RESUMEN
Pithecellobium dulce is distributed in America and Asia where is widely used in traditional medicine. This study describes the bioguided fractionation of the methanol extract (ME) obtained from the P. dulce fruit that showed in vitro activity against Hymenolepis nana; Artemia salina assay was used to determine toxicity; and the purified compound was computationally analysed to obtain its absorption-distribution-metabolism-excretion-and-toxicity properties (ADMET). The ME and its fractions were more active than praziquantel (PZQ), and the purified compound was characterized as N-malonyl-(+)-tryptophan (NMT). Parasites treated with NMT showed shorter paralysis and death times (5 and 7 min) than those treated with PZQ (15 and 30 min), both used at 20 mg/mL. Toxicity and ADMET prediction results supported the slight-hazardousness and efficacy of the assayed fractions/compound. This is the first report of the antiparasitary activity of both the P. dulce ME and NMT, showing their potential to treat human H. nana infections.
Asunto(s)
Fabaceae/química , Frutas/química , Hymenolepis nana/fisiología , Triptófano/aislamiento & purificación , Triptófano/farmacología , Animales , Artemia/efectos de los fármacos , Fraccionamiento Químico , Humanos , Hymenolepis nana/efectos de los fármacos , Extractos Vegetales/farmacologíaRESUMEN
OBJECTIVE: The main drug used against Hymenolepis nana is praziquantel (PZQ), which causes side effects and toxicity. In contrast, natural extracts have limited side effects and are safer. Past researches have proved that pumpkin seeds are effective as natural antimicrobial and antiparasitic treatment. The present study investigates a natural alternative and less expensive treatment against H. nana using pumpkin seeds. MATERIALS AND METHODS: Healthy female albino mice were divided into four groups: normal control, infected control with H. nana, infected and treated with PZQ, and lastly, the group infected and treated with pumpkin seeds' extract. RESULTS: Pumpkin seeds aqueous extract showed a significant reduction (P < 0.05) in the number and length of H. nana adult worms, number and viability of eggs in comparison to the infected control group and PZQ group. Pumpkin seed aqueous extract is proven to be an effective anthelmintic against H. nana. CONCLUSION: We recommend pumpkin seed extract as a natural alternative, less expensive and safe therapy for H. nana. This is the first study in Saudi Arabia to investigate the therapeutic effect of pumpkin seeds' extract on H. nana.
Asunto(s)
Antihelmínticos/farmacología , Cucurbita/química , Hymenolepis nana/efectos de los fármacos , Extractos Vegetales/farmacología , Semillas/química , Animales , Heces/parasitología , Femenino , Ratones , Recuento de Huevos de Parásitos , Praziquantel/farmacologíaRESUMEN
Hymenolepis nana is a common intestinal tapeworm that affects humans. Drugs are available for the treatment of this infection, including praziquantel (PZQ), nitazoxanide and niclosamide. Although the drug of choice is praziquantel, due to its high cure rates, indicators of the development of PZQ resistance by different parasites have begun to appear over recent decades. Therefore, this study was a trial to find an alternative to PZQ by assessing the activity of the crude aqueous extract of the medicinal herb Artemisia absinthium against H. nana. In vitro, the extract was used against adult worms at concentrations of 1 and 5 mg/ml, in comparison with 1 mg/ml of PZQ. The times of worm paralysis and death were determined. Ultrastructural morphological changes were studied using transmission electron microscopy (TEM). For the in vivo study, infected mice were divided into untreated, PZQ-treated and A. absinthium-treated groups (400 mg/kg and 800 mg/kg). Pre- and post-treatment egg counts per gram of faeces (EPG) were performed; then, the reduction percentages of the EPG and worm burden were calculated. The best results were obtained with praziquantel. Artemisia absinthium induced worm paralysis, death and ultrastructural alterations, such as tegumental damage, lipid accumulation, and destruction of the nephridial canal and the intrauterine eggs, in a dose-dependent manner. Additionally, significant reductions in the EPG and worm burden were recorded in A. absinthium-treated mice. Although the results obtained with A. absinthium were promising and comparable to PZQ, further studies using different extracts, active ingredients and concentrations against different parasites should be conducted.
Asunto(s)
Artemisia absinthium/química , Hymenolepis nana/efectos de los fármacos , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Praziquantel/farmacología , Praziquantel/uso terapéutico , Animales , Antihelmínticos/administración & dosificación , Antihelmínticos/farmacología , Antihelmínticos/uso terapéutico , Heces/parasitología , Himenolepiasis/tratamiento farmacológico , Himenolepiasis/parasitología , Hymenolepis nana/ultraestructura , Ratones , Microscopía Electrónica de Transmisión , Recuento de Huevos de Parásitos , Extractos Vegetales/administración & dosificación , Praziquantel/administración & dosificaciónRESUMEN
BACKGROUND: Embelia schimperi has been used for the treatment of intestinal parasites especially tapeworm infestations for centuries in Ethiopia. However, there is lack of scientific based evidences regarding the efficacy, safety and phytochemical analysis of this plant despite its frequent use as an anthelmintic. This study has therefore evaluated the efficacy and acute toxicity of E. schimperi thereby generating relevant preclinical information. METHODS: The anthelmintic activities of the crude hydroalcoholic extract of E. schimperi and the isolated compound, embelin, were conducted using in vivo and in vitro models against the dwarf tapeworm, Hymenolepis nana, and the hookworm, Necator americanus, respectively. LD50 of the crude hydroalcoholic extract was determined using Swiss albino mice following the OECD guidelines. Chemical characterization of the isolated embelin was conducted using UV-spectroscopy, HPLC and NMR. RESULTS: In the acute toxicity study no prominent signs of toxicity and mortality were recorded among the experimental animals at the highest administered dose. Hence the LD50 of the plant was found to be higher than 5000 mg/kg. In vivo cestocidal activity of the crude hydroalcoholic extract of E. schimperi showed 100% parasite clearance at 1000 mg/kg, while the diammonium salt of embelin showed 85.3% parasite clearance at 750 mg/kg. The in vitro anthelminthic activity study revealed that the LC50 value of the crude extract and albendazole were 228.7 and 51.33 µg/mL, respectively. CONCLUSION: The results clearly indicated that the hydroalcoholic extract of E. schimperi and the diammonium salt of the isolated compound embelin had anthelmintic activity against hookworm larva in vitro and H. nana in vivo. Hence the findings of this study showed Embelia schimperi appears to possess some anthelmintic activity that may support the usage of these plants by local traditional healers to treat helminthic infestations.
Asunto(s)
Antihelmínticos , Embelia/química , Extractos Vegetales , Plantas Medicinales/química , Animales , Antihelmínticos/química , Antihelmínticos/farmacología , Etiopía , Himenolepiasis/parasitología , Hymenolepis nana/efectos de los fármacos , Ratones , Extractos Vegetales/química , Extractos Vegetales/farmacologíaRESUMEN
This study investigated the anthelmintic activity of gingerenone A, [6]-dehydrogingerdione, [4]-shogaol, 5-hydroxy-[6]-gingerol, [6]-shogaol, [6]-gingerol, [10]-shogaol, [10]-gingerol, hexahydrocurcumin, 3R,5S-[6]-gingerdiol and 3S,5S-[6]-gingerdiol, a constituent isolate from the roots of ginger, for the parasite Hymenolepis nana. The cestocidal activity or ability to halt spontaneous parasite movement (oscillation/peristalsis) in H. nana of above constituents was reached from 24 to 72h in a time- and dose-dependent manner, respectively. The [10]-shogaol and [10]-gingero1 have maximum lethal efficacy and loss of spontaneous movement than the others at 24-72h. In addition, worms treated with 1 and 10µM [10]-gingero1, more than 30% had spontaneous movement of oscillation at 72h but [10]-shogaol at 72h only about 15-20% of oscillation. This showing that [10]-gingero1 had less loss of spontaneous movement efficacy than [10]-shogaol. After exposure to 200µM [10]-shogaol, 100% of H. nana had died at 12h rather than died at 24h for [10]-gingerol, showing that [10]-gingero1 had less lethal efficacy than [10]-shogaol. In addition, these constituents of ginger showed effects against peroxyl radical under cestocidal activity. In order to evaluate the cestocidal activity and cytokine production caused by ginger's extract R0 in the H. nana infected mice, we carried out in vivo examination about H. nana infected mice BALB/c mice were inoculated orally with 500 eggs. After post-inoculation, R0 (1g/kg/day) was administered orally for 10 days. The R0 exhibited cestocidal activity in vivo of significantly reduced worms number and cytokines production by in vitro Con A-stimulated spleen cells showed that INF-γ and IL-2 were significantly increases by R0. IL-4, IL-5, IL-6, IL-10 and IL-13 were significantly decreases and Murine KC and IL-12 were not significantly changes by R0. Together, these findings first suggest that these constituents of ginger might be used as cestocidal agents against H. nana.
Asunto(s)
Antihelmínticos/farmacología , Hymenolepis nana/efectos de los fármacos , Fitoterapia , Extractos Vegetales/farmacología , Zingiber officinale , Animales , Ratones , Ratones Endogámicos BALB C , Raíces de Plantas , RizomaRESUMEN
Hymenolepis nana (H. nana) is the most common tapeworm infection worldwide. It is more prevalent in warm climates where sanitation is poor, particularly among children. The effect and mechanism of action of praziquantel (PZQ), given at a dose of 25-mg/kg BW, and Carica papaya dried seed crude aqueous extract (CAE), given at a dose of 1.2-g/kg BW, were assessed on H. nana worms in experimentally infected mice. Tegumental changes were studied using the scanning electron microscope (SEM) and different parasitological parameters were observed. Each group of infected mice was divided into two subgroups. The first subgroup received either treatment before the 4th day after infection to investigate their effects on the cysticercoid stage. The other subgroup received treatments after the development of the adult stage, confirmed by eggs detection in stool. Both PZQ and C. papaya dried seed CAE resulted in a significant reduction of worm burden, total egg output and viable egg count. Marked tegumental changes were evident in adult worms treated with either treatment including shrinkage of the scolex and neck region with rostellar edema and complete loss of its hooks. However, all previous effects were exerted more rapidly in the case of PZQ treatment. They both significantly reduced cysticercoid stage size. Nevertheless, C. papaya outstand PZQ in having a deforming effect on adults arising from treated cysticercoids. It was concluded that C. papaya has significant anti-cestodal properties that enable its seed extract to be a very effective alternative to PZQ against H. nana.
Asunto(s)
Antihelmínticos/farmacología , Carica/química , Himenolepiasis/tratamiento farmacológico , Extractos Vegetales/farmacología , Praziquantel/farmacología , Animales , Hymenolepis nana/efectos de los fármacos , Hymenolepis nana/ultraestructura , Ratones , Microscopía Electrónica de Rastreo , Recuento de Huevos de Parásitos , Semillas/químicaRESUMEN
Nelumbo nucifera Gaertn. cv. Rosa-plena (Nelumbonaceae), commonly known as lotus, is a perennial aquatic plant grown and consumed throughout Asia. All parts of N. nucifera have been used for various medicinal purposes in oriental medicine. From the leaves of Nelumbo nucifera Gaertn. cv. Rosa-plena (an aquatic plant), liriodenine (1), lysicamine (2), (-)-anonaine (3), (-)-asimilobine (4), (-)-caaverine (5), (-)-N-methylasimilobine (6), (-)-nuciferine (7), (-)-nornuciferine (8), (-)-roemerine (9), 7-hydroxydehydronuciferine (10) and cepharadione B (11) were isolated and identification and anthelmintic activities of aporphine was evaluated against Anisakis simplex and Hymenolepis nana. This study found that the above constituents killed H. nana or reduced their spontaneous movements (oscillation/peristalsis). However, the above constituents at various concentrations demonstrated no larvicidal effect or ability to halt spontaneous parasite movement for 72 h against A. simplex, respectively. In addition, according to an assay of cestocidal activity against H. nana and nematocidal activity against A. simplex, we found that the above compounds showed greater lethal efficacy on H. nana than against A. simplex. Further investigation showed that these above constituents have effects against peroxyl radicals under cestocidal effect. Together, these findings suggest that these constituents of Nelumbo nucifera Gaertn. cv. Rosa-plena might be used as anthelmintic agents against H. nana.
Asunto(s)
Antihelmínticos/farmacología , Aporfinas/farmacología , Hymenolepis nana/efectos de los fármacos , Nelumbo/química , Alcaloides/aislamiento & purificación , Alcaloides/farmacología , Animales , Anisakis/efectos de los fármacos , Anisakis/fisiología , Antihelmínticos/aislamiento & purificación , Aporfinas/aislamiento & purificación , Medicamentos Herbarios Chinos/farmacología , Hymenolepis nana/fisiología , Movimiento/efectos de los fármacos , Hojas de la Planta/química , Factores de TiempoRESUMEN
BACKGROUND: Alpinia oxyphylla is a common remedy in traditional Chinese medicine. Yakuchinone A is a major constituent of A. oxyphylla and exhibits anti-inflammatory, antitumor, antibacterial, and gastric protective activities. METHODS: Antioxidant and antitumor characteristics of yakuchinone A in skin cancer cells as well as novel mechanisms for the inhibition of adipocyte differentiation, cestocidal activities against Hymenolepis nana adults, and nematocidal activities against Anisakis simplex larvae are investigated. RESULTS: Yakuchinone A presents the ability of the removal of DPPH·and ABTS+ free radicals and inhibition of lipid peroxidation. Yakuchinone A suppresses intracellular lipid accumulation during adipocyte differentiation in 3 T3-L1 cells and the expressions of leptin and peroxisome proliferator-activated receptor γ (PPARγ). Yakuchinone A induces apoptosis and inhibits cell proliferation in skin cancer cells. The inhibition of cell growth by yakuchinone A is more significant for non-melanoma skin cancer (NMSC) cells than for melanoma (A375 and B16) and noncancerous (HaCaT and BNLCL2) cells. Treatment BCC cells with yakuchinone A shows down-regulation of Bcl-2, up-regulation of Bax, and an increase in cleavage poly (ADP-ribose) polymerase (PARP). This suggests that yakuchinone A induces BCC cells apoptosis through the Bcl-2-mediated signaling pathway. The anthelmintic activities of yakuchinone A for A. simplex are better than for H. nana. CONCLUSIONS: In this work, yakuchinone A exhibits antioxidative properties, anti-adipocyte differentiation, antitumor activity, and anthelmintic activities against A. simplex and H. nana.
Asunto(s)
Alpinia/química , Antihelmínticos/farmacología , Antioxidantes/farmacología , Diferenciación Celular/efectos de los fármacos , Guayacol/análogos & derivados , Adipocitos/citología , Adipocitos/efectos de los fármacos , Adipogénesis/efectos de los fármacos , Animales , Anisakis/efectos de los fármacos , Antihelmínticos/química , Antioxidantes/química , Apoptosis/efectos de los fármacos , Línea Celular , Supervivencia Celular/efectos de los fármacos , Guayacol/química , Guayacol/farmacología , Humanos , Hymenolepis nana/efectos de los fármacos , Larva/efectos de los fármacos , Extractos Vegetales/química , Extractos Vegetales/farmacología , Transducción de Señal/efectos de los fármacosAsunto(s)
Anticestodos/uso terapéutico , Benzamidas/uso terapéutico , Himenolepiasis/tratamiento farmacológico , Hymenolepis nana/efectos de los fármacos , Nitrobencenos/uso terapéutico , Animales , Anticestodos/administración & dosificación , Anticestodos/química , Benzamidas/química , Benzamidas/farmacología , Modelos Animales de Enfermedad , Evaluación Preclínica de Medicamentos , Ratones , Nitrobencenos/química , Nitrobencenos/farmacologíaAsunto(s)
Anticestodos/farmacología , Benzamidas/farmacología , Himenolepiasis/tratamiento farmacológico , Hymenolepis nana/efectos de los fármacos , Animales , Anticestodos/química , Anticestodos/uso terapéutico , Benzamidas/química , Benzamidas/uso terapéutico , Evaluación Preclínica de Medicamentos , RatonesAsunto(s)
Anticestodos/uso terapéutico , Benzamidas/uso terapéutico , Bromobencenos/uso terapéutico , Himenolepiasis/tratamiento farmacológico , Hymenolepis nana/efectos de los fármacos , Nitrobencenos/uso terapéutico , Animales , Anticestodos/química , Benzamidas/química , Bromobencenos/química , Evaluación Preclínica de Medicamentos , Nitrobencenos/químicaAsunto(s)
Anticestodos/uso terapéutico , Benzamidas/uso terapéutico , Bromobencenos/uso terapéutico , Himenolepiasis/tratamiento farmacológico , Hymenolepis nana/efectos de los fármacos , Administración Oral , Animales , Anticestodos/administración & dosificación , Benzamidas/administración & dosificación , Bromobencenos/administración & dosificación , Evaluación Preclínica de Medicamentos , RatonesAsunto(s)
Anticestodos/uso terapéutico , Benzamidas/uso terapéutico , Himenolepiasis/tratamiento farmacológico , Hymenolepis nana/efectos de los fármacos , Animales , Anticestodos/química , Anticestodos/farmacología , Benzamidas/química , Benzamidas/farmacología , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos , Ratones , Ratones EndogámicosRESUMEN
OBJECTIVE: To investigate the antiparasitic effect of Nigella sativa oil (NSO) on Aspiculuris tetraptera (A. tetraptera) and Hymenolepis nana (H.nana) in mice in January 2005. METHODS: Mice were obtained from the animal house facility of the Faculty of Medicine, Yuzuncu Yil University, Van, Turkey. The natural infections were determined by the cellophane tape method and the centrifugal flotation method of stool samples. The infected mice with A. tetraptera and H.nana were divided into 4 groups; 2 treatment and 2 control groups. Nigella sativa oil was given at the dose of 250 ul/kg body weight orally for 2 consecutive days in the 2 treatment groups. All the mice were sacrificed on the seventh day after the last treatment. Gastrointestinal tract of the sacrificed animals was opened and washed with a serum physiologic. The contents were examined under a stereo microscope for counting and identifying of the parasites. The treatment and the control groups were compared using Mann-Whitney U-Test. RESULTS: Nigella sativa oil reduced both A. tetraptera and its eggs. The difference was significant between Group 1 and Group 3 (p<0.05). Nigella sativa oil reduced H.nana eggs starting from second day of the treatment until necropsy day during 5 days, but it was not significant between Group 2 and Group 4 (p>0.05). CONCLUSION: Antiparasitic effect of NSO is related to its stimulating immune system.
Asunto(s)
Antihelmínticos/farmacología , Himenolepiasis/veterinaria , Hymenolepis nana/efectos de los fármacos , Ratones/parasitología , Nigella sativa , Oxiuriasis/veterinaria , Aceites de Plantas/farmacología , Enfermedades de los Roedores/tratamiento farmacológico , Animales , Heces/parasitología , Himenolepiasis/tratamiento farmacológico , Masculino , Oxiuriasis/tratamiento farmacológico , Enfermedades de los Roedores/parasitología , Estadísticas no ParamétricasRESUMEN
The efficacy and safety of Mirazid in treatment of human hymenolepiosis were carried out in a rural village in Talkha Center (Dakahlia G.). Kato thick smear stool examination showed 51 cases of Hymenolepis nana (9 of them had concomitant parasitosis), two cases of H. dimninuta. Mirazid was given in a dose of 10 mg/kg/d for nine consecutive days an hour before breakfast for hymenolepiosis cases, as capsule for adults and suppository for children. All cases were subjected to history taking before treatment and six weeks post-treatment and stool examination was repeated as well weekly for six weeks post-treatment. There was overt clinical improvement. Side effects were negligible. Parasitologic cure rate was 40/41 or 95.2% for H. nana one week post-treatment, and 100% for H. diminuta one week post-treatment, up to six weeks follow-up for all treated patients. Two unresponded H. nana patients were cured by another Mirazid course.