scholarly journals The Pharmacological Activities of the Metabolites of N-[(Trimethylamineboryl)-Carbonyl]-L-Phenylalanine Methyl Ester

1996 ◽  
Vol 3 (5) ◽  
pp. 219-226 ◽  
Author(s):  
M. C. Miller ◽  
A. Sood ◽  
B. F. Spielvogel ◽  
R. P. Shrewsbury ◽  
I. H. Hall
Keyword(s):  
Methyl Ester ◽  
Parent Compound ◽  
Hypolipidemic Activity ◽  
Significant Activity ◽  
Male Mice ◽  
Anti Inflammatory ◽  
Foot Pad ◽  
Phenylalanine Methyl Ester ◽  
Better Than

The metabolites of N-[(trimethylamineboryl)-carbonyl]-L-phenylalanine methyl ester 1 proved to be active in a number of pharmacological screens where the parent had previously demonstrated potent activity. The proposed metabolites demonstrated significant activity as cytotoxic, hypolipidemic, and anti-inflammatory agents. In cytotoxicity screens several of the proposed metabolites afforded better activity than the parent compound against the growth of suspended and solid tumor cell lines. Evaluation of in vivo hypolipidemic activity demonstrated that the proposed metabolites of 1 were only moderately active and were generally less effective than the parent compound. Interestingly, L-phenylalanine methyl ester hydrochloride 3, which contains no boron atom, demonstrated equivalent hypolipidemic activity as the parent at 8 mg/kg/day in CF1 male mice. As anti-inflammatory agents the proposed metabolites demonstrated variable capacities to reduce foot pad inflammation. These compounds were similarly effective as the parent 1 at blocking local pain and were generally better than the parent at protecting CF1 male mice from LPS induced sepsis.

scholarly journals Antitrypanosomal activity of purine nucleosides can be enhanced by their conversion to O-acetylated derivatives.

1996 ◽  
Vol 40 (11) ◽  
pp. 2567-2572 ◽  
Author(s):  
J R Sufrin ◽  
D Rattendi ◽  
A J Spiess ◽  
S Lane ◽  
C J Marasco ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Parent Compound ◽  
Nucleoside Analogs ◽  
Significant Activity ◽  
Structural Class ◽  
Antitrypanosomal Activity ◽  
Salvage Pathways ◽  
Purine Salvage Pathways

Fifteen purine nucleosides and their O-acetylated ester derivatives were examined for in vitro antitrypanosomal activity against the LAB 110 EATRO isolate of Trypanosoma brucei brucei and two clinical isolates of Trypanosoma brucei rhodesiense. Initial comparisons of activity were made for the LAB 110 EATRO isolate. Three nucleoside analogs exhibited no significant activity (50% inhibitory concentrations [IC50s] of > 100 microM), whether they were O acetylated or unacetylated; three nucleosides showed almost equal activity (IC50s of < 5 microM) for the parent compound and the O-acetylated derivative; nine nucleosides showed significantly improved activity (> or = 3-fold) upon O acetylation; of these nine analogs, six displayed activity at least 10-fold greater than that of their parent nucleosides. The most significant results were those for four apparently inactive compounds which, upon O acetylation, displayed IC50s of < or = 25 microM. When the series of compounds was tested against T. brucei rhodesiense isolates (KETRI 243 and KETRI 269), their antitrypanosomal effects were comparable to those observed for the EATRO 110 strain. Thus, our studies of purine nucleosides have determined that O acetylation consistently improved their in vitro antitrypanosomal activity. This observed phenomenon was independent of their cellular enzyme targets (i.e., S-adenosylmethionine, polyamine, or purine salvage pathways). On the basis of our results, the routine preparation of O-acetylated purine nucleosides for in vitro screening of antitrypanosomal activity is recommended, since O acetylation transformed several inactive nucleosides into compounds with significant activity, presumably by improving uptake characteristics. O-acetylated purine nucleosides may offer in vivo therapeutic advantages compared with their parent nucleosides, and this possibility should be considered in future evaluations of this structural class of trypanocides.

scholarly journals EVALUATION OF ANTI-INFLAMMATORY AND ANTI-ARTHRITIC POTENTIAL OF FRACTIONS OF ECLIPTA PROSTRATA LINN

2019 ◽  
pp. 158-166
Author(s):  
HITESH MALHOTRA ◽  
MANJUSHA CHOUDHARY
Keyword(s):  
Ethyl Acetate ◽  
In Vitro Models ◽  
Chloroform Fraction ◽  
Significant Activity ◽  
Alcoholic Extract ◽  
Eclipta Prostrata ◽  
Edema Model ◽  
Anti Inflammatory

Objective: The objective of the study was to establish the anti-inflammatory and anti-arthritic potential of various fractions of Eclipta prostrata Linn. Methods: The four fractions, i.e., n-butanol, ethyl acetate, chloroform, and n-hexane from hydro-alcoholic extract were obtained. First, the fractions were evaluated through in vitro models, and then they were evaluated by in vivo anti-inflammatory model, i.e., carrageenan-induced paw edema model. Further, two active fractions were evaluated for the anti-arthritic activity using formaldehyde induced arthritis model. Results: The fractions at a dose of 100 and 200 mg/kg showed an anti-inflammatory activity, but the ethyl acetate and chloroform fraction will show maximum anti-inflammatory potential. Hence, they are further evaluated for anti-arthritic potential where they show significant activity. Conclusion: From the results, it is concluded that the ethyl acetate and chloroform fraction show significant anti-arthritic activity.

scholarly journals Preparation and Anti-Tumour Activity of Some Arylbismuth(III) Oxine Complexes

1998 ◽  
Vol 5 (5) ◽  
pp. 295-304 ◽  
Author(s):  
Katharine A. Smith ◽  
Glen B. Deacon ◽  
W. Roy Jackson ◽  
Edward R. T. Tiekink ◽  
Silvina Rainone ◽  
...  
Keyword(s):  
Phenyl Group ◽  
Significant Activity ◽  
X Ray ◽  
Crystallographic Study ◽  
Anti Tumour Activity ◽  
In Vivo Testing ◽  
Tumour Activity ◽  
Better Than

New arylbismuth(lll) oxinates, PhBi(MeOx)2, (p-MeC6H4)Bi(Ox)2, (p-MeC6H4)Bi(MeOx)2, (p-ClC6H4)Bi(Ox)2, and (p-ClC6H4)Bi(MeOx)2 (Ox− = quinolin-8-olate and MeOx−=2-methylquinolin-8-olate) have been prepared by reaction of the appropriate diarylbismuth chlorides with Na(Ox) or Na(MeOx) in the presence of 15-crown-5. An X-ray crystallographic study has shown PhBi(MeOx)2 to be a five coordinate monomer with distorted square pyramidal stereochemistry. Chelating MeOx ligands have a cisoid arrangement in the square plane and the phenyl group is apical. The lattice is stabilised by significant π-π interactions between centrosymmetric molecules. A range of these complexes has been shown to have high in vitro biological activity (comparable with or better than cisplatin) against L1210 leukaemia, the corresponding cisplatin resistant line, and a human ovarian cell line, SKOV-3. However, initial in vivo testing against a solid mouse plasmacytoma (PC6) and P388 leukaemia has not revealed significant activity.

Chlorogenic acid methyl ester exerts strong anti-inflammatory effectsviainhibiting the COX-2/NLRP3/NF-κB pathway

2018 ◽  
Vol 9 (12) ◽  
pp. 6155-6164 ◽  
Author(s):  
Lang Zhang ◽  
Ya Fan ◽  
Hanwen Su ◽  
Li Wu ◽  
Yuying Huang ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Chlorogenic Acid ◽  
Acid Methyl Ester ◽  
Acid Methyl ◽  
Cox 2 ◽  
Anti Inflammatory

In vivoandin vitrostudies show that chlorogenic acid methyl ester (CME) has been proven to be a potential nutraceutical for preventing inflammation.

Synthesis and Anti-Inflammatory and Antiulcer Activity of a Glycyrrhizic Acid Conjugate with L-Phenylalanine Methyl Ester

2020 ◽  
Vol 54 (3) ◽  
pp. 225-228
Author(s):  
L. A. Baltina ◽  
T. A. Sapozhnikova ◽  
S. F. Gabdrakhmanova ◽  
N. S. Makara ◽  
R. M. Kondratenko ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Glycyrrhizic Acid ◽  
Antiulcer Activity ◽  
Acid Conjugate ◽  
Anti Inflammatory ◽  
Phenylalanine Methyl Ester

scholarly journals Preliminary screening of Waltheria indica (L.) plant for its anti-inflammatory activity

2017 ◽  
Vol 9 (2) ◽  
Author(s):  
Amol Chandekar ◽  
Amber Vyas ◽  
Neeraj Upamanyu ◽  
Atul Tripathi ◽  
Surendra Agrawal
Keyword(s):  
Inflammatory Activity ◽  
In Vivo Model ◽  
Significant Activity ◽  
Standard Drug ◽  
Rat Paw Edema ◽  
Test Models ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Acute And Chronic Inflammation

<p dir="ltr"><span>The investigation on anti-inflammatory activity of the various extract of </span><span>Waltheria indica </span><span>L. </span><span>was reported to find out the pharmacological basis for its ethnomedical use. </span><span>The anti-inflammatory activity of the pet ether (PEW) and methanol (MEW) extracts of the leaves of </span><span>Waltheria indica </span><span>L. (</span><span>Malvaceae</span><span>)</span><span>were evaluated by using in vivo (Carrageenan &amp; histamine induced rat paw edema, cotton pellet granuloma test) models. It was observed that, all the extracts showed significant activity in the in-vivo model at the dose of 500 mg/kg b.w. orally, when compared with control and standard drugs. Of the two extracts tested, methanol extract MEW showed most significant activity well in comparison to the standard drug.  Therefore, present study suggests, potential of leaves of </span><span>Waltheria indica </span><span>L. in both models of acute and chronic inflammation.</span></p><p dir="ltr"> </p>

scholarly journals One-Pot Multicomponent Synthesis and Bioevaluation of Tetrahydroquinoline Derivatives as Potential Antioxidants, α-Amylase Enzyme Inhibitors, Anti-Cancerous and Anti-Inflammatory Agents

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2710
Author(s):  
Samra Farooq ◽  
Aqsa Mazhar ◽  
Areej Ghouri ◽  
Ihsan-Ul-Haq ◽  
Naseem Ullah
Keyword(s):  
Enzyme Inhibitors ◽  
Reducing Power ◽  
Proliferative Potential ◽  
Significant Activity ◽  
Multicomponent Synthesis ◽  
One Pot ◽  
Ic50 Value ◽  
Anti Inflammatory

Mankind has always suffered from multiple diseases. Therefore, there has been a rigorous need in the field of medicinal chemistry for the design and discovery of new and potent molecular entities. In this work, thirteen tetrahydroquinoline derivatives were synthesized and evaluated biologically for their antioxidant, α-amylase enzyme inhibitory, anti-proliferative and anti-inflammatory activities. SF8 showed the lowest IC50 of 29.19 ± 0.25 µg/mL by scavenging DPPH free radicals. SF5 showed significant antioxidant activity in total antioxidant capacity (TAC) and total reducing power (TRP) assays. SF5 and SF9 showed the maximum inhibition of α-amylase enzyme i.e., 97.47% and 89.93%, respectively, at 200 µg/mL concentration. Five compounds were shortlisted to determine their anti-proliferative potential against Hep-2C cells. The study was conducted for 24, 48 and 72 h. SF8 showed significant results, having an IC50 value of 11.9 ± 1.04 µM at 72 h when compared with standard cisplatin (IC50 value of 14.6 ± 1.01 µM). An in vitro nitric oxide (NO) assay was performed to select compounds for in vivo anti-inflammatory activity evaluation. SF13 scavenged the NO level to a maximum of 85% at 50 µM concentration, followed by SF1 and SF2. Based on the NO scavenging assay results, in vivo anti-inflammatory studies were also performed and the results showed significant activity compared to the standard, acetylsalicylic acid (ASA).

scholarly journals Aspirin-triggered 15-Epi-Lipoxin A4 (LXA4) and LXA4 Stable Analogues Are Potent Inhibitors of Acute Inflammation: Evidence for Anti-inflammatory Receptors

1997 ◽  
Vol 185 (9) ◽  
pp. 1693-1704 ◽  
Author(s):  
Tomoko Takano ◽  
Stefano Fiore ◽  
Jane F. Maddox ◽  
Hugh R. Brady ◽  
Nicos A. Petasis ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Specific Binding ◽  
Chinese Hamster Ovary Cells ◽  
Chinese Hamster ◽  
Neutrophil Infiltration ◽  
Eicosatetraenoic Acid ◽  
Myeloperoxidase Activity ◽  
Leukotriene D4 ◽  
Anti Inflammatory

Lipoxins are bioactive eicosanoids that are immunomodulators. In human myeloid cells, lipoxin (LX) A4 actions are mediated by interaction with a G protein–coupled receptor. To explore functions of LXA4 and aspirin-triggered 5(S),6(R),15(R)-trihydroxy-7,9,13-trans-11-cis–eicosatetraenoic acid (15-epi-LXA4) in vivo, we cloned and characterized a mouse LXA4 receptor (LXA4R). When expressed in Chinese hamster ovary cells, the mouse LXA4R showed specific binding to [3H]LXA4 (Kd ≈ 1.5 nM), and with LXA4 activated GTP hydrolysis. Mouse LXA4R mRNA was most abundant in neutrophils. In addition to LXA4 and 15-epi-LXA4, bioactive LX stable analogues competed with both [3H]LXA4 and [3H]leukotriene D4 (LTD4)– specific binding in vitro to neutrophils and endothelial cells, respectively. Topical application of LXA4 analogues and novel aspirin-triggered 15-epi-LXA4 stable analogues to mouse ears markedly inhibited neutrophil infiltration in vivo as assessed by both light microscopy and reduced myeloperoxidase activity in skin biopsies. The 15(R)-16-phenoxy-17,18, 19,20-tetranorLXA4 methyl ester (15-epi-16-phenoxy-LXA4), an analogue of aspirin triggered 15-epi-LXA4, and 15(S)-16-phenoxy-17,18,19,20-tetranor-LXA4 methyl ester (16-phenoxy-LXA4) were each as potent as equimolar applications of the anti-inflammatory, dexamethasone. Thus, we identified murine LXA4R, which is highly expressed on murine neutrophils, and showed that both LXA4 and 15-epi-LXA4 stable analogues inhibit neutrophil infiltration in the mouse ear model of inflammation. These findings provide direct in vivo evidence for an anti-inflammatory action for both aspirin-triggered LXA4 and LXA4 stable analogues and their site of action in vivo.

scholarly journals In vitro and In vivo Anti-inflammatory Activity of the Extracts of Whole Plant Argyreia imbricata (Roth) Sant. & Patel

2020 ◽  
Vol 11 (4) ◽  
pp. 7317-7322
Author(s):  
Sebastin V ◽  
Gopalakrishnan G ◽  
Sreejith M ◽  
Anoob Kumar K I
Keyword(s):  
Ethyl Acetate ◽  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
Albino Rats ◽  
Significant Activity ◽  
In Vivo Evaluation ◽  
Whole Plant ◽  
Anti Inflammatory

Plants of the genus Argyreia have ethnomedicinal importance, and several pharmacological activities are also reported. In this study, the anti-inflammatory activity of different extracts of Argyreia imbricata was evaluated by in vitro and in vivo methods. In both evaluations, standard, Diclofenac sodium was used for comparative evaluation. In this study, extraction of powdered whole plant material was done with different solvents viz., petroleum ether, chloroform, ethyl acetate and methanol by soxhelation. In vitro anti-inflammatory activity of all the prepared extracts was evaluated by stabilization of human red blood cell (HRBC) membrane in different temperature and tonicity conditions. Among the six different concentrations of four tested extracts, the ethyl acetate and methanol extracts (1000μg/ml) showed significant activity in the in vitro evaluation. They were selected for the in vivo evaluation on the paw oedema induced by carrageenan on Wistar albino rats. Two doses, 200mg.kg-1 and 400mg.kg-1 of the test extracts were subjected to evaluation. Both the tested extracts showed the activity, particularly, the methanol extract in the dose of 400mg.kg-1 showed significant activity. Results of this study strongly supported the anti-inflammatory activity of the tested extracts. Further, studies on toxicity, identification, isolation of the active constituents may give useful results.

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