@article {1053, title = {Antimalarial Activity of Microalgae Extracts Based on Inhibition of PfMQO, a Mitochondrial Plasmodium falciparum Enzyme}, journal = {Pharmacognosy Journal}, volume = {11}, year = {2019}, month = {November 2019}, pages = {1477-1482}, type = {Original Article}, chapter = {1477}, abstract = {

Malaria is an important global disease that threatened human life. The resistance Plasmodium sp. to the available medicines encourages the search for new antimalarial substances based on new mechanisms on the inhibition of PfMQO (the mitochondrial Plasmodium falciparum enzyme). Objective: The purposes of this study was to screen antimalarial substances from microalgae based on the inhibition of PfMQO. Materials and Methods: Five microalgae were extracted by maceration using chloroform pa and ethanol pa. These ten crude extracts obtained were tested for the inhibitory activity against the PfMQO enzyme. Results: The highest inhibitory activity against PfMQO enzyme was chloroform extract of S. costatum with 91.050\% of inhibition and 0.043 μg/mL of IC50. The ethanol extract of S. platensis showed 91.999\% and 5.25 μg/mL of inhibition and IC50, respectively. These results indicated that the two extracts provide high antimalarial activity exceeded a theoretical standard of antimalarial bioactive compounds. Conclusion: Chloroform extract of S. costatum and ethanol extract of S. platensis are promising sources of antimalarial compounds based on the inhibition of PfMQO.

}, keywords = {Antimalarial, Inhibitory activity, Microalgae, P falciparum, Screening}, doi = {10.5530/pj.2019.11.228}, author = {Endang Ariyani Setyowati and Alim Isnansetyo and Tjut Sugandawaty Djohan and Raden Wisnu Nurcahyo} } @article {354, title = {Antimalarial and Antioxidant Potentials of Extract and Fractions of Aerial part of Borreria ocymoides DC (Rubiaceae).}, journal = {Pharmacognosy Journal}, volume = {9}, year = {2017}, month = {May 2017}, pages = {534-540}, type = {Original Article}, chapter = {534}, abstract = {

Introduction: Borreria ocymoides (Burm F) DC is a weak, erect and decumbent herb that has several folkloric, ethno medicinal uses and is included in antimalarial preparations by some traditional healers. It is also used in treatment of ring worm, eczema and microbial infections. Objectives: To evaluate antimalarial activity of extract and fractions of Borreria ocymoides in Plasmodium berghei infected mice and to investigate their antioxidant activity using 1, 1-diphenyl-2-picryl-hydrazile (DPPH). Methods: The methanol extract of aerial part of B. ocymoides and the solvent fractions obtained from partition between organic solvents were assessed for antimalarial activity against chloroquine sensitive Plasmodium berghei NK65 infected mice using the suppressive and curative test procedures. Chloroquine (10 mg/ml) was used as positive control. The antioxidant activity was evaluated using DPPH radical scavenging ability and determination of total phenolic content. Results: The crude extract (250 and 500 mg kg-1) produced a dose dependent anti-plasmodial activity in the suppressive and curative tests. The chemo suppression activity was best in the ethyl acetate fraction (87.31\%) and in the order ethyl acetate \>dichloromethane \> hexane \> aqueous fraction. The DPPH radical scavenging activity of the extract increased with concentration. The antioxidant activity was less than ascorbic acid used as positive control. Oral administration up to 5 g/kg produced no noticeable deleterious effect 24 hours after dosing and up to 7 days afterwards. Conclusion: The results indicated that the extract has a potent anti-plasmodial activity against Plasmodium berghei and the activity seems to reside in the mid-polar fractions. Thus, the plant is a potential source of new antimalarial agents.

}, keywords = {Antimalarial, Antioxidant, Borreria ocymoides, Plasmodium berghei, Solvent fractions}, doi = {10.5530/pj.2017.4.86}, url = {/files/PJ-9-4/10.5530pj.2017.4.86}, author = {Sunday Adeleke Adesegun and Celestina Ifeoma Orabueze and Herbert Alexander Babatunde Coker} } @article {76, title = {In vivo Antimalarial Evaluation of Embelin and its Semi-Synthetic Aromatic Amine Derivatives}, journal = {Pharmacognosy Journal}, volume = {7}, year = {2015}, month = {01/2015}, pages = {305-310}, type = {Original Article}, chapter = {305}, abstract = {

Background: In less developed countries like Ethiopia, malaria is traditionally treated by remedies prepared from medicinal plants. One such plant that falls in this category is Embelia schimperi Vatke whose fruits are employed for the treatment of a variety of ailments including taeniasis and malaria. Objective: In the present study, the in vivo antimalarial activity of embelin isolated from the fruits of Embelia schimperi Vatke and its semisynthetic aromatic amine derivatives was evaluated. Methods: Silica gel column chromatography was used to isolate embelin from the ethyl acetate extract of the fruits of E. schimperi. Aromatic substituted embelin derivatives were semi-synthesized by using a one-step condensation reaction of embelin with aromatic amines. The compounds were characterized based on their UV, IR, HR-ESIMS, 1H and 13C NMR and DEPT-135 spectral data. Antimalarial activity was evaluated using a modified Peter\’s 4-day suppressive test against chloroquine sensitive Plasmodium berghei infection in mice. Results: Embelin and the semi-synthetic derivatives showed significant (p\<0.05) in vivo antimalarial activity in a dose-dependent manner with 47.8-74.7\% parasite suppression at tested doses of 100-400 mg/kg. Among the compounds semi-synthesized, 5-(p-tolylamino)-2-hydroxy-3-undecylcyclohexa- 2,5-diene-1,4-dione showed maximum antimalarial activity (74.7 \% suppression) at a dose of 400 mg/kg. No major signs of toxicity were observed when either embelin or the semi-synthesized derivatives were administrated to mice at the highest tested dose (2 g/kg). Conclusion: The results underline that the antimalarial activity of embelin can be improved by preparing its aromatic semi-synthetic amine derivatives without affecting the safety of the parent molecule.

}, keywords = {A 4-Day suppressive test, Antimalarial, Aromatic substituted embelin, Embelia schimperi, Embelin.}, doi = {10.5530/pj.2015.5.10}, author = {Kibrnesh Bezu and Daniel Bisrat and Kaleab Asres} }