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Ethnopharmacological relevance

Cordyceps species which is well-known as ‘winter worm summer grass’ has long been used as tonics and stimulants to enhance energy, exhibiting a potential for energy metabolism. Clinical trials have suggested their beneficial effect on lipid metabolic disorders such as hyperlipidemia.

Materials and methods

The effect of Cordyceps militaris on metabolic parameters was investigated using C58BL/6J mice induced by high-fat diet (HFD). The effect was first determined by assessing the body and organ weight. For further investigation, sections of epididymal adipose tissue were stained with hematoxylin and eosin and the size of epididymal adipocyte was measured by Image analysis system. Fat accumulation in frozen liver sections was assessed by the Oil Red O staining and the plasma biochemical parameters were also assessed. Active constituents were characterized using chromatographic and spectroscopic analysis.

Results

The administration of Cordyceps militaris extract (CE) at the dose of 100 mg/kg and 300 mg/kg reduced body weight gain and food efficiency ratio induced by HFD. The amount of epididymal fat and size of adipocytes were also decreased by CE treatment. In addition, liver weight and fat deposition in liver were dramatically reduced in CE-treated group. The treatment of CE also showed beneficial effects on plasma parameters related to lipid profiles. Further study for the characterization of active constituents of Cordyceps resulted in the isolation of two new compounds such as cordyrroles A (1) and B (7) together with 12 known compounds including pyrrole alkaloids and nucleotide derivatives. Among the isolated compounds, cordyrrole A significantly inhibited adipocyte differentiation and pancreatic lipase activity, whereas cordyrrole B was more effective at inhibiting pancreatic lipase. Cordycepin, a characteristic compound of Cordyceps militaris, decreased the rate of adipocyte differentiation.

Conclusion

Treatment of CE inhibited HFD-induced metabolic disorders, mainly by improvement in metabolic parameters. As active constituents, pyrrole alkaloids and nucleotide derivatives were characterized. These results suggested that Cordyceps militaris might be beneficial for the treatment of metabolic disorders obesity through the combined actions of diverse constituents.  相似文献   

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Aim of the study

The purpose of this study is to isolate the pure compounds from the extracts of Cordyceps militaris obtained through solid-state cultivation process, and evaluate their anti-inflammatory and anticancer properties.

Materials and methods

Silica gel column chromatographic purification of Cordyceps militaris extracts resulted in the isolation of 10 pure compounds (1-10). The compounds 1-10 were examined for their growth inhibitory properties against nitric oxide (NO), tumor necrosis factor (TNF)-α and interleukin (IL)-12 enhanced production from LPS/IFN-γ-stimulated macrophages. Additionally, the anti-proliferation effects of 1-10 on human cancer cell lines, colon (colon 205), prostate (PC-3), and hepatoma (HepG2) cells were also analyzed.

Results

Compound 8 displayed potent growth inhibition on NO, TNF-α and IL-12 production with an IC50 value of 7.5, 6.3, and 7.6 μg/ml, respectively. A similar inhibitory trend on these inflammatory mediators was observed for 3, 7, 9 and 10 with an IC50 values ranging from 10.8 to 17.2 μg/ml. On the other hand, compounds 3 and 8 were potent anti-proliferative agents with an IC50 value of 35.6 and 32.6 μg/ml toward PC-3 and colon 205 cell lines, respectively. The compounds 1 and 2 showed potent anti-proliferation in PC-3 and colon 205 cells, while only 3 displayed such effect in HepG2 cells.

Conclusion

The present study provides scientific supporting information for the ethnopharmacological use of Cordyceps militaris as an anti-inflammatory and anticancer agent.  相似文献   

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Ethnopharmacological relevance

Cordyceps militaris has been used as a traditional herbal medicine for treating allergy in East Asia.

Aim of the study

We investigated the anti-allergic efficacy of Cordyceps militaris and its mechanism of action.

Materials and methods

β-Hexosaminidase release of mast cells, a key parameter of degranulation, was evaluated. Anti-allergic potential of Cordyceps militaris was studied using passive cutaneous anaphylaxis (PCA) in vivo. The anti-allergic mechanism of Cordyceps militaris was investigated by immunoblotting analysis, RT-PCR and other biological approaches in mast cells.

Results

GSCM EtOAc extract (GSCME) inhibited antigen-induced degranulation with a IC50 value (28.5 μg/ml) in RBL-2H3 cells and antigen-induced passive cutaneous anaphylaxis (PCA) response with a ED50 value (665 mg/kg) in vivo. The release of interleukin (IL-4) and tumor necrosis factor (TNF-α were decreased by GSCME in RBL-2H3 cells. In order to elucidate the anti-allergic mechanisms of GSCME in mast cells, we examined the activated levels of signaling molecules. GSCME inhibited the phosphorylation Syk, ERK, p38 and JNK expression. Identified genistein, daidzein, genistein 7-O-β-d-glucoside 4″-O-methylate, genistein 4′-O-β-d-glucoside 4″-O-methylate, glycitein 7-O-β-d-glucoside 4″-O-methylate, daidzein 7-O-β-d-glucoside 4″-O-methylate and adenosine in GSCME, inhibited antigen-induced degranulation in RBL-2H3 cells.

Conclusions

Our study suggests that GSCME might be used as a therapeutic agent for allergic diseases.  相似文献   

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Ethnopharmacological relevance

For thousands of years antlers have been used in Asian countries to promote rapid healing, treat weight loss, slow growth in children, strengthen weak bones, and alleviate cold hands and feet.

Aim of the study

The present study was performed to examine the effect of fermentation on the ability of antler to act as a stimulator of bone growth.

Materials and methods

This study used pre-osteoblast MC3T3-E1 cells to examine factors related to bone growth, such as cell proliferation, production of alkaline phosphatase (ALP), and deposition of extracellular matrix proteins (e.g., collagens, osteonectin, bone sialoprotein (BSP)), via the treatment of non-fermented and fermented antler.

Results

Antler fermentation using Cordyceps militaris was carried out at 25 °C for seven days. The total content of sugar, sialic acid, and protein increased with fermentation time. Cell proliferation was greater in the fermented antler- (FA-) treated groups than in the NFA- (non-fermented antler-) treated groups, in which proliferation increased significantly up to 137% of the basal value. Significant increases in mRNA expression and ALP activity were found at FA concentrations of 50-100 μg/ml; at 100 μg/ml the activity had increased 119% compared to the control activity. For NFA and FA the expression levels of type I collagen mRNA significantly increased in a dose-dependent manner at all treatment doses. However, significant differences between the antler groups were not observed. Mineralization significantly increased by NFA and FA treatment to 183% and 241%, respectively, when compared to colostrum, as a positive control (165%).

Conclusions

Antler treatment increased the proliferation of osteoblasts and bone matrix proteins, such as type I collagen and BSP. Antler fermented with Cordyceps militaris showed enhanced activity, and its stimulatory effects on cell proliferation and ALP production were greater than those of NFA. We surmise that these increases in activity were related to increased sialic acid content. Therefore, the results of this study suggest that the physiological effects of antler, including bone growth, may be increased through the fermentation process.  相似文献   

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Ethnopharmacological relevance

Cordyceps sorbolifera has been used in Traditional Chinese Medicine for improving the renal function. Cyclosporine A (CsA) is an important immunosuppressive agent in the prevention of renal allograft rejection, but long-term usage of CsA could lead to chronic nephrotoxicity and renal graft failure. The study was aimed to investigate whether the mycelia glycoproteins of Cordyceps sobolifera (CSP) exert prevention effects on CsA-induced nephrotoxicity.

Materials and methods

Sprague-Dawley (SD) rats were randomly assigned into four groups (n=6 per group): normal saline (control group), CSP group, CsA group, and CSP-CsA group (CsA combined treatment with CSP). Glomerular and tubular functions were assessed and histological studies were performed.

Results

CSP, prepared by hot water extraction, ethanol precipitation and membrane dialysis, was found to be composed of three glycoproteins with average molecular weights of 543, 31, and 6.3 kDa, respectively. CsA impaired urea clearance and creatinine clearance were significantly improved by concomitant administration of CSP. TUNEL histochemical stain revealed that CSP significantly decreased CsA-induced apoptosis in renal tubular cells. The reducing effect of caspase-3 activation by CSP was suggested through the over-expression of the anti-apoptosis protein Bcl-2 in renal tubule cells. In assessment of CSP protection of renal tubule function, we found that CSP restored CsA induced magnesium wasting by increasing the magnesium reabsorption channels TRMP6 and TRMP7.

Conclusion

The results suggested that CSP had a significant suppressive activity on CsA-induced apoptosis and protective activity against nephron loss possibly via its restoring activity by increasing the magnesium reabsorption channels TRMP6 and TRMP7 on CsA induced magnesium wasting.  相似文献   

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樊慧婷  林洪生 《中国中药杂志》2013,38(15):2549-2552
蛹虫草是一种能寄生在多种鳞翅目昆虫蛹及幼虫上的虫草菌,在免疫调节、抗肿瘤、抗病毒和抗感染等方面有很强的活性,值得深入研究和开发.该文分别从蛹虫草的有效成分及药理作用综述最新研究进展.  相似文献   

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Ethnopharmacological relevance

Cordyceps sinensis has been used as a precious herbal medicine for thousands of years in China. Its polysaccharide fraction has been confirmed possessing immunomodulatory function and we have reported the acid polysaccharide fraction (APSF), from an anamorph of C. sinensis, has stimulating activity on macrophages. The mechanism still needs to be further elucidated.

Materials and methods

In order to investigate the effects of APSF on macrophage's phenotypes, Ana-1 mouse macrophages were polarized to M2 phenotype by culturing the cells with culture supernatant of H22 cells. M2 phenotype was determined by measuring the expression of TNF-α and checking cell surface markers mannose receptor (MR) and scavenger receptor (SR). After cultured with H22 supernatant for 72 h, the TNF-α level of Ana-1 cells was decreased while the SR and MR expressions were up-regulated, suggesting that Ana-1 cells were polarized towards M2 macrophages. Then the effects of APSF on M2 macrophages were investigated by measuring mRNA levels of TNF-α, inducible nitric oxide synthase (iNOS), IL-12 and IL-10. Nuclear NF-κB was detected by Western blotting.

Results

APSF treatment increased the expressions of TNF-α, IL-12 and iNOS, and reduced the expression of IL-10 of Ana-1 cells. Besides, the expressions of SR and MR were down-regulated by APSF. And the result of Western blotting showed NF-κB level was decreased in M2 macrophages and up-regulated after APSF treatment.

Conclusions

APSF may convert M2 macrophages to M1 phenotype by activating NF-κB pathway.  相似文献   

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Ethnopharmacological relevance

Enicostema axillare (Lam.) A. Raynal., (Gentianaceae) has been used in traditional Indian system of medicine as depurative and for the treatment of psoriasis, intermittent fever and cancer. Ethnobotanical survey conducted in Theni District indicated a high consensus for this plant as blood purifier and to treat dermatopathy and venereal infections. The present study evaluated the immunomodulatory activity of the methanol extract of Enicostema axillare.

Materials and methods

In vivo immunomodulatory activity of Enicostema axillare methanol extract (100 and 200 mg/kg b.w) was evaluated by assessing its effect on the total and differential leukocyte count, organ weight, hemaggultinating antibody titer, plaque forming cells, quantitative hemolysis of SRBC and delayed type hypersensitivity. Sheep red blood cells (SRBC, 5 × 108 cells/0.1 mL) were used to immunize the animals. In vitro immunomodulatory potential of the extract was studied using peritoneal macrophages by evaluating its effects on NBT reduction, NO production and cytokine release.

Results

The animals treated with Enicostema axillare methanol extract showed a significant (P ≤ 0.05) increase in weight of the thymus and spleen. The total leukocyte and lymphocyte count was increased significantly (P < 0.005) by the treatment. There was no significant alteration in neutrophil count. A dose dependent increase in antibody titer value was observed. A decreased response to DTH reaction induced by SRBC was recorded. A potential phagocytic response was seen on treatment with the extracts at 10 and 25 μg/mL. The extract inhibited the release of pro-inflammatory cytokines and production of NO significantly in a dose dependent manner.

Conclusion

These findings suggested that the methanol extract of Enicostema axillare acted on both humoral and cell mediated immune functions and decreased the release of pro-inflammatory cytokines in the peritoneal macrophages.  相似文献   

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Ethnopharmacological relevance

Ethnopharmacological survey indicated leaves of Byrsonima fagifolia Nied. (Malpighiaceae) against gastrointestinal disorders.

Aim of the study

The methanolic extract from the leaves of Byrsonima fagifolia (denominated BF) was evaluated for toxic, mutagenic, gastroprotective, antidiarrheal, antibacterial and immunomodulatory activities.

Materials and methods

The preventive and healing action of BF against gastric ulcer was evaluated in experimental models in rodents. We evaluated immunomodulatory (by murine peritoneal macrophages), antidiarrheal (by induced diarrhea with castor oil and intestinal motility) and antibacterial action of BF against standard strain of Escherichia coli, Staphylococcus aureus and Helicobacter pylori. The safety of use of BF was also evaluated by mutagenic (Ames assay) and by analyses of toxicity parameters.

Results

Phytochemical BF profile indicated the presence of phenolic compounds with antioxidant and radical-scavenging properties. BF significantly inhibited gastric lesions induced by ethanol and HCl/ethanol and endogenous mucosal sulphydryl groups (SHs) participated efficaciously in BF gastroprotection. BF blocked development of inflammation process and also has antidiarrheal actions. This extract accelerated the healing of the gastric ulcerated mucosa by stimulating proliferative factors and by increasing production of gastric mucus with no toxic action. The substances responsible for the protective action are concentrated in the ethyl acetate fraction that demonstrated no mutagenic action in vitro.

Conclusions

Byrsonima fagifolia presents gastroprotective, healing and antidiarrheal activities supporting previous claims that its traditional use by Brazilians can treat these gastrointestinal ailments.  相似文献   

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Ethnopharmacological relevance

An investigation of topical anti-inflammatory activity was undertaken on plants used in Central America traditional medicine.

Aim of study

Four herbal drugs used in the folk medicine of Central America to treat inflammatory skin affections (Acacia cornigera bark, Byrsonima crassifolia bark, Sphagneticola trilobata leaves and Sweetia panamensis bark) were evaluated for their topical anti-inflammatory activity.

Materials and methods

Petroleum ether, chloroform and methanol extracts were obtained for herbal medicines and then extracts were tested on Croton oil-induced ear dermatitis model in mice.

Results

Almost all the extracts reduced the Croton oil-induced ear dermatitis in mice and the chloroform ones showed the highest activity, with ID50 (dose giving 50% oedema inhibition) values ranging from 112 μg/cm2 (Byrsonima crassifolia) to 183 μg/cm2 (Sphagneticola trilobata). As reference, ID50 of the non-steroidal anti-inflammatory drug indomethacin was 93 μg/cm2.

Conclusions

Lipophilic extracts from these species can be regarded as potential sources of anti-inflammatory principles.  相似文献   

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Aim of the study

In a search for new plant-derived biologically active compounds against malaria parasites, we have carried out an ethnopharmacological study to evaluate the susceptibility of cultured Plasmodium falciparum to extracts and fractions from seven Cameroonian medicinal plants used in malaria treatment. We have also explored the inhibition of the Plasmodium falciparum cysteine protease Falcipain-2.

Materials and methods

Plant materials were extracted by maceration in organic solvents, and subsequently partitioned or fractionated to afford test fractions. The susceptibility of erythrocytes and the W2 strain of Plasmodium falciparum to plant extracts was evaluated in culture. In addition, the ability of annonaceous extracts to inhibit recombinant cysteine protease Falcipain-2 was also assessed.

Results and discussion

The extracts showed no toxicity against erythrocytes. The majority of plant extracts were highly active against Plasmodium falciparumin vitro, with IC50 values lower than 5 μg/ml. Annonaceous extracts (acetogenin-rich fractions and interface precipitates) exhibited the highest potency. Some of these extracts exhibited modest inhibition of Falcipain-2.

Conclusion

These results support continued investigation of components of traditional medicines as potential new antimalarial agents.  相似文献   

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Ethnopharmacological relevance

Tripterygium wilfordii Hook. f. (Celastraceae) has been traditionally used as folk medicine for centuries in China for the treatment of immune-inflammatory diseases.

Aim of the study

This study aimed to assess the antiangiogenic activities which support the therapeutic use of Tripterygium wilfordii and its terpenoids for angiogenesis disease such as cancer.

Materials and methods

The ethanol extract of Tripterygium wilfordii and subsequent fractions were evaluated on an in vivo antiangiogenic zebrafish embryo model.

Results

Three antiangiogenic terpenoids were isolated by bioassay-guided purification, namely, celastrol (4), cangoronine (5) and triptolide (7). Among them, triptolide manifested the most potent antiangiogenic activity against vessel formation by nearly 50% at 1.2 μM. Semi-quantitative RT-PCR analysis revealed that triptolide dose- and time-dependently reduced the mRNA expression of angiopoietin (angpt)2 and tie2 in zebrafish, indicating the involvement of angpt2/tie2 signaling pathway in the antiangiogenic action of triptolide.

Conclusions

The discovery of an alternative pathway further confirms the value of ethnopharmacological investigations into traditional botanicals for leads for potential drug development.  相似文献   

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Ethnopharmacological relevance

Premna odorata Blanco (Lamiaceae) is a medicinal plant traditionally used in Albay Province, in southeastern Luzon, Philippines to treat tuberculosis. This study aimed to determine the antitubercular property of the crude extract and sub-extracts of the leaves, and to isolate the bioactive principles from the active fractions.

Materials and methods

Through extraction, solvent polarity-based fractionation and silica gel chromatography purification of the DCM sub-extract, compound mixtures from the bioactive fractions were isolated and screened for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv using the colorimetric Microplate Alamar Blue assay (MABA).

Results

The crude methanolic extract and sub-extracts showed poor inhibitory activity against Mycobacterium tuberculosis H37Rv (MIC≥128 µg/mL). However, increased inhibitory potency was observed for fractions eluted from the DCM sub-extract (MIC=54 to 120 µg/mL). Further purification of the most active fraction (MIC=54 µg/mL) led to the isolation of a 1-heneicosyl formate (1), 4:1 mixture of β-sitosterol (2), stigmasterol (3) and diosmetin (4), which were identified through GC–MS analysis (with dereplication) and NMR experiments. The MIC of compound 1 was 8 µg/mL.

Conclusions

The results of this study provide scientific basis for the traditional use of Premna odorata as treatment for tuberculosis.  相似文献   

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Ethnopharmacological relevance: Heteropterys tomentosa

A. Juss (Malpighiaceae), commonly mistaken as Heteropterys aphrodisiaca, is chronically used by the Brazilian population to improve general health due to its claimed protective effects against a wide range of medical conditions.

Aim of the study

This study in rodents aimed to verify the adaptogenic potential of the hydroalcoholic extracts of the roots (the most commonly used portion), branches and leaves of the plant.

Materials and methods

The phytochemical constitution of the extracts was analyzed through thin-layer chromatography and high-performance liquid chromatography. Restriction- and cold-induced stress in rats treated for 14 days with 100 or 300 mg/kg of the extracts were used to evaluate parameters such as ulceration, adrenals, thymus and spleen weights, as well as ACTH and corticosterone plasmatic levels. The stress response also was evaluated in mice by self-analgesia induced by restraint stress, after 7 days of treatment at doses of 100 and 300 mg/kg. The learning and memory of aged rats treated with extracts of root or branches at the dose of 50 mg/kg for 80 days were evaluated in the elevated T-maze test.

Results

The chemical constituents of the three parts of the plant were relatively similar in the presence of saponins, hydrolysable tannins, flavonoids, polyphenols and triterpenes. None of the three extracts were capable of protecting the stomach from ulcerations in rats submitted to cold restraint stress or protecting from alterations in adrenal or spleen weight (p>0.05). Furthermore, the extracts did not inhibit increases in plasma levels of corticosterone and adrenocorticotropic hormone. Moreover, the extracts did not inhibit self-analgesia induced by restraint stress in mice and did not improve the performance of aged rats in the T-maze test (p>0.05).

Conclusion

The tests employed in this study did not show evidence of adaptogenic activity in the three extracts of Heteropterys tomentosa.  相似文献   

18.

Ethnopharmacological relevance

Nelumbo nucifera Gaertn. (Nymphaeaceae) is a well-known aquatic plant which has been used for the treatment of several disorders including skin disease, cough, inflammation, fever and many other disorders.

Aim of the study

To explore the immunomodulatory activity of extract of rhizome (NNRE) and seed (NNSE) of the plant.

Materials and methods

The immunomodulatory activity of NNRE and NNSE was evaluated using various in vivo models including the total and differential leukocyte count (TLC and DLC), nitroblue-tetrazolium reduction (NBT) test, neutrophil adhesion test, phagocytic response and delayed type hypersensitivity (DTH) reaction. Sheep red blood cells (SRBC, 5 × 109 cells/ml) were used to immunize the animals. NNRE and NNSE at the doses of 100 and 300 mg/kg were administrated.

Result

The TLC and lymphocyte count increased significantly but the neutrophil count was decreased for NNRE and NNSE treated groups compared to the control. A dose-dependent potentiation of DTH reaction induced by SRBC was observed from the extracts. The percentage of neutrophil adhesion to the nylon fiber was increased in NNRE treated groups (63.22 and 62.91%) compared to the NNSE treated group (54.86 and 54.23%). A potential phagocytic response was seen on treatment of the extracts, and significant changes were observed in the formation of formazone crystals.

Conclusion

This finding suggests that the extract of rhizome and seed Nelumbo nucifera stimulate defense system by modulating several immunological parameters.  相似文献   

19.

Aim of the study

This study investigated effect of a crude extract of Dodonaea viscosa on the proteinase and phospholipase production and adherence to epithelial cells by Candida albicans isolated from HIV positive and HIV negative patients.

Materials and methods

Twenty Candida albicans strains isolated from HIV positive and 20 from HIV negative patients were investigated. The isolates were exposed to subinhibitory concentration of crude plant extract and adherence, proteinase and phospholipase production were assessed. The results were analysed using Student's t-test and a two-way ANOVA.

Results

Dodonaea viscosa var. angustifolia inhibited the adherence of Candida albicans to oral epithelial cells (p = <0.01) but no significant effect of the plant extract on proteinase and phospholipase production was observed. Results from Candida albicans strains isolated from HIV positive and HIV negative patients were similar.

Conclusions

Dodonaea viscosa var. angustifolia inhibited the adherence of Candida albicans to oral epithelial cells, which is the initial step of colonization in the infection process. This plant has a therapeutic potential at subinhibitory concentration.  相似文献   

20.

Ethnopharmacological relevance

Mucuna pruriens is a tropical legume anecdotally reputed to have anthelmintic properties. This study was conducted to examine the validity of such claims.

Aim of the study

The aim of this study was to determine if ingestion of Mucuna seeds reduces helminth parasite infestation in lambs.

Materials and methods

Thirty-six Dorper × Katahdin ram lambs were assigned to three treatments, a cottonseed meal based control diet, a diet in which Mucuna replaced cottonseed meal and the control diet with levamisole (7.5 mg/kg body weight) administration. All diets were isonitrogenous and isocaloric. The 12 lambs in each treatment were assigned randomly to 4 pens, each containing 3 lambs. Lambs were trickle infected three times per week by gavage with infectious Haemonchus contortus larvae (2000 larvae/lamb) for 3 weeks.

Results

Levamisole treatment decreased fecal egg counts by 87% and abomasal worm counts by 83%. Mucuna intake did not statistically affect fecal egg counts or abomasal worm counts, though numerical (P > 0.10) reductions of 7.4% and 18.1%, respectively were evident. Anemia indicators, feed intake, and lamb growth were unaffected by treatment.

Conclusions

Levamisole reduced the Haemonchus parasite burden in lambs significantly but feeding Mucuna reduced the burden by levels unlikely to eliminate the clinical effects of parasitism.  相似文献   

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