Antimalaria Activity of Cassia spectabilis DC Leaf and Its Inhibition Effect in Heme Detoxification

2020 ◽  
Author(s):  
Wiwied - Ekasari ◽  
Dewi Resty Basuki ◽  
Heny - Arwati ◽  
Tutik Sri Wahy
Keyword(s):  
Antimalarial Activity ◽  
Ethanol Extract ◽  
Ic50 Value ◽  
Cassia Spectabilis ◽  
In Vivo Testing ◽  
Chloroquine Diphosphate ◽  
Better Than

Abstract Background In previous studies, Cassia spectabilis DC leaf has shown a good antimalarial activity. Therefore, this study is a follow-up study of leaf activity and mechanism of C. spectabilis DC as an antimalarial. Methods In vitro antimalarial activity testing using P. falciparum which was done with bioassay guide isolation in order to obtain the active compound. In vivo testing towards infected P. berghei mice was conducted to determine the effects of antimalarial prophylaxis and antimalarial activity in combination with artesunate. Whereas, heme detoxification inhibition testing as one of the antimalarial mechanisms was carried out using the Basilico method. Results The results showed that active antimalarial isolate obtained from C. spectabilis DC leaf had a structural pattern that was identical to (-)-7-hydroxyspectaline. Prophylactic test on infected P. berghei mice obtained the highest dose of inhibition percentage of 90% ethanol extract of C. spectabilis DC leaf was 68.61% while positive (doxycycline) control at 100 mg kg-1 was 73.54%. In antimalarial testing in combination with artesunate, it was found that administering 150 mg kg-1 (three times a day) of C. spectabilis DC (D0 − D2) + artesunate (D2) was better than the standard combination of amodiaquine + artesunate with 99.18% and 92.88% inhibition percentage. For the inhibitory activity of heme detoxification from ethanol extract 90%, C. spectabilis DC leaf had IC50 value of 0.375 mg mL-1 which was better than chloroquine diphosphate. Conclusion These results showed that C. spectabilis DC leaves possesses potent antimalarial activity and may offer a potential agent for effective and affordable antimalarial phytomedicine.

scholarly journals Aktivitas Penghambatan Ekstrak Etanol Daun Cassia Spectabilis Terhadap Pertumbuhan Plasmodium falciparum dan Plasmodium berghei

2017 ◽  
Vol 3 (1) ◽  
pp. 17 ◽  
Author(s):  
Wiwied Ekasari ◽  
Nindya Tresiana ◽  
Suciati Iryani ◽  
Tutik Sri Wahyuni ◽  
Heny Arwaty
Keyword(s):  
Plasmodium Falciparum ◽  
Methanol Extract ◽  
Antimalarial Activity ◽  
Ethanolic Extract ◽  
Ethanol Extract ◽  
In Vivo Test ◽  
Ic50 Value ◽  
Cassia Spectabilis

Background: Antimalarial screening against nine species of the genus Cassia showed that the methanol extract of leaves Cassia spectabilis have the highest activity. Since it will be used as a traditional medicine, hence it is needed further studies of antimalarial activity of these plants by choosing a safer solvent, namely ethanol. Objective: In vitro anti-malarial activity against Plasmodium falciparum was conducted using the method of Trager and Jensen. Methods: The serial solution tested were: 100, 10, 1,  0.1 and 0.01 µg/ mL, while the in vivo test was performed based on Peter’s test (The days suppressive test) that using P. berghei (strain ANKA) infected mice. Results: The results showed that ethanolic extract of C. spectabilis leaves has inhibitory activity against P. falciparum with IC50 value of 12.52 µg/ mL and against P. berghei with ED50 value of 131.5 mg/kg body weight. Conclusions: A further study to see the potential of ethanol extract from C. Spectabilis leaves as anti-malaria is warranted. 

scholarly journals Antiplasmodial activity of Ethanolic extract of Cassia spectabilis DC leaf and its inhibition effect in Heme detoxification

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Wiwied Ekasari ◽  
Dewi Resty Basuki ◽  
Heny Arwati ◽  
Tutik Sri Wahyuni
Keyword(s):  
Ethanolic Extract ◽  
Positive Control ◽  
Antiplasmodial Activity ◽  
In Vivo Test ◽  
Cassia Spectabilis ◽  
Chloroquine Diphosphate ◽  
Better Than

Abstract Background In previous studies, Cassia spectabilis DC leaf has shown a good antiplasmodial activity. Therefore, this study is a follow-up study of the extract of leaf of C. spectabilis DC on its in vitro and in vivo antiplasmodial activity and mechanism as an antimalarial. Methods The extract was fractionated, sub-fractionated and isolated to obtain the purified compound. In vitro antiplasmodial activity test against Plasmodium falciparum to find out the active compound. In vivo test against P. berghei ANKA-infected mice was conducted to determine prophylactic activity and antiplasmodial activity either alone or in combination with artesunate. The inhibition of heme detoxification test as one of the antimalarial mechanisms was carried out using the Basilico method. Results The results showed that active antimalarial compound isolated from C. spectabilis DC leaf had a structural pattern that was identical to (−)-7-hydroxycassine. Prophylactic test of 90% ethanolic extract of C. spectabilis DC leaf alone against P. berghei ANKA-infected mice obtained the highest percentage inhibition was 68.61%, while positive control (doxycycline 13 mg/kg) was 73.54%. In combination with artesunate, 150 mg/kg three times a day of C. spectabilis DC (D0-D2) + artesunate (D2) was better than the standard combination of amodiaquine + artesunate where the inhibition percentages were 99.18 and 92.88%, respectively. The IC50 of the extract for the inhibitory activity of heme detoxification was 0.375 mg/ml which was better than chloroquine diphosphate (0.682 mg/ml). Conclusion C. spectabilis DC leaf possessed potent antiplasmodial activity and may offer a potential agent for effective and affordable antimalarial phytomedicine.

scholarly journals Aktivitas Penghambatan Ekstrak Etanol Daun Cassia Spectabilis Terhadap Pertumbuhan Plasmodium falciparum dan Plasmodium berghei

2017 ◽  
Vol 3 (1) ◽  
pp. 17
Author(s):  
Wiwied Ekasari ◽  
Nindya Tresiana ◽  
Suciati Iryani ◽  
Tutik Sri Wahyuni ◽  
Heny Arwaty
Keyword(s):  
Plasmodium Falciparum ◽  
Methanol Extract ◽  
Antimalarial Activity ◽  
Ethanolic Extract ◽  
Ethanol Extract ◽  
In Vivo Test ◽  
Ic50 Value ◽  
Cassia Spectabilis

Background: Antimalarial screening against nine species of the genus Cassia showed that the methanol extract of leaves Cassia spectabilis have the highest activity. Since it will be used as a traditional medicine, hence it is needed further studies of antimalarial activity of these plants by choosing a safer solvent, namely ethanol. Objective: In vitro anti-malarial activity against Plasmodium falciparum was conducted using the method of Trager and Jensen. Methods: The serial solution tested were: 100, 10, 1,  0.1 and 0.01 µg/ mL, while the in vivo test was performed based on Peter’s test (The days suppressive test) that using P. berghei (strain ANKA) infected mice. Results: The results showed that ethanolic extract of C. spectabilis leaves has inhibitory activity against P. falciparum with IC50 value of 12.52 µg/ mL and against P. berghei with ED50 value of 131.5 mg/kg body weight. Conclusions: A further study to see the potential of ethanol extract from C. Spectabilis leaves as anti-malaria is warranted. 

scholarly journals Preparation and Anti-Tumour Activity of Some Arylbismuth(III) Oxine Complexes

1998 ◽  
Vol 5 (5) ◽  
pp. 295-304 ◽  
Author(s):  
Katharine A. Smith ◽  
Glen B. Deacon ◽  
W. Roy Jackson ◽  
Edward R. T. Tiekink ◽  
Silvina Rainone ◽  
...  
Keyword(s):  
Phenyl Group ◽  
Significant Activity ◽  
X Ray ◽  
Crystallographic Study ◽  
Anti Tumour Activity ◽  
In Vivo Testing ◽  
Tumour Activity ◽  
Better Than

New arylbismuth(lll) oxinates, PhBi(MeOx)2, (p-MeC6H4)Bi(Ox)2, (p-MeC6H4)Bi(MeOx)2, (p-ClC6H4)Bi(Ox)2, and (p-ClC6H4)Bi(MeOx)2 (Ox− = quinolin-8-olate and MeOx−=2-methylquinolin-8-olate) have been prepared by reaction of the appropriate diarylbismuth chlorides with Na(Ox) or Na(MeOx) in the presence of 15-crown-5. An X-ray crystallographic study has shown PhBi(MeOx)2 to be a five coordinate monomer with distorted square pyramidal stereochemistry. Chelating MeOx ligands have a cisoid arrangement in the square plane and the phenyl group is apical. The lattice is stabilised by significant π-π interactions between centrosymmetric molecules. A range of these complexes has been shown to have high in vitro biological activity (comparable with or better than cisplatin) against L1210 leukaemia, the corresponding cisplatin resistant line, and a human ovarian cell line, SKOV-3. However, initial in vivo testing against a solid mouse plasmacytoma (PC6) and P388 leukaemia has not revealed significant activity.

scholarly journals Various Parts of Helianthus annuus Plants as New Sources of Antimalarial Drugs

2019 ◽  
Vol 2019 ◽  
pp. 1-7
Author(s):  
Wiwied Ekasari ◽  
Dwi Widya Pratiwi ◽  
Zelmira Amanda ◽  
Suciati ◽  
Aty Widyawaruyanti ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Helianthus Annuus ◽  
Antimalarial Activity ◽  
Ethanol Extract ◽  
The Other ◽  
Antimalarial Agent ◽  
A Value ◽  
Ethanol Extracts

Background. Each part of H. annuus plants is traditionally used as medicinal remedies for several diseases, including malaria. Antimalarial activity of the leaf and the seed has already been observed; however, there is no report about antimalarial activity of the other parts of H. annuus plants. In this study, we assess in vitro and in vivo antimalarial activity of each part of the plants and its mechanism as antimalarial agent against inhibition of heme detoxification. Objective. To investigate the antimalarial activity of various parts of H. annuus. Methods. Various parts of the H. annuus plant were tested for in vitro antimalarial activity against Plasmodium falciparum 3D7 strain (chloroquine-sensitive), in vivo antimalarial activity against P. berghei using Peters’ 4-day suppressive test in BALB/c mice, curative and prophylaxis assay, and inhibition of heme detoxification by evaluating β-hematin level. Results. Ethanol extract of the roots showed the highest antimalarial activity, followed by ethanol extract of leaves, with IC50 values of 2.3 ± 1.4 and 4.3 ± 2.2 μg/mL, respectively and the percentage inhibition of P. berghei of 63.6 ± 8.0 and 59.3 ± 13.2 at a dose of 100 mg/kg, respectively. Ethanol extract of roots produced an ED50 value of 10.6 ± 0.2 mg/kg in the curative test and showed an inhibition of 79.2% at a dose of 400 mg/kg in the prophylactic assay. In inhibition of heme detoxification assay, root and leaf ethanol extracts yielded a lower IC50 value than positive (chloroquine) control with a value of 0.4 ± 0.0 and 0.5 ± 0.0 mg/mL, respectively. Conclusion. There were promising results of the ethanol extracts of root of H. annuus as a new source for the development of a new plant-based antimalarial agent.

scholarly journals In Vitro and In Vivo Antimalarial Activity of LZ1, a Peptide Derived from Snake Cathelicidin

Toxins ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 379 ◽  
Author(s):  
Yaqun Fang ◽  
Xiaoqin He ◽  
Pengcheng Zhang ◽  
Chuanbin Shen ◽  
James Mwangi ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Potential Candidate ◽  
Dependent Manner ◽  
Strong Suppression ◽  
Atp Production ◽  
Ic50 Value ◽  
Function Impairment ◽  
Global Threat

Antimalarial drug resistance is an enormous global threat. Recently, antimicrobial peptides (AMPs) are emerging as a new source of antimalarials. In this study, an AMP LZ1 derived from snake cathelicidin was identified with antimalarial activity. In the in vitro antiplasmodial assay, LZ1 showed strong suppression of blood stage Plasmodium falciparum (P. falciparum) with an IC50 value of 3.045 μM. In the in vivo antiplasmodial assay, LZ1 exerted a significant antimalarial activity against Plasmodium berghei (P. berghei) in a dose- and a time- dependent manner. In addition, LZ1 exhibited anti-inflammatory effects and attenuated liver-function impairment during P. berghei infection. Furthermore, by employing inhibitors against glycolysis and oxidative phosphorylation in erythrocytes, LZ1 specifically inhibited adenosine triphosphate (ATP) production in parasite-infected erythrocyte by selectively inhibiting the pyruvate kinase activity. In conclusion, the present study demonstrates that LZ1 is a potential candidate for novel antimalarials development.

Discovery of 3-Cinnamamido-N-Substituted Benzamides as Potential Antimalarial Agents

2020 ◽  
Vol 16 ◽  
Author(s):  
Haicheng Liu ◽  
Yushi Futamura ◽  
Honghai Wu ◽  
Aki Ishiyama ◽  
Taotao Zhang ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Antimalarial Activity ◽  
In Vitro Assays ◽  
Compound Library ◽  
Antimalarial Agents ◽  
Phenotypic Screen ◽  
Ic50 Values ◽  
Substituted Benzamides

Background: Malaria is one of the most devastating parasitic diseases, yet the discovery of antimalarial agents remains profoundly challenging. Very few new antimalarials have been developed in the past 50 years, while the emergence of drug-resistance continues to appear. Objective: This study focuses on the discovery, design, synthesis, and antimalarial evaluation of 3-cinnamamido-N-substituted benzamides. Method: In this study, a screening of our compound library was carried out against the multidrug-sensitive Plasmodium falciparum 3D7 strain. Derivatives of the hit were designed, synthesized and tested against P. falciparum 3D7 and the in vivo antimalarial activity of the most active compounds was evaluated using the method of Peters’ 4-day suppressive test. Results: The retrieved hit compound 1 containing a 3-cinnamamido-N-substituted benzamide skeleton showed moderate antimalarial activity (IC50 = 1.20 µM) for the first time. A series of derivatives were then synthesized through a simple four-step workflow, and half of them exhibited slightly better antimalarial effect than the precursor 1 during the subsequent in vitro assays. Additionally, compounds 11, 23, 30 and 31 displayed potent activity with IC50 values of approximately 0.1 µM, and weak cytotoxicity against mammalian cells. However, in vivo antimalarial activity is not effective which might be ascribed to the poor solubility of these compounds. Conclusion: In this study, phenotypic screen of our compound library resulted in the first report of 3-cinnamamide framework with antimalarial activity and 40 derivatives were then designed and synthesized. Subsequent structure-activity studies showed that compounds 11, 23, 30 and 31 exhibited the most potent and selective activity against P. falciparum 3D7 strain with IC50 values around 0.1 µM. Our work herein sets another example of phenotypic screen-based drug discovery, leading to potentially promising candidates of novel antimalarial agents once given further optimization.

scholarly journals Stage-dependent effect of deferoxamine on growth of Plasmodium falciparum in vitro

Blood ◽  
1990 ◽  
Vol 76 (6) ◽  
pp. 1250-1255 ◽  
Author(s):  
S Whitehead ◽  
TE Peto
Keyword(s):  
Plasmodium Falciparum ◽  
Growth Inhibition ◽  
Antimalarial Activity ◽  
Clinical Malaria ◽  
Inhibitory Effect ◽  
Parasite Development ◽  
And Control ◽  
Speed Of Onset

Abstract Deferoxamine (DF) has antimalarial activity that can be demonstrated in vitro and in vivo. This study is designed to examine the speed of onset and stage dependency of growth inhibition by DF and to determine whether its antimalarial activity is cytostatic or cytocidal. Growth inhibition was assessed by suppression of hypoxanthine incorporation and differences in morphologic appearance between treated and control parasites. Using synchronized in vitro cultures of Plasmodium falciparum, growth inhibition by DF was detected within a single parasite cycle. Ring and nonpigmented trophozoite stages were sensitive to the inhibitory effect of DF but cytostatic antimalarial activity was suggested by evidence of parasite recovery in later cycles. However, profound growth inhibition, with no evidence of subsequent recovery, occurred when pigmented trophozoites and early schizonts were exposed to DF. At this stage in parasite development, the activity of DF was cytocidal and furthermore, the critical period of exposure may be as short as 6 hours. These observations suggest that iron chelators may have a role in the treatment of clinical malaria.

Aspiration Revisited: Prospective Evaluation of a Physiologically Pressurized Model With Animal Correlation and Broader Applicability to Filler Complications

2021 ◽  
Author(s):  
Hyoung-Jin Moon ◽  
Won Lee ◽  
Ji-Soo Kim ◽  
Eun-Jung Yang ◽  
Hema Sundaram
Keyword(s):  
Normal Saline ◽  
False Negative ◽  
Vascular Complications ◽  
Filler Injection ◽  
Negative Results ◽  
Needle Position ◽  
False Negative Results ◽  
In Vivo Testing

Abstract Background Aspiration testing before filler injection is controversial. Some believe that aspiration can help prevent inadvertent intravascular injection, while others cite false-negative results and question its value given that the needle position always changes somewhat during injection procedures. Objectives To test the relation of false-negative results to the viscosity of the material within the needle lumen and determine whether a less viscous material within the needle lumen could decrease the incidence of false-negative results. Methods In vitro aspiration tests were performed using 30-G and 27-G needle gauges, two cross-linked hyaluronic acid fillers, normal saline bags pressurized at 140 and 10 mmHg to mimic human arterial and venous pressures, and three needle lumen conditions (normal saline, air, and filler). Testing was repeated three times under each study condition (72 tests in total). For in vivo correlation, aspiration tests were performed on femoral arteries and central auricular veins in three rabbits (4–5 aspirations per site, 48 tests in total). Results In vitro and in vivo testing using 30-G needles containing filler both showed false-negative results on aspiration testing. In vitro and in vivo testing using needles containing saline or air showed positive findings. Conclusions False-negative results from aspiration testing may be reduced by pre-filling the needle lumen with saline rather than a filler. The pressurized system may help overcome challenges of animal models with intravascular pressures significantly different from those of humans. The adaptability of this system to mimic various vessel pressures may facilitate physiologically relevant studies of vascular complications.

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