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

BackgroundParasitic infection is one of the main problems in equidae, particularly donkeys.AimThis 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.MethodsThe 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.ResultsIn 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.ConclusionThe 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.

2021-01-01·Heliyon

In vitro anthelmintic activity of Chenopodium album and in-silico prediction of mechanistic role on Eisenia foetida

Article

作者: Choudhary, Neeraj ; Singh, Gurpal ; Khatik, Gopal L ; Suttee, Ashish ; Choudhary, Sunanda

Helminths born diseases are related to pitiable management practices and improper control strategies. The medicinal plants contain various phytoconstituents that are liable for their anthelmintic activity. The aerial parts of the Chenopodium album were successively extracted with microwaves assisted extraction using petroleum ether, ethyl acetate, methanol, hydroalcoholic and aqueous solvents to get respective extracts (CAPE, CAEE, CAME, CAHE, and CAAE). All the extracts were analyzed for preliminary phytochemical screening for the identification of phytoconstituents. The anthelmintic activity was analyzed on Indian adult earthworms Eisenia foetida using piperazine citrate (PCT) as a standard drug. All the extracts (apart from CAAE) lead to paralysis and fatality of the earthworms. CAEE extract exhibits highly significant anthelmintic activity at a 10 mg/ml concentration by causing paralysis and fatality of earthworms and was more potent than PCT suspension. At a concentration of 10 mg/ml, paralysis and death time for CAEE was recorded as (10.08 ± 1.11) and (65.28 ± 2.09) respectively, while for standard piperazine citrate, it was recorded as (22.96 ± 1.12) and (65.09 ± 1.23). The CAEE exhibits two major compounds by LC-MS, i.e., NG and DG, that are mainly accountable for the Chenopodium album anthelmintic activity. The plant possesses GABA-mimetic action and thereby leads to flaccid, reversible paralysis of the body wall muscle.

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