Changes in tropomyosin derived antigenicity of banana prawn (Fenneropenaeus merguiensis) due to high pressure processing (HPP) at 600 MPa for 5 or 10 min at various temperatures (40, 80, 120 °C) were ...investigated. HPP of prawn samples at 40 and 80 °C for 5 min increased tropomyosin derived antigenicity by almost double, whereas HPP at 120 °C for 10 min decreased antigenicity by 65%, detected using ELISA kit. A significant (P ≤ 0.05) reduction of tropomyosin antigenicity after pepsin digestion was noticeable in prawns after HPP, but not in control prawn sample. However, further digestion of the control and HPP sample with pancreatin enzyme decreased antigenicity to ∼0 mg mL-1. The combination of HPP and high temperature (120 °C) in the current study can potentially reduce tropomyosin-derived antigenicity in whole prawn muscle, whereas SIF digestion with pancreatin enzyme may present a new prospective method to produce hypo-antigenic, enzymatically digested prawn products.
•HPP of prawn for 10 min at 120 °C decreases tropomyosin antigenicity by 65%.•HPP (600 MPa) of prawn at 40 and 80 °C increases antigenicity by almost double.•Pepsin enzyme digestion significantly reduces antigenicity in HPP prawn samples.•No significant effect of pepsin enzyme on untreated prawn antigenicity.•Further digestion with pancreatin reduces tropomyosin antigenicity to ∼0 mg mL-1.
Milk proteins are considered a reservoir of peptides possessing various bioactivities. Using ultrafiltration followed by reversed phase-high performance liquid chromatography, antioxidant peptides ...were purified from crude peptide extract of probiotic yoghurt supplemented with pineapple peel powder stored for 28 days at 4 °C. Two β-casein-derived peptides, 193YQEPVLGPVRGPFPIIV209 and 69SLPQNIPPLTQTPVVVPPF87 (designated P17 and P19, respectively), were identified and their antioxidant and anticancer activities assessed. P17 showed high scavenging activity against 2,2′-azino-bis(3-ethyl benzothiazoline-6-sulphonic acid) radicals, with an IC50 of 29.88 μg mL−1, compared with P19 (IC50 1.44 mg mL−1). Furthermore, the proliferation of HT-29 colon cancer cell line was inhibited (41.49% and 38.55%, respectively, by P17 and P19 at 3 mg mL−1) via inducing apoptosis and cell cycle arrest in G2/M-phase. In vitro gastrointestinal digestion of peptides resulted in increased bioactivities. These findings indicate a potential for utilising both of these peptides to manage oxidative stress mediated diseases and disorders including cancers.
The reported diketopiperazine calpain inhibitor,
cis-
l-
l-3,6-bis-(4-hydroxybenzyl)-1,4-dimethylpiperazine-2,5-dione
1, and its analogues
3 and
4 were synthesized from the corresponding amino acids. ...The previously assigned structure of
1 is confirmed but neither synthetic
1 nor its
N-methylphenylalanine analogues
3 and
4 inhibit porcine erythrocyte calpain I.
Synthesis of diketopiperazine calpain inhibitor
1 and its analogues
3 and
4 is described.
A series of 6-aralkyl substituted 2,4-diaminothieno2,3-
dpyrimidines in which the 6-aryl group is separated from the thieno2,3-
dpyrimidine ring by two to five methylene groups were synthesized and ...studied as inhibitors of dihydrofolate reductase from
Pneumocystis carinii,
Toxoplasma gondii,
Mycobacterium avium, and rat liver. Compounds in which the thieno2,3-
dpyrimidine ring is separated from the 6-aryl substituent by three methylene groups were the most potent inhibitors of the series (with IC
50 values ranging from 0.24 and 11.0 μM) but those with two methylene groups between the aromatic rings were the most selective agents.
The prevalence of allergic disorders may stem from reduced microbial exposure during childhood. Allergic disorders (rhinitis, asthma, atopic dermatitis) result from a systemic inflammatory reaction ...triggered by Th2-cell-mediated immune responses against ‘innocuous’ environmental antigens. Initial interpretations proposed an immune deviation of allergen-specific responses from a Th1 to a Th2 profile resulting from reduced production of interleukin-12 and interferons by natural immune cells stimulated by bacterial products. Both stereotypical and selective responses of innate host cells are invoked by different microorganisms. Early in an infection, pathogens can therefore imprint their ‘signatures’ on antigen-presenting cells and subsequent immune responses. This interaction between microorganisms and enterocytes is important for the controlled production of cytokines and chemokines. Some probiotic microorganisms can modulate the
in vitro expression of pro- and anti-inflammatory cytokines in a strain-dependent manner, probably skew the immune response towards Th1 phenotype and play an important role in allergy prevention.
A series of conformationally restricted congeners of pentamidine in which the flexible pentyl bridge of pentamidine was replaced by trans-1,2-bismethylenecyclopropyl, phenyl, pyridinyl, piperazinyl, ...homopiperazinyl, and piperidinyl groups were synthesized. The compounds were evaluated for trypanocidal activity in vitro and in vivo against one drug-sensitive and three drug-resistant trypanosome isolates. The DNA binding affinity of the compounds was also studied using calf thymus DNA and poly(dA-dT). The nature of the linker influenced the DNA binding affinity as well as the trypanocidal activity of the compounds. trans-1,2-Bis(4-amidinophenoxymethylene)cyclopropane (1) was over 25-fold more potent than pentamidine against the drug-resistant isolate KETRI 243As-10-3, albeit with comparable DNA binding affinity. N,N ‘-Bis(4-amidinophenyl)homopiperazine (8) was the most potent trypanocide in vitro against all four trypanosome isolates studied, but N,N ‘-bis(4-amidinophenyl)piperazine (6) was the most effective agent in vivo against both drug-sensitive and drug-resistant trypanosomes.
The present study determined the anti-inflammatory activity of
Wissadula amplissima var rostrata (Schum. & Thonn.), and calculated
the total phenolic content and total antioxidant capacity of the ...plant
in an attempt to justify the traditional uses of the plant in the
Ashanti region of Ghana for the management of spider,wasps and bee
stings. Powdered dried leaves of Wissadula amplissima were Soxhlet
extracted with Petroleum Ether (PWA, yield: 1.46% w/w); Chloroform
(CWA, yield: 1.18% w/w) and Methanol (MWA, yield: 3.39% w/w). These
fractions were tested for anti-inflammatory activity using
carrageenan-induced foot edema in 7 day old chicks. The effect before
the induction of inflammation (pre-emptive protocol) paradigm was used
for the assessment. Oral administration of PWA, CWA and MWA (30 -
300 mg/kg) dose dependently reduced edema with maximal effects of
68.25±2.03%, 77.83±0.81% and 62.21±2.61% respectively.
Similarly the NSAID, Diclofenac (10 - 100 mg/Kg, i.p) and the
steroidal anti-inflammatory drug dexamethasone (0.3 - 3 mg/Kg,
i.p) used as positive controls, dose-dependently inhibited the edema
with maximal effect of 87.96±1.11% and 67.47±3.51%
respectively. The potencies exhibited by all three extracts were
comparable to that shown by Diclofenac but higher than that of
Dexamethasone. Phenols were detected in all three extracts with the
highest concentration in the MWA. The extracts also scavenged DPPH with
EC50 values of 0.9784, 0.9096 and 0.2767 for PWA, CWA, MWA
respectively. The results of this study give scientific credence to the
local use of Wissadula amplissima to modulate inflammation induced by
stings of animals.
Eight dicationic compounds related to pentamidine were studied for trypanocidal activity in seven trypanosome isolates. In vitro studies revealed that diamidines are more potent than diimidazolines. ...For example,
2 (a diamidine) and
4 (a diimidazoline) inhibited the growth of KETRI 243 with IC
50 values of 2.3 and 900 nM, respectively. Introduction of polar groups into the linker decreased the effectiveness of the compounds against drug-resistant trypanosomes. In compounds with a 2-butene linker between the cationic groups,
trans-isomers were more potent than
cis-isomers. The
cis- and
trans-buteneamidines cured infection caused by
Trypanosoma
brucei
brucei (EATRO Lab 110) and protected mice against infection by
Trypanosoma
brucei
rhodesiense isolates, some of which are resistant to diamidines and melarsoprol.
A series of peptide aldehyde derivatives in which the P
2 chiral carbon has been replaced with a nitrogen atom were synthesized as urea-based peptidomimetic inhibitors of μ-calpain.
A series of ...peptide aldehyde derivatives in which the P
2 chiral carbon has been replaced with nitrogen were synthesized as urea-based peptidomimetic inhibitors of μ-calpain. The compounds mirrored the general SAR of peptidyl aldehyde calpain inhibitors but displayed greater selectivity for μ-calpain over cathepsin B.
A series of peptidyl α-ketoacids and α-ketoesters was synthesized and studied as μ-calpain inhibitors. Docking studies revealed that the μ-calpain inhibitory activity of the compounds is influenced ...by hydrogen bonding interactions and the potential for ionic interaction with active site residues as well as placement of a planar N-terminal capping group into the S3 pocket of the enzyme.
PDF
