost 0.5 μm from the endothelial surface into the lumen. Red blood cells under normal flow conditions are excluded from a region extending even farther into the lumen. Examination of cultured endothelial cells has shown that the glycocalyx contains hyaluronan, a glycosaminoglycan which is known to create matrices with molecular sieving properties. To test the hypothesis that hyaluronan might be involved in establishing the permeation properties of the apical surface glycocalyx in vivo, hamster microvessels in the cremaster muscle were visualized using video microscopy. After infusion of one of several FITC-dextrans (70, 145, 580, and 2,000 kDa) via a femoral cannula, microvessels were observed with bright-field and fluorescence microscopy to obtain estimates of the anatomic diameters and the widths of fluorescent dextran columns and of red blood cell columns (means ± SE). The widths of the red blood cell and dextran exclusion zones were calculated as one-half the difference between the bright-field anatomic diameter and the width of the red blood cell column or dextran column. After 1 h of treatment with active Streptomyces hyaluronidase, there was a significant increase in access of 70- and 145-kDa FITC-dextrans to the space bounded by the apical glycocalyx, but no increase in access of the red blood cells or in the anatomic diameter in capillaries, arterioles, and venules. Hyaluronidase had no effect on access of FITC-Dextrans 580 and 2,000. Infusion of a mixture of hyaluronan and chondroitin sulfate after enzyme treatment reconstituted the glycocalyx, although treatment with either molecule separately had no effect. These results suggest that cell surface hyaluronan plays a role in regulating or establishing permeation of the apical glycocalyx to macromolecules. This finding and our prior observations suggest that hyaluronan and other glycoconjugates are required for assembly of the matrix on the endothelial surface. We hypothesize that hyaluronidase creates a more open matrix, enabling smaller dextran molecules to penetrate deeper into the glycocalyx.


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