Objective: To screen plant extract fractions and elucidate the components present in Caesalpinia crista(C. crista) leaves for cholinergic and anti-amyloidogenic activities for the treatment of Alzheimer's diseases...Objective: To screen plant extract fractions and elucidate the components present in Caesalpinia crista(C. crista) leaves for cholinergic and anti-amyloidogenic activities for the treatment of Alzheimer's diseases. Methods: This work has been carried out to study the action of C. crista extracts from nonpolar to polar solvents toward inhibition of oxidative stress, cholinergic and amyloidosis. The antioxidant activity was studied using DPPH total antioxidant assay; cholinergic assay by Ellman's method and anti-amyloidogenic assay by thioflavin-T fluorescence and transmission electron microscopy. Results: The quantification of polyphenols was carried out following C. crista methanolic extract(CCMeOH) HPLC fingerprinting, along with LC-MS and elucidated by MS LAMPS database. GC-MS of CCMeOH was screened for potential moieties. In vitro experimental results showed that the CCMe OH was potential extract that exhibited active inhibition of antioxidant property, cholinergic enzymes acetylcholinesterase and butyrylcholinesterase. For anti-amyloidogenic evaluations, among all the extracts, the CCMe OH was found to have the potential toward inhibiting the oligomers, fibrillation of Aβ42 with good defibrillation of amyloid cascading properties. Conclusions: These results are also supported by the presence of polyphenols as the active ingredients. Multi-potent target drug therapy is a promising option in treating the Alzheimer's diseases. Methanolic extract of C. crista shows potential activity against cholinergic enzymes, Aβ42 aggregation with antioxidant activity.展开更多
Multicellular organisms use chemical messengers to transmit signals among organelles and to other cells. Relatively small hydrophobic molecules such as lipids are excellent candidates for this signaling purpose. In mo...Multicellular organisms use chemical messengers to transmit signals among organelles and to other cells. Relatively small hydrophobic molecules such as lipids are excellent candidates for this signaling purpose. In most proteins, palmitic acid and other saturated and some unsaturated fatty acids are esterified to the free thiol of cysteines and to the N-amide terminal. This palmitoylation process enhances the surface hydrophobicity and membrane affinity of protein substrates and plays important roles in modulating proteins’ trafficking, stability, and sorting etc. Protein palmitoylation has been involved in numerous cellular processes, including signaling, apoptosis, and neuronal transmission. The palmitoylation process is involved in multiple diseases such as Huntington’s disease, various cardiovascular and T-cell mediated immune disorders, as well as cancer. Protein palmitoylation through the thioester (S-acylation) is unique in that it is the only reversible lipid modification. Our study on lipopolysaccharide (LPS) and deoxynivalenol (DON) treatment to rats provides some insights to the complex role of protein palmitoylation in chemical and microbial toxicity. In contrast, myrisoylated proteins contain the 14-carbon fatty acid myristate attached via amide linkage to the N-terminal glycine residue of protein, and occur cotranslationally. The bacterial outer membrane enzyme lipid A palmitoyltransferase (PagP) confers resistance to host immune defenses by transferring a palmitate chain from a phospholipid to the lipid A component of LPS. PagP is sensitive to cationic antimicrobial peptides (CAMP) which are included among the products of the Toll-like receptor 4 (TLR4) signal transduction pathway. This modification of lipid A with a palmitate appears to both and protects the pathogenic bacteria from host immune defenses and attenuates the activation of those same defenses through the TLR4 signal transduction pathway.展开更多
Stress and emotion are associated with several illnesses from headaches to heart diseases and immune deficiencies to central nervous system. Terminalia arjuna has been referred as traditional Indian medicine for sever...Stress and emotion are associated with several illnesses from headaches to heart diseases and immune deficiencies to central nervous system. Terminalia arjuna has been referred as traditional Indian medicine for several ailments. The present study aimed to elucidate the effect of T. arjuna bark extract(TA) against picrotoxin-induced anxiety. Forty two male Balb/c mice were randomly divided into six experimental groups(n = 7): control, diazepam(1.5 mg·kg^(–1)), picrotoxin(1 mg·kg^(–1)) and three TA treatemt groups(25, 50, and 100 mg/kg). Behavioral paradigms and PCR studies were performed to determine the effect of TA against picrotoxin-induced anxiety. The results showed that TA supplementation increased locomotion towards open arm(EPM) and illuminated area(light-dark box test), and increased rearing frequency(open field test) in a dose dependent manner, compared to picrotoxin(P < 0.05). Furthermore, TA increased number of licks and shocks in Vogel's conflict. PCR studies showed an up-regulation of several genes, such as BDNF, IP_3, D_2L, CREB, GABAA, SOD, GPx, and GR in TA administered groups. In conclusion, alcoholic extract of TA bark showed protective activity against picrotoxin in mice by modulation of genes related to synaptic plasticity, neurotransmitters, and antioxidant enzymes.展开更多
基金Jain University,Bangalore for the financial support
文摘Objective: To screen plant extract fractions and elucidate the components present in Caesalpinia crista(C. crista) leaves for cholinergic and anti-amyloidogenic activities for the treatment of Alzheimer's diseases. Methods: This work has been carried out to study the action of C. crista extracts from nonpolar to polar solvents toward inhibition of oxidative stress, cholinergic and amyloidosis. The antioxidant activity was studied using DPPH total antioxidant assay; cholinergic assay by Ellman's method and anti-amyloidogenic assay by thioflavin-T fluorescence and transmission electron microscopy. Results: The quantification of polyphenols was carried out following C. crista methanolic extract(CCMeOH) HPLC fingerprinting, along with LC-MS and elucidated by MS LAMPS database. GC-MS of CCMeOH was screened for potential moieties. In vitro experimental results showed that the CCMe OH was potential extract that exhibited active inhibition of antioxidant property, cholinergic enzymes acetylcholinesterase and butyrylcholinesterase. For anti-amyloidogenic evaluations, among all the extracts, the CCMe OH was found to have the potential toward inhibiting the oligomers, fibrillation of Aβ42 with good defibrillation of amyloid cascading properties. Conclusions: These results are also supported by the presence of polyphenols as the active ingredients. Multi-potent target drug therapy is a promising option in treating the Alzheimer's diseases. Methanolic extract of C. crista shows potential activity against cholinergic enzymes, Aβ42 aggregation with antioxidant activity.
文摘Multicellular organisms use chemical messengers to transmit signals among organelles and to other cells. Relatively small hydrophobic molecules such as lipids are excellent candidates for this signaling purpose. In most proteins, palmitic acid and other saturated and some unsaturated fatty acids are esterified to the free thiol of cysteines and to the N-amide terminal. This palmitoylation process enhances the surface hydrophobicity and membrane affinity of protein substrates and plays important roles in modulating proteins’ trafficking, stability, and sorting etc. Protein palmitoylation has been involved in numerous cellular processes, including signaling, apoptosis, and neuronal transmission. The palmitoylation process is involved in multiple diseases such as Huntington’s disease, various cardiovascular and T-cell mediated immune disorders, as well as cancer. Protein palmitoylation through the thioester (S-acylation) is unique in that it is the only reversible lipid modification. Our study on lipopolysaccharide (LPS) and deoxynivalenol (DON) treatment to rats provides some insights to the complex role of protein palmitoylation in chemical and microbial toxicity. In contrast, myrisoylated proteins contain the 14-carbon fatty acid myristate attached via amide linkage to the N-terminal glycine residue of protein, and occur cotranslationally. The bacterial outer membrane enzyme lipid A palmitoyltransferase (PagP) confers resistance to host immune defenses by transferring a palmitate chain from a phospholipid to the lipid A component of LPS. PagP is sensitive to cationic antimicrobial peptides (CAMP) which are included among the products of the Toll-like receptor 4 (TLR4) signal transduction pathway. This modification of lipid A with a palmitate appears to both and protects the pathogenic bacteria from host immune defenses and attenuates the activation of those same defenses through the TLR4 signal transduction pathway.
文摘Stress and emotion are associated with several illnesses from headaches to heart diseases and immune deficiencies to central nervous system. Terminalia arjuna has been referred as traditional Indian medicine for several ailments. The present study aimed to elucidate the effect of T. arjuna bark extract(TA) against picrotoxin-induced anxiety. Forty two male Balb/c mice were randomly divided into six experimental groups(n = 7): control, diazepam(1.5 mg·kg^(–1)), picrotoxin(1 mg·kg^(–1)) and three TA treatemt groups(25, 50, and 100 mg/kg). Behavioral paradigms and PCR studies were performed to determine the effect of TA against picrotoxin-induced anxiety. The results showed that TA supplementation increased locomotion towards open arm(EPM) and illuminated area(light-dark box test), and increased rearing frequency(open field test) in a dose dependent manner, compared to picrotoxin(P < 0.05). Furthermore, TA increased number of licks and shocks in Vogel's conflict. PCR studies showed an up-regulation of several genes, such as BDNF, IP_3, D_2L, CREB, GABAA, SOD, GPx, and GR in TA administered groups. In conclusion, alcoholic extract of TA bark showed protective activity against picrotoxin in mice by modulation of genes related to synaptic plasticity, neurotransmitters, and antioxidant enzymes.
