Spillage of cyst contents during surgical operation is the major cause of recurrence after hydatid cyst surgery. Instillation of a scolicidal agent into a hepatic hydatid cyst is the most commonly employed measure to prevent this complication. SB202190 is a pyridinyl imidazole derivative and is known to be a specific inhibitor of p38 MAPK. In the present study, the scolicidal effect of SB202190 was investigated. Freshly isolated Echinococcus granulosus protoscolices were subjected to SB202190 treatment (10, 20, 40, and 80 microM), and the effects on parasite viability were monitored by trypan blue staining. Corresponding effects were visualized by scanning and transmission electron microscopy. Dose-dependent protoscolex death within a few days of SB202190 treatment was observed. Although the in vitro scolicidal effect of SB202190 was satisfactory, the in vivo efficacy of this drug and also possible side effects remain to be further investigated.
Animals ; Anthelmintics/*pharmacology ; Dose-Response Relationship, Drug ; Echinococcus granulosus/*drug effects/ultrastructure ; Imidazoles/*pharmacology ; Microscopy, Electron, Scanning ; Microscopy, Electron, Transmission ; Parasitic Sensitivity Tests ; Pyridines/*pharmacology ; Survival Analysis

Treatment of hydatid disease is mainly surgical, with medical treatment being reserved as a coadjuvant treatment. Use of effective scolicidal agents during surgery of cystic echinococcosis is essential to reduce the recurrence rate. The goal of this study was to evaluate the in vitro scolicidal effects of hydroalcoholic extracts of Satureja khuzestanica leaves and aqueous extracts of Olea europaea leaves on hydatid cyst protoscolices. Echinococcus granulosus protoscolices were collected from the liver of sheep infected with the hydatid cyst. Various concentrations of plant extracts were used in different exposure times for viability assay of protoscolices. Among the olive leaf extracts tested, 0.1% and 0.01% concentrations had strong scolicidal effects in 120 min. S. khuzestanica 0.1% had very strong scolicidal effects in 30, 60, and 120 min of exposure times and the mortality rate decreased with the lower concentration. The finding have shown that the scolicidal activity of S. khuzestanica against cystic echinococosis protoscolices were more effective, while the O. europaea extract showed less effects.
Animals ; Anthelmintics/*pharmacology ; Dose-Response Relationship, Drug ; Echinococcosis/drug therapy/*parasitology ; Echinococcus granulosus/drug effects/physiology ; Humans ; Olea/*chemistry ; Plant Extracts/*pharmacology ; Plant Leaves/chemistry ; Satureja/*chemistry

Animals ; Anthelmintics ; pharmacology ; therapeutic use ; Culture Media ; Echinococcosis ; drug therapy ; parasitology ; Echinococcus granulosus ; drug effects ; growth & development ; pathogenicity ; ultrastructure ; Parasitic Sensitivity Tests

AIMTo synthesize novel derivatives of hydroxylbenzenedisulfonanilide with high insecticidal activity against the Fasciola hepatica.

METHODSo-(m-, p-) Chlorphenol were used to synthesize the title compounds by sulphonation and nucleiphilic-substitution reaction. The uncoupling activity (insecticidal activity) of these compounds were tested by determining the influence on mitochondrial respiration control ratio (RCR) and the variation of inorganic phosphate in oxidative phosphorylation (delta Pi).

RESULTSCompounds 1-14 are new compounds. The structures of the compounds were determined by IR, HNMR and elemental analysis. Most new compounds have relatively high uncoupling activities, especially compounds 3, 5, 6 and 9.

CONCLUSIONCompounds 3, 5, 6 and 9 will become novel fasciolicides and are worth further studying.

Anilides ; chemical synthesis ; chemistry ; pharmacology ; Animals ; Anthelmintics ; chemical synthesis ; chemistry ; pharmacology ; Fasciola hepatica ; drug effects ; Mitochondria, Liver ; physiology ; Molecular Structure ; Oxygen Consumption ; drug effects ; Sulfonamides ; chemical synthesis ; chemistry ; pharmacology

Spigelia anthelmia Linn is used as a herb and is a common annual weed of cultivation in open re-growths, on unused land in towns as well as on road sides. The plant can grow to approximately 30 cm in height. The aim of this study was to screen extracts of Spigelia anthelmia for their anthelmintic activity against an experimental Nippostrongylus braziliensis infection in rats. Acute oral toxicity occurred at a dose of 1,140 mg/kg, while anthelmintic trials against Nippostrongylus braziliensis in rats using the aqueous fraction showed a progressive decrease in worm count with increasing dose (10, 13, 16, 20 and 25 mg per kg body weight) (p < 0.05). At 25 mg per kg body weight, the worm count was significantly lower than that at 10 mg per kg body weight (p < 0.05).
Animals ; Anthelmintics/*pharmacology/toxicity ; Drug Evaluation, Preclinical ; Lethal Dose 50 ; Loganiaceae/*chemistry ; Medicine, African Traditional ; Nigeria ; Nippostrongylus/*growth&development ; Phytotherapy/*methods ; Plant Extracts/*pharmacology/toxicity ; Rats ; Rats, Wistar ; Strongylida Infections/*drug therapy/parasitology

The present work evaluated the effects of alcoholic extracts of salvia (Salvia officinalis), thyme (Thymus vulgaris), and 2 pure compounds (thymol and menthol) on the viability of Echinococcus granulosus protoscolices in vitro. Four different concentrations of each extract (2,500, 1,500, 1,000, and 500 microg/ml) and 3 different concentrations each of thymol and menthol (50, 10, and 1 microg/ml) were used. Concentration of 2,500 microg/ml of both extracts showed a significant protoscolicidal activity on the 6th day. Complete loss of viability of protoscolices occurred with 500 microg/ml concentration of both extracts at day 6 and day 7 post-treatment (PT), respectively. Pure compounds, i.e., menthol and thymol, showed potent effects with 50 microg/ml concentration at day 2 and day 5 PT, respectively. These effects were compared with those of albendazole sulfoxide (800 microg/ml), a commonly used treatment drug for hydatidosis. Krebs-Ringer solution and the hydatid cystic fluid at a ratio of 4:1 was a good preservative solution which kept the protoscolices viable for 15 days.
Animals ; Anthelmintics/isolation & purification/*pharmacology ; Camels ; Cell Survival/drug effects ; Echinococcosis, Pulmonary/*parasitology ; Echinococcus granulosus/*drug effects/isolation & purification ; Lung/parasitology ; Medicine, Traditional/methods ; Plant Extracts/isolation & purification/*pharmacology ; Plants, Medicinal/*chemistry ; Salvia officinalis/chemistry ; Thymus Plant/chemistry ; Time Factors

A number of herbs belonging to the genus Jatropha of Euphorbiaceae family are noted for their medicinal benefits. The genus Jatropha is one of the prospective biodiesel yielding crops. The plants which have been so far explored include J. curcas, J. gossypifolia, J. glandulifera, J. multifida and J. podagrica. Although, the plants of this genus are widely distributed, there is an exiguity of scientific literature proclaiming the medicinal benefits of the plants belonging to genus Jatropha. The present paper is a pragmatic approach to accrue the findings on this very significant genus.
Analgesics ; pharmacology ; therapeutic use ; Animals ; Anthelmintics ; pharmacology ; therapeutic use ; Anti-Inflammatory Agents ; pharmacology ; therapeutic use ; Anticonvulsants ; pharmacology ; therapeutic use ; Antidiarrheals ; pharmacology ; therapeutic use ; Antineoplastic Agents, Phytogenic ; pharmacology ; therapeutic use ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Humans ; Hypoglycemic Agents ; pharmacology ; therapeutic use ; Jatropha ; chemistry ; classification

The methanolic extract obtained from the root portion of Caltha palustris var. alba was evaluated for its anthelmintic efficacy against gastrointestinal nematodes of sheep under both in vitro and in vivo conditions using worm motility inhibition (WMI) assay and fecal egg count reduction (FECR) assay, respectively. The extract was subjected to antimicrobial activity using agar-well diffusion method against different bacterial strains. In addition the extract was evaluated for cytotoxic and antioxidant activity against cultured THP-1(Leukemia), A-549 (Lung), HCT-15 (Colon), Cervix (HeLa) and PC-3(Prostrate) cell lines by SRB and DPPH radical scavenging assays. The extract used resulted in mean %WMI of 94.44%, as observed when the worms were put in lukewarm buffer for 30 min after exposure to different treatments. The mean mortality index of the sample was 0.95. The lethal concentration (LC50) was 0.11 mg·mL(-1). Cell lines were exposed to concentration of 100 μg·mL(-1) of extract for 48 h, which reduced the viability of these cell lines. The same plant extract also showed 55.58% DPPH radical scavenging activity.
Animals ; Anthelmintics ; pharmacology ; Anti-Bacterial Agents ; pharmacology ; Antineoplastic Agents, Phytogenic ; pharmacology ; therapeutic use ; Antioxidants ; pharmacology ; Bacteria ; drug effects ; Biphenyl Compounds ; metabolism ; Feces ; parasitology ; Gastrointestinal Tract ; parasitology ; HeLa Cells ; Humans ; Nematoda ; drug effects ; Neoplasms ; drug therapy ; Phytotherapy ; Picrates ; metabolism ; Plant Extracts ; pharmacology ; therapeutic use ; Ranunculaceae ; Sheep ; parasitology

Surgery remains the preferred treatment for hydatid cyst (cystic echinococcosis, CE). Various scolicidal agents have been used for inactivation of protoscolices during surgery, but most of them are associated with adverse side effects. The present study aimed to evaluate the in vitro scolicidal effect of Nigella sativa (Ranunculaceae) essential oil and also its active principle, thymoquinone, against protoscolices of hydatid cysts. Protoscolices were aseptically aspirated from sheep livers having hydatid cysts. Various concentrations of the essential oil (0.01-10 mg/ml) and thymoquinone (0.125-1.0 mg/ml) were used for 5 to 60 min. Viability of protoscolices was confirmed by 0.1% eosin staining. Furthermore, the components of the N. sativa essential oil were identified by gas chromatography/mass spectroscopy (GC/MS). Our study revealed that the essential oil of N. sativa at the concentration of 10 mg/ml and its main component, thymoquinone, at the concentration of 1 mg/ml had potent scolicidal activities against protoscolices of Echinococcus granulosus after 10 min exposure. Moreover, thymoquinone (42.4%), p-cymene (14.1%), carvacrol (10.3%), and longifolene (6.1%) were found to be the major components of N. sativa essential oil by GC/MS analysis. The results of this study indicated the potential of N. sativa as a natural source for production of a new scolicidal agent for use in hydatid cyst surgery. However, further studies will be needed to confirm these results by checking the essential oil and its active component in in vivo models.
Animals ; Anthelmintics/isolation & purification/*pharmacology ; Benzoquinones/isolation & purification/*pharmacology ; Biological Assay ; Echinococcosis/parasitology/veterinary ; Echinococcus granulosus/*drug effects/isolation & purification ; Gas Chromatography-Mass Spectrometry ; Nigella sativa/*chemistry ; Oils, Volatile/chemistry/isolation & purification/*pharmacology ; Seeds/chemistry ; Sheep ; Sheep Diseases/parasitology ; Survival Analysis ; Time Factors

The fact that the fruit and bark of plant belonging to family Melia could be used as digestive tract-parasiticide and agricultural insecticide was recorded about two thousand years ago in ancient China. Toosendanin (TSN, C30H38O11, FW=574), a triterpenoid derivative, was extracted from the bark of Melia toosendan Sieb. et Zucc. by Chinese scientists in 1950os and used as an ascarifuge in China instead of imported sendanin. Studies have demonstrated that TSN possesses special biological actions as well as considerable various values in scientific research, clinic medicine and agriculture. The first is that by interfering with neurotransmitter release by causing an initial facilitation, TSN eventually blocks synaptic transmission at both the neuromuscular junction and central synapses. The action might result from TSN-induced Ca(2+)-sensitivity change and final elimination of transmitter release machinery. The second is that despite sharing many similar actions with botulinum neurotoxin (BoNT) on blocking neuromuscular transmission, TSN has a markedly antibotulismic action in vivo and in vitro: TSN-treatment saves the botulism mice or monkeys from death; TSN-incubation in vitro or TSN-injection in vivo endows neuromuscular junction with a high tolerance to BoNT. Studies suggest that the antibotulismic action is achieved by preventing BoNT from approaching its enzymatic substrate, SNARE protein. The third, in recent years, it is also observed that TSN can induce differentiation and apoptosis in several cell lines, and suppress proliferation of various human cancer cells. The TSN-induced differentiation is Ca(2+)-dependent and the mitochondria-dependent apoptosis pathway is involved in the TSN-induced apoptosis. The fourth is that TSN inhibits various K(+) channels and selectively facilitates Ca(2+) current through L-type Ca(2+) channels and hence elevates [Ca(2+)](i). The TSN-induced [Ca(2+)](i) increase and overload could be responsible for the TSN-induced biphasic effect on neurotransmitter release, cell differentiation, apoptosis as well as the cytotoxicity of TSN.
Animals ; Anthelmintics ; pharmacology ; Apoptosis ; drug effects ; Ascariasis ; drug therapy ; Botulinum Toxins ; antagonists & inhibitors ; Calcium ; metabolism ; Calcium Channels, L-Type ; drug effects ; Cell Differentiation ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; Humans ; Medicine, Chinese Traditional ; Potassium Channel Blockers ; pharmacology ; Synaptic Transmission ; drug effects