Objective:To explore some Fumaria species which were recorded to be traditionally used against malaria and other protozoal diseases.Methods:Consequently,in the current study,antiprotozoal effect of the ethanol extract...Objective:To explore some Fumaria species which were recorded to be traditionally used against malaria and other protozoal diseases.Methods:Consequently,in the current study,antiprotozoal effect of the ethanol extracts obtained from five Fumaria species(Fumaria densiflora,Fumaria cilicica,Fumaria rostellata,Fumaria kralikii,and Fumaria parviflora)was investigated against the parasites;Plasmodium falciparum(malaria)and Trypanosoma bruceirhodesiense(human African trypanosomiasis)at 0.81 and 4.85μg/mL concentrations.Results:Among them,Fumaria densiflora extract exerted the highest antiplasmodial(93.80%)and antitrypanasomal effect(55.40%),while the ethanol extracts of Fumaria kralikii(43.45%)and Fumaria rostellata(41.65%)showed moderate activity against Plasmodium falciparum.Besides,phenolic acid contents of the extracts were analyzed using high performance liquid chromatography(HPLC)and trans-cinnamic(4.32 mg/g)and caffeic(3.71 mg/g)acids were found to be the dominant phenolic acids in Fumaria densiflora.Conclusions:According to our results,Fumaria densiflora deserve further study for its promising antiprotozoal activity.展开更多
Introduction: Thymus vulgaris is used in traditional medicine to treat gastrointestinal diseases because of its antifungal, antibacterial, and antispasmodic activity. Objective: To verify whether Thymus vulgaris also ...Introduction: Thymus vulgaris is used in traditional medicine to treat gastrointestinal diseases because of its antifungal, antibacterial, and antispasmodic activity. Objective: To verify whether Thymus vulgaris also has antiprotozoal activity against Trichomonas vaginalis, Giardia lamblia and Entamoeba histolytica trophozoites. Materials and methods: Conventional cultures of parasites were measured on the third day during the logarithmic growth phase. The antiprotozoal activity of the methanol extract and its fractions were evaluated comparing growth in cultures with and without extracts. Next, the extract was fractionated by polarity-based partitioning. Then, the purity of each fraction was determined by thin layer chromatography (TLC). The percentage of growth inhibition was calculated with respect to untreated controls. The 50% inhibitory concentration (IC50) of each extract was calculated by PROBIT analysis. Results: We found that a methanol extract of the aerial parts of Thymus vulgaris, at 300 μg/mL, inhibited the in vitro growth of G. lamblia and T. vaginalis, while E. histolytica growth was poorly inhibited. The methanol extract was further separated into mixtures of ursolic, oleanolic, and betulinic acids. The IC50 values of ursolic acid against G. lamblia and T. vaginalis were 8.12 μg/mL and 5.51 μg/mL, respectively. Conclusions: The methanol extract fraction containing ursolic acid obtained from Thymus vulgaris has antiprotozoal activity against G. lamblia and T. vaginalis trophozoites.展开更多
The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosom...The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosoma (T. cruzi and T. brucei brucei), Leishmania infantum and chloroquine and pyrimethanine-resistant K1strain of P. falciparum and against MRC-5 cell-lines respectively. Results indicated that the 80% methanol extract showed a cytotoxic effect against MRC-5 cell lines with CC50 value of 0.54 μg/ml. It however exhibited pronounced and non selective activity against T. cruzi (IC50 = 1.52 μg/ml, SI = 0.03) and L. infantum (IC50 = 2.41 μg/ml, SI = 0.22). It however displayed pronounced and selective effect against T. brucei brucei (IC50 2.16) and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum (IC50 2.16). All soluble fractions and subfractions from the partition of the 80% methanol extract were found to exhibit an antiprotozoal activity with IC50 values ranging from T .cruzi, T. b. brucei, L. infantum and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values of 0.33, 81, 81 and >81 respectively. The chloroform soluble fraction rich in alkaloid was cytotoxic against MRC-5 cell lines (CC50 = 27.09 μg/ml) and showed good activity against T. b. brucei (IC50 = 8.36 and SI = 3.24) and moderate activity against T. cruzi, L. infantum and chloroquine-pyrimethane-resistant K1 strain of P. falciparum (20 50 50 = 1.55 and 0.43 μg/ml respectively), they however displayed pronounced antiprotozoal activity against T. cruzi, T. b. brucei and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values ranging from P. falciparum (SI = >6.2 and >1.72 respectively). These extracts however showed good and low activity respectively against L. infantum (IC50 = 24.05 and 6.82 μg/ml respectively).展开更多
Protozoan infections(e.g.,malaria,trypanosomiasis,and toxoplasmosis)pose a considerable global burden on public health and socioeconomic problems,leading to high rates of morbidity and mortality.Due to the limited ars...Protozoan infections(e.g.,malaria,trypanosomiasis,and toxoplasmosis)pose a considerable global burden on public health and socioeconomic problems,leading to high rates of morbidity and mortality.Due to the limited arsenal of effective drugs for these diseases,which are associated with devastating side effects and escalating drug resistance,there is an urgent need for innovative antiprotozoal drugs.The emergence of drug repurposing offers a low-cost approach to discovering new therapies for protozoan diseases.In this review,we summarize recent advances in drug repurposing for various human protozoan diseases and explore cost-effective strategies to identify viable new treatments.We highlight the cross-applicability of repurposed drugs across diverse diseases and harness common chemical motifs to provide new insights into drug design,facilitating the discovery of new antiprotozoal drugs.Challenges and opportunities in the field are discussed,delineating novel directions for ongoing and future research.展开更多
Parasitic disease is one of the most serious diseases in humans and animals. Animal antiparasitic drugs are mainly used to kill, expel and prevent animal parasites, and they are divided into anthelmintics, antiprotozo...Parasitic disease is one of the most serious diseases in humans and animals. Animal antiparasitic drugs are mainly used to kill, expel and prevent animal parasites, and they are divided into anthelmintics, antiprotozoals, insecticides, and so on. Animal antiparasitic drugs play an important role in the prevention and control of animal parasitic diseases, healthy development of animal husbandry and security of public health. In recent years, as people pay more attention paid to parasitic diseases, the research and development of antiparasitic drugs have made great progresses. Mastering the research and application progresses of antiparasitic drugs is of great significance to clinical medication and basic research. This paper reviews the history, current situation, the latest progresses and future development directions of research and application of antiparasitic drugs.展开更多
Objective:To determine the antibacterial,antifungal,antiprotozoal,cytotoxic,and phytochemical properties of ethanol extracts of leaves of Voacanga globosa(Blanco) Merr.(V.globosa). Methods:The extracts were tested aga...Objective:To determine the antibacterial,antifungal,antiprotozoal,cytotoxic,and phytochemical properties of ethanol extracts of leaves of Voacanga globosa(Blanco) Merr.(V.globosa). Methods:The extracts were tested against bacteria and fungus through disc diffusion assay; against protozoa through growth curve determination,antiprotozoal and cytotoxicity assays. Results:The extract revealed antibacterial activities,inhibiting the growth of Staphylococcus aureus,Bacillus cereus,Pseudomonas aeruginosa,Micrococcus luteus,and Salmonella typhimurium.Antifungal assay showed that it inhibited Candida albicans.The antiprotozoal assay against Trichomonas vaginalis and Entamoeba histolytica showed that V.globosa can inhibit the parasites,wherein the action can be comparable to metronidazole.With the in situ cell death detection kit.Trichomonas vaginalis and Entamoeba histolytica exposed to V.globosa leaf extract was observed to fluoresce simultaneously in red and yellow signals signifying apoptotic-like changes.Preliminary phytochemical screening revealed the chemical composition of plant extract containing alkaloids,saponins,2-deoxysugars,and hydrolysabie tannins.Conclusions: Thus,thus study provides scientific evidence on the traditional use of V.globosa leaf extract in treating microbial diseases.Further,the leaf extract can possibly be used to produce alternative forms of antimicrobials.展开更多
AIM:To investigate the efficacy and tolerability of albendazole and metranidazole treatment in giardiasis. METHODS:The open comparative randomized trial was carried out prospectively from December 1999 to July 2001 in...AIM:To investigate the efficacy and tolerability of albendazole and metranidazole treatment in giardiasis. METHODS:The open comparative randomized trial was carried out prospectively from December 1999 to July 2001 in Duzce City of Turkey.The diagnosis was based on the presence of signs and symptoms compatible with giardiasis including a positive stool examination of giardia cysts or trophozoite.Metranidazole group consisted of 29 patients and was given metranidazole 500 mg,three times a day for 5 d and albendazole group was consisted of 28 patients and was given albendazole 400 mg/d for 5 d. RESULTS:There were no significant differences in demographical and therapeutical effects and patient's compliance between both groups.But side effects were seen more in metranidazole group than in albendazole group. CONCLUSION:Albendazole is as effective as metranidazole in adults' giardiasis.Albendazole has less side effect potentials than metranidazole in the treatment of giardiasis.展开更多
Objective:To search for the most active antimicrobial and antioxidant sub-fractions related to traditional use of Ziziphus oxyphylla(Z.oxyphylla)and Cedrela serrata(C.serrata)in Pakistan against infectious and liver d...Objective:To search for the most active antimicrobial and antioxidant sub-fractions related to traditional use of Ziziphus oxyphylla(Z.oxyphylla)and Cedrela serrata(C.serrata)in Pakistan against infectious and liver diseases.Methods:Factions of different polarity were tested in vitro for their antiprotozoal,antimalarial,antibacterial and antifungal activity against different pathogens.Cytotoxicity on MRC-5 cell lines(human lung fibroblasts)as well as,in vitro radical scavenging activity was evaluated using the 1,1-diphenyl-2-picrylhydrazyl radical assay.Results:The highest antiprotozoal activity was observed for the CHCl_(3)fractions of Z.oxyphylla roots and leaves,and C.serrata bark.The CHCl_(3)and Et OAc fractions of Z.oxyphylla roots,the CHCl_(3)fraction of Z.oxyphylla leaves,the Et OAc and the residual Me OH:H_(2)O fraction of C.serrata bark showed antibacterial activity against Staphylococcus aureus.The same residual Me OH:H_(2)O fraction of C.serrata bark was active against Candida albicans.The highest antioxidant activity was observed for the more hydrophilic Et OAc fractions of Z.oxyphylla leaves,C.serrata bark and leaves,and the residual Me OH:H_(2)O fraction of C.serrata bark.Conclusions:This study supports at least in part the traditional uses of these plants for antimicrobial purposes and against liver diseases.展开更多
Results from the in vitro evaluation of the antiparasitaire activity of the aqueous extract, the 80% methanol extract and its fractions from the leaves of Brucea sumatrana against Trypanosoma brucei brucei, T. cruzi, ...Results from the in vitro evaluation of the antiparasitaire activity of the aqueous extract, the 80% methanol extract and its fractions from the leaves of Brucea sumatrana against Trypanosoma brucei brucei, T. cruzi, Leishmania infantum, the multidrug-resistant K1 and chloroquine-sensitive NF54 strains of Plasmodium falciparum indicated that all samples from the leaves extract presented interesting antiparasitaire activity at different extents. The 80% methanol extract, its chloroform acid, petroleum ether and 80% methanol soluble fractions and the aqueous extract exhibited strong activity against Trypanosoma b. brucei, T. cruzi, L. infantum and the multidrug-resistant K1 strain of P. falciparum with IC<sub>50</sub> values from <0.25 to 4.35 μg/ml as well as against chloroquine-sensitive NF54 strain of P. falciparum with IC<sub>50</sub> values ranging from <0.02 to 2.0.4 μg/ml. Most samples were cytotoxic against MRC-5 cell lines (0.2 <sub>50</sub>) < 34.24 μg/ml) and showed good selective effect against all tested parasites. In acute toxicity, the aqueous extract was found to be non-toxic and its LD<sub>50 </sub>was estimated to be greater than 5 g/kg. In addition, it did not significantly modify the concentration levels of some evaluated biochemical and hematological parameters in treated rats. These results constitute a scientific validation supporting and justifying the traditional use of the leaves of B. sumatrana for the treatment of malaria, sleeping sickness and at some extent Chagas disease.展开更多
文摘Objective:To explore some Fumaria species which were recorded to be traditionally used against malaria and other protozoal diseases.Methods:Consequently,in the current study,antiprotozoal effect of the ethanol extracts obtained from five Fumaria species(Fumaria densiflora,Fumaria cilicica,Fumaria rostellata,Fumaria kralikii,and Fumaria parviflora)was investigated against the parasites;Plasmodium falciparum(malaria)and Trypanosoma bruceirhodesiense(human African trypanosomiasis)at 0.81 and 4.85μg/mL concentrations.Results:Among them,Fumaria densiflora extract exerted the highest antiplasmodial(93.80%)and antitrypanasomal effect(55.40%),while the ethanol extracts of Fumaria kralikii(43.45%)and Fumaria rostellata(41.65%)showed moderate activity against Plasmodium falciparum.Besides,phenolic acid contents of the extracts were analyzed using high performance liquid chromatography(HPLC)and trans-cinnamic(4.32 mg/g)and caffeic(3.71 mg/g)acids were found to be the dominant phenolic acids in Fumaria densiflora.Conclusions:According to our results,Fumaria densiflora deserve further study for its promising antiprotozoal activity.
文摘Introduction: Thymus vulgaris is used in traditional medicine to treat gastrointestinal diseases because of its antifungal, antibacterial, and antispasmodic activity. Objective: To verify whether Thymus vulgaris also has antiprotozoal activity against Trichomonas vaginalis, Giardia lamblia and Entamoeba histolytica trophozoites. Materials and methods: Conventional cultures of parasites were measured on the third day during the logarithmic growth phase. The antiprotozoal activity of the methanol extract and its fractions were evaluated comparing growth in cultures with and without extracts. Next, the extract was fractionated by polarity-based partitioning. Then, the purity of each fraction was determined by thin layer chromatography (TLC). The percentage of growth inhibition was calculated with respect to untreated controls. The 50% inhibitory concentration (IC50) of each extract was calculated by PROBIT analysis. Results: We found that a methanol extract of the aerial parts of Thymus vulgaris, at 300 μg/mL, inhibited the in vitro growth of G. lamblia and T. vaginalis, while E. histolytica growth was poorly inhibited. The methanol extract was further separated into mixtures of ursolic, oleanolic, and betulinic acids. The IC50 values of ursolic acid against G. lamblia and T. vaginalis were 8.12 μg/mL and 5.51 μg/mL, respectively. Conclusions: The methanol extract fraction containing ursolic acid obtained from Thymus vulgaris has antiprotozoal activity against G. lamblia and T. vaginalis trophozoites.
文摘The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosoma (T. cruzi and T. brucei brucei), Leishmania infantum and chloroquine and pyrimethanine-resistant K1strain of P. falciparum and against MRC-5 cell-lines respectively. Results indicated that the 80% methanol extract showed a cytotoxic effect against MRC-5 cell lines with CC50 value of 0.54 μg/ml. It however exhibited pronounced and non selective activity against T. cruzi (IC50 = 1.52 μg/ml, SI = 0.03) and L. infantum (IC50 = 2.41 μg/ml, SI = 0.22). It however displayed pronounced and selective effect against T. brucei brucei (IC50 2.16) and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum (IC50 2.16). All soluble fractions and subfractions from the partition of the 80% methanol extract were found to exhibit an antiprotozoal activity with IC50 values ranging from T .cruzi, T. b. brucei, L. infantum and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values of 0.33, 81, 81 and >81 respectively. The chloroform soluble fraction rich in alkaloid was cytotoxic against MRC-5 cell lines (CC50 = 27.09 μg/ml) and showed good activity against T. b. brucei (IC50 = 8.36 and SI = 3.24) and moderate activity against T. cruzi, L. infantum and chloroquine-pyrimethane-resistant K1 strain of P. falciparum (20 50 50 = 1.55 and 0.43 μg/ml respectively), they however displayed pronounced antiprotozoal activity against T. cruzi, T. b. brucei and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values ranging from P. falciparum (SI = >6.2 and >1.72 respectively). These extracts however showed good and low activity respectively against L. infantum (IC50 = 24.05 and 6.82 μg/ml respectively).
基金financially supported by the National Natural Science Foundation of China(Grant Nos.:32270690 and 32070671)the Postdoctor Research Fund of West China Hospital,Sichuan University,China(Grant No.:2024HXBH059)。
文摘Protozoan infections(e.g.,malaria,trypanosomiasis,and toxoplasmosis)pose a considerable global burden on public health and socioeconomic problems,leading to high rates of morbidity and mortality.Due to the limited arsenal of effective drugs for these diseases,which are associated with devastating side effects and escalating drug resistance,there is an urgent need for innovative antiprotozoal drugs.The emergence of drug repurposing offers a low-cost approach to discovering new therapies for protozoan diseases.In this review,we summarize recent advances in drug repurposing for various human protozoan diseases and explore cost-effective strategies to identify viable new treatments.We highlight the cross-applicability of repurposed drugs across diverse diseases and harness common chemical motifs to provide new insights into drug design,facilitating the discovery of new antiprotozoal drugs.Challenges and opportunities in the field are discussed,delineating novel directions for ongoing and future research.
基金Supported by Earmarked Fund for China Agriculture Research System(CAR-38)Twelfth Five-Year National Key Technology Research and Development Program(2015BAD1101)~~
文摘Parasitic disease is one of the most serious diseases in humans and animals. Animal antiparasitic drugs are mainly used to kill, expel and prevent animal parasites, and they are divided into anthelmintics, antiprotozoals, insecticides, and so on. Animal antiparasitic drugs play an important role in the prevention and control of animal parasitic diseases, healthy development of animal husbandry and security of public health. In recent years, as people pay more attention paid to parasitic diseases, the research and development of antiparasitic drugs have made great progresses. Mastering the research and application progresses of antiparasitic drugs is of great significance to clinical medication and basic research. This paper reviews the history, current situation, the latest progresses and future development directions of research and application of antiparasitic drugs.
基金supported by a research grant from the Commission on Higher Education(CHED) of the Philippines
文摘Objective:To determine the antibacterial,antifungal,antiprotozoal,cytotoxic,and phytochemical properties of ethanol extracts of leaves of Voacanga globosa(Blanco) Merr.(V.globosa). Methods:The extracts were tested against bacteria and fungus through disc diffusion assay; against protozoa through growth curve determination,antiprotozoal and cytotoxicity assays. Results:The extract revealed antibacterial activities,inhibiting the growth of Staphylococcus aureus,Bacillus cereus,Pseudomonas aeruginosa,Micrococcus luteus,and Salmonella typhimurium.Antifungal assay showed that it inhibited Candida albicans.The antiprotozoal assay against Trichomonas vaginalis and Entamoeba histolytica showed that V.globosa can inhibit the parasites,wherein the action can be comparable to metronidazole.With the in situ cell death detection kit.Trichomonas vaginalis and Entamoeba histolytica exposed to V.globosa leaf extract was observed to fluoresce simultaneously in red and yellow signals signifying apoptotic-like changes.Preliminary phytochemical screening revealed the chemical composition of plant extract containing alkaloids,saponins,2-deoxysugars,and hydrolysabie tannins.Conclusions: Thus,thus study provides scientific evidence on the traditional use of V.globosa leaf extract in treating microbial diseases.Further,the leaf extract can possibly be used to produce alternative forms of antimicrobials.
文摘AIM:To investigate the efficacy and tolerability of albendazole and metranidazole treatment in giardiasis. METHODS:The open comparative randomized trial was carried out prospectively from December 1999 to July 2001 in Duzce City of Turkey.The diagnosis was based on the presence of signs and symptoms compatible with giardiasis including a positive stool examination of giardia cysts or trophozoite.Metranidazole group consisted of 29 patients and was given metranidazole 500 mg,three times a day for 5 d and albendazole group was consisted of 28 patients and was given albendazole 400 mg/d for 5 d. RESULTS:There were no significant differences in demographical and therapeutical effects and patient's compliance between both groups.But side effects were seen more in metranidazole group than in albendazole group. CONCLUSION:Albendazole is as effective as metranidazole in adults' giardiasis.Albendazole has less side effect potentials than metranidazole in the treatment of giardiasis.
基金the Higher Education Commission(HEC)of Pakistan for obtaining a fellowship with grant number(1-8/HEC/HRD/2011/2162)
文摘Objective:To search for the most active antimicrobial and antioxidant sub-fractions related to traditional use of Ziziphus oxyphylla(Z.oxyphylla)and Cedrela serrata(C.serrata)in Pakistan against infectious and liver diseases.Methods:Factions of different polarity were tested in vitro for their antiprotozoal,antimalarial,antibacterial and antifungal activity against different pathogens.Cytotoxicity on MRC-5 cell lines(human lung fibroblasts)as well as,in vitro radical scavenging activity was evaluated using the 1,1-diphenyl-2-picrylhydrazyl radical assay.Results:The highest antiprotozoal activity was observed for the CHCl_(3)fractions of Z.oxyphylla roots and leaves,and C.serrata bark.The CHCl_(3)and Et OAc fractions of Z.oxyphylla roots,the CHCl_(3)fraction of Z.oxyphylla leaves,the Et OAc and the residual Me OH:H_(2)O fraction of C.serrata bark showed antibacterial activity against Staphylococcus aureus.The same residual Me OH:H_(2)O fraction of C.serrata bark was active against Candida albicans.The highest antioxidant activity was observed for the more hydrophilic Et OAc fractions of Z.oxyphylla leaves,C.serrata bark and leaves,and the residual Me OH:H_(2)O fraction of C.serrata bark.Conclusions:This study supports at least in part the traditional uses of these plants for antimicrobial purposes and against liver diseases.
文摘Results from the in vitro evaluation of the antiparasitaire activity of the aqueous extract, the 80% methanol extract and its fractions from the leaves of Brucea sumatrana against Trypanosoma brucei brucei, T. cruzi, Leishmania infantum, the multidrug-resistant K1 and chloroquine-sensitive NF54 strains of Plasmodium falciparum indicated that all samples from the leaves extract presented interesting antiparasitaire activity at different extents. The 80% methanol extract, its chloroform acid, petroleum ether and 80% methanol soluble fractions and the aqueous extract exhibited strong activity against Trypanosoma b. brucei, T. cruzi, L. infantum and the multidrug-resistant K1 strain of P. falciparum with IC<sub>50</sub> values from <0.25 to 4.35 μg/ml as well as against chloroquine-sensitive NF54 strain of P. falciparum with IC<sub>50</sub> values ranging from <0.02 to 2.0.4 μg/ml. Most samples were cytotoxic against MRC-5 cell lines (0.2 <sub>50</sub>) < 34.24 μg/ml) and showed good selective effect against all tested parasites. In acute toxicity, the aqueous extract was found to be non-toxic and its LD<sub>50 </sub>was estimated to be greater than 5 g/kg. In addition, it did not significantly modify the concentration levels of some evaluated biochemical and hematological parameters in treated rats. These results constitute a scientific validation supporting and justifying the traditional use of the leaves of B. sumatrana for the treatment of malaria, sleeping sickness and at some extent Chagas disease.
