The relative anthelmintic efficacy of plant-derived cysteine proteinases on intestinal nematodes

2013 ◽  
Vol 89 (2) ◽  
pp. 165-174 ◽  
Author(s):  
W. Luoga ◽  
F. Mansur ◽  
D.J. Buttle ◽  
I.R. Duce ◽  
M.C. Garnett ◽  
...  
Keyword(s):  
Ananas Comosus ◽  
Cysteine Proteinases ◽  
Kiwi Fruit ◽  
Intestinal Nematode ◽  
Anthelmintic Efficacy ◽  
Heligmosomoides Bakeri ◽  
Papaya Latex ◽  
Stem Bromelain

AbstractWe examined the in vitro and in vivo efficacy of plant cysteine proteinases (CPs) derived from pineapple (Ananas comosus) and kiwi fruit (Actinidia deliciosa), and compared their efficacy as anthelmintics to the known effects of CPs from the latex of papaya (Carica papaya) against the rodent intestinal nematode, Heligmosomoides bakeri. Both fruit bromelain and stem bromelain had significant in vitro detrimental effects on H. bakeri but in comparison, actinidain from kiwi fruit had very little effect. However, in vivo trials indicated far less efficacy of stem bromelain and fruit bromelain than that expected from the in vitro experiments (24.5% and 22.4% reduction in worm burdens, respectively) against H. bakeri. Scanning electron microscopy revealed signs of cuticular damage on worms incubated in fruit bromelain, stem bromelain and actinidain, but this was far less extensive than on those incubated in papaya latex supernatant. We conclude that, on the basis of presently available data, CPs derived from pineapples and kiwi fruits are not suitable for development as novel anthelmintics for intestinal nematode infections.

scholarly journals Anthelmintic action of plant cysteine proteinases against the rodent stomach nematode,Protospirura muricola,in vitroandin vivo

Parasitology ◽  
2006 ◽  
Vol 134 (1) ◽  
pp. 103-112 ◽  
Author(s):  
G. STEPEK ◽  
A. E. LOWE ◽  
D. J. BUTTLE ◽  
I. R. DUCE ◽  
J. M. BEHNKE
Keyword(s):  
Detrimental Effect ◽  
Gastrointestinal Nematodes ◽  
Cysteine Proteinases ◽  
Trichuris Muris ◽  
Kiwi Fruit ◽  
Heligmosomoides Polygyrus ◽  
Anthelmintic Efficacy ◽  
Papaya Latex

Cysteine proteinases from the fruit and latex of plants, including papaya, pineapple and fig, were previously shown to have a rapid detrimental effect,in vitro, against the rodent gastrointestinal nematodes,Heligmosomoides polygyrus(which is found in the anterior small intestine) andTrichuris muris(which resides in the caecum). Proteinases in the crude latex of papaya also showed anthelmintic efficacy against both nematodesin vivo. In this paper, we describe thein vitroandin vivoeffects of these plant extracts against the rodent nematode,Protospirura muricola, which is found in the stomach. As in earlier work, all the plant cysteine proteinases examined, with the exception of actinidain from the juice of kiwi fruit, caused rapid loss of motility and digestion of the cuticle, leading to death of the nematodein vitro. In vivo, in contrast to the efficacy againstH. polygyrusandT. muris, papaya latex only showed efficacy againstP. muricolaadult female worms when the stomach acidity had been neutralized prior to administration of papaya latex. Therefore, collectively, our studies have demonstrated that, with the appropriate formulation, plant cysteine proteinases have efficacy against nematodes residing throughout the rodent gastrointestinal tract.

scholarly journals Corrigendum

Parasitology ◽  
2007 ◽  
Vol 134 (4) ◽  
pp. 607-607
Keyword(s):  
Active Site ◽  
Active Enzyme ◽  
Distilled Water ◽  
Cysteine Proteinases ◽  
Anthelmintic Efficacy ◽  
Order Of Magnitude ◽  
Papaya Latex ◽  
Published Paper

Stepek, G., Lowe A. E., Buttle D. J., Duce I. R. and Behnke J. M. (2007). Anthelmintic action of plant cysteine proteinases against the rodent stomach nematode, Protospirura muricola, in vitro and in vivo. Parasitology134, 103–112 (Published online 11 October 2006. doi:10.1017/S0031182006001302)The authors of the above article regret that several errors appear in their published paper:On Page 105: In the methods section entitled “In vivo assessment of anthelmintic efficacy of plant cysteine proteinases”, the sentence:‘Five grams of papaya latex were mixed with 8 ml of sterile distilled water (dH2O), filtered, and the amount of active enzyme present was measured, by active-site titration, to be 331 nmol’should read:‘Five grams of papaya latex were mixed with 8 ml of sterile distilled water (dH2O), filtered, and the amount of active enzyme present was measured, by active-site titration, to be 13·24 micromol’And the sentence:‘Each group of mice received a different treatment: 0·2 ml of papaya latex alone (containing 8 nmol active enzyme), …’should read:‘Each group of mice received a different treatment: 0·2 ml of papaya latex alone (containing 331 nmol active enzyme), …’On Page 110: In column 2, line 5, the sentence:‘The amount of active enzyme administered in each dose (8 nmol) is based …’should read:‘The amount of active enzyme administered in each dose (331 nmol) is based …’And on lines 10–15, the sentence:‘Assuming the volume of a mouse stomach to be 1 ml and the enzyme to be present throughout the stomach at equal dilution, the concentration of enzyme would be in the order of 8 microM, which is somewhat lower than the in vitro concentrations.’Should read:Assuming the volume of a mouse stomach to be 1 ml and the enzyme to be present throughout the stomach at equal dilution, the concentration of enzyme would be in the order of 330 microM, which is about an order of magnitude higher than effective in vitro concentrations. A possible reason for the …’

The anthelmintic efficacy of papaya latex in a rodent–nematode model is not dependent on fasting before treatment

2011 ◽  
Vol 86 (3) ◽  
pp. 311-316 ◽  
Author(s):  
W. Luoga ◽  
F. Mansur ◽  
D.J. Buttle ◽  
I.R. Duce ◽  
M.C. Garnett ◽  
...  
Keyword(s):  
Beneficial Effect ◽  
Food Deprivation ◽  
Anthelmintic Activity ◽  
Systematic Evaluation ◽  
Cysteine Proteinases ◽  
Anthelmintic Efficacy ◽  
C3h Mice ◽  
Supernatant Extract ◽  
Heligmosomoides Bakeri ◽  
Papaya Latex

AbstractIn earlier studies of the anthelmintic activity of plant cysteine proteinases (CPs), a period of food deprivation was routinely employed before administration of CPs, but there has been no systematic evaluation as to whether this does actually benefit the anthelmintic efficacy. Therefore, we assessed the effect of fasting on the efficacy of CPs from papaya latex (PL) against Heligmosomoides bakeri in C3H mice. We used a refined, supernatant extract of papaya latex (PLS) with known active enzyme content. The animals were divided into three groups (fasted prior to treatment with PLS, not fasted but treated with PLS and fasted but given only water). The study demonstrated clearly that although food deprivation had been routinely employed in much of the earlier work on CPs in mice infected with nematodes, fasting has no beneficial effect on the efficacy of PLS against H. bakeri infections. Administration of CPs to fed animals will also reduce the stress associated with fasting.

The anthelmintic efficacy of natural plant cysteine proteinases against Hymenolepis microstoma in vivo

2014 ◽  
Vol 89 (5) ◽  
pp. 601-611 ◽  
Author(s):  
F. Mansur ◽  
W. Luoga ◽  
D.J. Buttle ◽  
I.R. Duce ◽  
A. Lowe ◽  
...  
Keyword(s):  
Anthelmintic Activity ◽  
Cysteine Proteinases ◽  
Anthelmintic Efficacy ◽  
Novel Drugs ◽  
Papaya Latex ◽  
Host Parasite ◽  
Convenient Model ◽  
Hymenolepis Microstoma

AbstractLittle is known about the efficacy of cysteine proteinases (CP) as anthelmintics for cestode infections in vivo. Hymenolepis microstoma is a natural parasite of house mice, and provides a convenient model system for the assessment of novel drugs for anthelmintic activity against cestodes. The experiments described in this paper indicate that treatment of H. microstoma infections in mice with the supernatant of papaya latex (PLS), containing active cysteine proteinases, is only minimally efficacious. The statistically significant effects seen on worm burden and biomass showed little evidence of dose dependency, were temporary and the role of cysteine proteinases as the active principles in PLS was not confirmed by specific inhibition with E-64. Worm fecundity was not affected by treatment at the doses used. We conclude also that this in vivo host–parasite system is not sensitive enough to be used reliably for the detection of cestocidal activity of compounds being screened as potential, novel anthelmintics.

scholarly journals Bromelain, a Group of Pineapple Proteolytic Complex Enzymes (Ananas comosus) and Their Possible Therapeutic and Clinical Effects. A Summary

Foods ◽  
2021 ◽  
Vol 10 (10) ◽  
pp. 2249
Author(s):  
Carolina Varilla ◽  
Massimo Marcone ◽  
Lisete Paiva ◽  
Jose Baptista
Keyword(s):  
Malignant Cell ◽  
The Body ◽  
Ananas Comosus ◽  
Therapeutic Effects ◽  
Clinical Effects ◽  
Pineapple Fruit ◽  
Stem Bromelain ◽  
Anti Inflammatory

Bromelain is a complex combination of multiple endopeptidases of thiol and other compounds derived from the pineapple fruit, stem and/or root. Fruit bromelain and stem bromelain are produced completely distinctly and comprise unique compounds of enzymes, and the descriptor “Bromelain” originally referred in actuality to stem bromelain. Due to the efficacy of oral administration in the body, as a safe phytotherapeutic medication, bromelain was commonly suited for patients due to lack of compromise in its peptidase efficacy and the absence of undesired side effects. Various in vivo and in vitro studies have shown that they are anti-edematous, anti-inflammatory, anti-cancerous, anti-thrombotic, fibrinolytic, and facilitate the death of apoptotic cells. The pharmacological properties of bromelain are, in part, related to its arachidonate cascade modulation, inhibition of platelet aggregation, such as interference with malignant cell growth; anti-inflammatory action; fibrinolytic activity; skin debridement properties, and reduction of the severe effects of SARS-Cov-2. In this paper, we concentrated primarily on the potential of bromelain’s important characteristics and meditative and therapeutic effects, along with the possible mechanism of action.

The anthelmintic efficacy of natural plant cysteine proteinases against the equine tapeworm, Anoplocephala perfoliatain vitro

2015 ◽  
Vol 90 (5) ◽  
pp. 561-568 ◽  
Author(s):  
F. Mansur ◽  
W. Luoga ◽  
D.J. Buttle ◽  
I.R. Duce ◽  
A.E. Lowe ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Hymenolepis Diminuta ◽  
Cysteine Proteinases ◽  
Active Ingredients ◽  
Natural Plant ◽  
Nematode Parasites ◽  
Anthelmintic Efficacy ◽  
Anoplocephala Perfoliata ◽  
Papaya Latex

AbstractPapaya latex has been demonstrated to be an efficacious anthelmintic against murine, porcine, ovine and canine nematode parasites, and even those infecting poultry, and it has some efficacy against rodent cestodes. The active ingredients of papaya latex are known to be cysteine proteinases (CPs). The experiments described in this paper indicate that CPs in papaya latex, and also those in pineapples, are highly efficacious against the equine cestode Anoplocephala perfoliatain vitro, by causing a significant reduction in motility leading to death of the worms. The susceptibility of A. perfoliata to damage by CPs was considerably greater than that of the rodent cestodes Hymenolepis diminuta and H. microstoma. Our results are the first to report anthelmintic efficacy of CPs against an economically important equine helminth. Moreover, they provide further evidence that the spectrum of activity of CPs is not restricted to nematodes and support the idea that these plant-derived enzymes can be developed into useful broad-spectrum anthelmintics.

Host genetic influences on the anthelmintic efficacy of papaya-derived cysteine proteinases in mice

Parasitology ◽  
2015 ◽  
Vol 142 (7) ◽  
pp. 989-998 ◽  
Author(s):  
WENCESLAUS LUOGA ◽  
FADLUL MANSUR ◽  
GILLIAN STEPEK ◽  
ANN LOWE ◽  
IAN R. DUCE ◽  
...  
Keyword(s):  
Standard Dose ◽  
Inbred Mouse ◽  
Mouse Strains ◽  
Intestinal Nematode ◽  
Anthelmintic Efficacy ◽  
Cimetidine Treatment ◽  
Heligmosomoides Bakeri ◽  
Host Genetic ◽  
Papaya Latex ◽  
Responder Mouse

SUMMARYEight strains of mice, of contrasting genotypes, infected with Heligmosomoides bakeri were studied to determine whether the anthelmintic efficacy of papaya latex varied between inbred mouse strains and therefore whether there is an underlying genetic influence on the effectiveness of removing the intestinal nematode. Infected mice were treated with 330 nmol of crude papaya latex or with 240 nmol of papaya latex supernatant (PLS). Wide variation of response between different mouse strains was detected. Treatment was most effective in C3H (90·5–99·3% reduction in worm counts) and least effective in CD1 and BALB/c strains (36·0 and 40·5%, respectively). Cimetidine treatment did not improve anthelmintic efficacy of PLS in a poor drug responder mouse strain. Trypsin activity, pH and PLS activity did not differ significantly along the length of the gastro-intestinal (GI) tract between poor (BALB/c) and high (C3H) drug responder mouse strains. Our data indicate that there is a genetic component explaining between-mouse variation in the efficacy of a standard dose of PLS in removing worms, and therefore warrant some caution in developing this therapy for wider scale use in the livestock industry, and even in human medicine.

scholarly journals Nematicidal effects of cysteine proteinases against sedentary plant parasitic nematodes

Parasitology ◽  
2007 ◽  
Vol 134 (12) ◽  
pp. 1831-1838 ◽  
Author(s):  
G. STEPEK ◽  
R. H. C. CURTIS ◽  
B. R. KERRY ◽  
P. R. SHEWRY ◽  
S. J. CLARK ◽  
...  
Keyword(s):  
Plant Extracts ◽  
Specific Inhibitor ◽  
Parasitic Nematodes ◽  
Cysteine Proteinases ◽  
Plant Parasitic Nematodes ◽  
Second Stage ◽  
Anthelmintic Efficacy ◽  
Plant Parasitic

SUMMARYCysteine proteinases from the fruit and latex of plants, such as papaya, pineapple and fig, have previously been shown to have substantial anthelmintic efficacy, in vitro and in vivo, against a range of animal parasitic nematodes. In this paper, we describe the in vitro effects of these plant extracts against 2 sedentary plant parasitic nematodes of the genera Meloidogyne and Globodera. All the plant extracts examined caused digestion of the cuticle and decreased the activity of the tested nematodes. The specific inhibitor of cysteine proteinases, E-64, blocked this activity completely, indicating that it was essentially mediated by cysteine proteinases. In vitro, plant cysteine proteinases are active against second-stage juveniles of M. incognita and M. javanica, and some cysteine proteinases also affect the second-stage juveniles of Globodera rostochiensis. It is not known yet whether these plant extracts will interfere with, or prevent invasion of, host plants.

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