Evaluation of in vivo anthelmintic efficacy of certain indigenous plants against experimentally- induced Ascaridia galli infection in local birds (Gallus domesticus)

Article

作者: Sarma, Jadav ; Debnath, Sumitra ; Hazarika, Archana ; Deka, Dilip

The present study was an attempt to evaluate the anthelmintic efficacy of certain indigenous plants against experimentally induced Ascaridia galli infection in local birds (Gallus domesticus). Two indigenous plants viz., Nyctanthes arbor-tristis and Butea monosperma were used based on indigenous technical knowledge (ITK) and ethno-medical uses. Three types of extracts, viz. ethanolic, hydro-ethanolic and aqueous extracts of each of the two plants were prepared and three doses at the rate of 100, 500 and 1000 mg/kg were used for in vivo studies. Piperazine hydrate liquid was used as standard drug at 200 mg/kg body weight. All biochemical and haematological parameters showed a significant increase from 14th day post treatment in birds of all the groups treated with N. arbor-tristis extract at all the doses irrespective of the solvent used. However, the increase in biochemical and haematological parameters with B. monosperma was observed from 21st day of post treatment in all the groups at all the doses. Similarly, piperazine treated group also showed significant increase from 14th day of post treatment. There was significant reduction in egg output in the droppings of the birds treated with ethanolic, hydroethanolic and aqueous extracts of N. arbor-tristis and B. monosperma when compared with infected controls from 7th day onwards.

2021-12-01·Acta pharmaceutica (Zagreb, Croatia)

Piperazine sulfonamides as DPP-IV inhibitors: Synthesis, induced-fit docking and in vitro biological evaluation

Article

作者: Alwarafi, Ebtisam ; Khalaf, Reema Abu ; Sabbah, Dima

Abstract:

Diabetes mellitus is a chronic illness that needs persistent medical attention and continuous patient self-management to avoid acute complications. Dipeptidyl peptidase-IV (DPP-IV) inhibitors minimize glucagon and blood glucose levels by increasing the incretin levels, glucagon-like peptide (GLP-1) and glucose-dependent insulinotropic poly-peptide (GIP), leading to insulin secretion from pancreatic beta cells. In the present study, nine 1,4-bis(phenylsulfonyl) piperazine derivatives 1a-i were synthesized and identified using 1H NMR, 13C NMR, MS and IR spectroscopies. These compounds were tested in vitro and showed inhibitory activity ranging from 11.2 to 22.6 % at 100 µmol L–1 concentration. Piperazine sulfonamide derivatives were found to be promising DPP-IV inhibitors, where the presence of electron-withdrawing groups such as Cl (1a-c) improved the activity of the compounds more than electron-donating groups such as CH3 (1d-f) at the same position. Additionally, meta-substitution is disfavored (1b, 1e, 1g). Induced-fit docking studies suggested that the targeted compounds 1a-i occupy the binding domain of DPP-IV and form H-bonding with the backbones of R125, E205, E206, F357, K554, W629, Y631, Y662 and R669.

2021-01-01·Open veterinary journal

Oxidative stress in Strongylus spp. infected donkeys treated with piperazine citrate versus doramectin

Article

作者: Ghandour, Rehab A ; Hassan, Dalia ; Khalphallah, Arafat ; Bayomi, Sara A ; Hafez, Ahmed ; Elmeligy, Enas ; Abu-Seida, Ashraf M ; El-Khabaz, Khaled A S ; Elsayed, Hanan K ; Abdelbaset, Abdelbaset

Background:

Parasitic infection is one of the main problems in equidae, particularly donkeys.

Aim:

This study evaluated the oxidative stress in donkeys infected with Strongylus spp by determining the correlation between antioxidants levels; malondialdehyde (MDA), total antioxidant capacity (TAC), and the severity of parasitic infection. It also compared the therapeutic efficacy of piperazine citrate as an oral anthelmintic drug and Doramectin as an injectable one.

Methods:

The study was conducted on 40 donkeys naturally infected with Strongylus spp. These donkeys were divided into two groups (20 donkeys each) according to treatment; One group was treated with piperazine citrate (P_ipTG) and the other with doramectin (D_oraTG). Thorough clinical examination, hematological, biochemical, and parasitological assays were performed before (Day 0) and after treatment (Days 7, 14, 21, and 28). All data were statistically analyzed by independent-sample t-test or paired t-test.

Results:

In both groups, mean values of MDA were significantly reduced, while those of TAC were significantly elevated after treatment on days 7, 14, 21, and 28. These significant changes were reported after treatment between P_ipTG and D_oraTG in favor of D_oraTG. Serum concentrations of MDA were significantly reduced, while those of TAC were significantly elevated for D_oraTG treatment group when their values were compared with those of P_ipTG either on days 7, 14, 21, or 28. Significant correlations were reported in P_ipTG and D_oraTG. Negative significant correlations were reported between fecal egg count (FEC) and each of whole blood picture indices (RBCS, Hb, and PCV), serum TAC and faecal egg count reduction percentage FECR%. A positive correlation was seen between FEC and MDA. MDA exhibited a negative correlation with both blood picture and TAC; hence, TAC was positively correlated with these blood picture indices in both P_ipTG and D_oraTG. In P_ipTG, anthelmintic resistance (R) was present on days 7 and 14, while it was suspected (S) at day 21 then it was absent (N) at day 28. In D_oraTG, anthelmintic resistance was suspected (S) on day 7, then it became absent (N) on days 14, 21, and 28 post therapy.

Conclusion:

The immunological status of the infected donkeys had greatly improved after treatment. The therapeutic efficacy of injectable doramectin was more efficient than that of oral piperazine citrate in Strongylus spp. infected donkeys.

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外链

KEGG	Wiki	ATC	Drug Bank
D02127	枸橼酸哌嗪	P02CB01	-

研发状态

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适应症	国家/地区	公司	日期
蠕虫病	中国	四川峨嵋山药业有限公司	1981-01-01
蛔虫病	美国	GlaxoSmithKline, Inc.	1957-01-25
蛲虫病	美国	GlaxoSmithKline, Inc.	1957-01-25