scholarly journals Pachypodostyflavone, a New 3-methoxy Flavone and Other Constituents with Antifilarial Activities from the Stem Bark of Duguetia staudtii

2021 ◽  
Vol 8 (02) ◽  
pp. e56-e61
Author(s):  
Alexis Sylvain Wafo Mbobda ◽  
Alain Wembe Ngouonpe ◽  
Gervais Mouthé Happi ◽  
Bel Youssouf G. Mountessou ◽  
Elvis Monya ◽  
...  
Keyword(s):  
Adult Male ◽  
Spectroscopic Data ◽  
High Resolution Mass Spectrometry ◽  
Stem Bark ◽  
Methoxy Flavone ◽  
Bioassay Guided Fractionation ◽  
Onchocerca Ochengi ◽  
Negative Controls ◽  
Flavone Derivative

AbstractA new flavone derivative named pachypodostyflavone (1), along with 8 known compounds (2–9) and a mixture of β-sitosterol and stigmasterol were isolated from the stem bark of Duguetia staudtii (Annonaceae), based on a bioassay-guided fractionation. Their structures were determined using high-resolution mass spectrometry and NMR spectroscopic data, as well as by comparison with the literature values of their analogs. Selected isolated compounds were evaluated for their in vitro antifilaricidal activities on Onchocerca ochengi microfilariae and adult worms. Inhibition of motility was evaluated spectroscopically on microfilaria and adult male worms. Viability was determined on adult female worms by the MTT/ Formazan assay. Auranofin at 10 µM and 2% DMSO were used as positive and negative controls, respectively. Compounds 1 and 7 showed potent anti-onchocerca activities with 100% activity at 250 µg/mL on both O. ochengi adult male and female worms, while compound 5 displayed 100% activity at 30 µg/mL.

In-vitro uptake of ivermectin by adult male Onchocerca ochengi

1998 ◽  
Vol 92 (6) ◽  
pp. 711-720 ◽  
Author(s):  
H. F. Cross ◽  
A. Renz ◽  
A. J. Trees
Keyword(s):  
Adult Male ◽  
Onchocerca Ochengi ◽  
In Vitro Uptake

scholarly journals Cytotoxic Steroids from The Stem Bark of Chisocheton cumingianus (Meliaceae)

Molekul ◽  
2017 ◽  
Vol 12 (1) ◽  
pp. 1 ◽  
Author(s):  
Dewa Gede Katja ◽  
Kindi Farabi ◽  
Nurlelasari Nurlelasari ◽  
Desi Harneti ◽  
Euis Julaeha ◽  
...  
Keyword(s):  
Spectroscopic Data ◽  
Stem Bark ◽  
Leukemia Cells ◽  
Cytotoxic Effects ◽  
Cytotoxicity Activity ◽  
Chemical Structures ◽  
Cytotoxic Steroids ◽  
Murine Leukemia

Three cytotoxic steroids, stigmasterol (1), stigmast-5-en-3b-ol (2) and b-sitosterol-3-O-acetate (3) were isolated from the stem bark of Chisocheton cumingianus. The chemical structures of those compounds were identified based on spectroscopic data and by comparison with those data previously reported. All of the compounds isolated were evaluated for their cytotoxic effects against P-388 murine leukemia cells in vitro. Compounds 1-3 showed cytotoxicity activity against P-388 murine leukemia cells with IC50values of 12.4, 60.8, and ˃ 100 mg/mL, respectively.

scholarly journals Chemical and Bioactivity Evaluation of the Bark of Neonauclea purpurea

2012 ◽  
Vol 7 (2) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Netiya Karaket ◽  
Kanyaratt Supaibulwatana ◽  
Supatsara Ounsuk ◽  
Valérie Bultel-Poncé ◽  
Van Cuong Pham ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Traditional Medicine ◽  
Resistant Strain ◽  
Antimalarial Activity ◽  
Indole Alkaloids ◽  
Vero Cells ◽  
Stem Bark ◽  
Meoh Extract ◽  
Bioassay Guided Fractionation

Bioassay-guided fractionation of the MeOH extract from the stem bark of Neonauclea purpurea used in traditional medicine, resulted in the isolation of 2 indole alkaloids, cadambine (1) and α-dihydrocadambine (2), as well as a quinolic compound, 2,6-dimethoxy-1,4-benzoquinone (3). Antimalarial activity evaluation showed that compounds 2 and 3 exhibited mild in vitro antimalarial activity against Plasmodium falciparum, the chloroquine-resistant strain K1 with IC50 values of 6.6 and 11.3 μM, respectively. Compounds 1 and 2 showed no cytotoxicity to monkey (Vero) cells, but compound 3 showed weak cytotoxicity with an IC50 value of 1.19 μM.

scholarly journals Prenylated Isoflavanones from the Stem Bark of Erythrina poeppigiana (Leguminosae) and its Antimalarial Properties

2017 ◽  
Vol 12 (8) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Tati Herlina ◽  
Anderson Arnold Aloanis ◽  
Dikdik Kurnia ◽  
Desi Harneti ◽  
Rani Maharani ◽  
...  
Keyword(s):  
Methanol Extract ◽  
Ethyl Acetate Extract ◽  
Antimalarial Activity ◽  
Stem Bark ◽  
In Vitro Bioassay ◽  
Erythrina Poeppigiana ◽  
Antimalarial Agents ◽  
Bioassay Guided Fractionation ◽  
Promising Source

During the course of our continuous search for novel antimalarial compounds derived from the Indonesian Erythrina plants, the methanol extract of the stem bark of Erythrina poeppigiana demonstrated significant antimalarial activity against Plasmodium falciparum parasites, in vitro. Bioassay-guided fractionation of the ethyl acetate extract resulted in the isolation of three known platyisoflavanone (1), erypogein D (2), and sophoraisoflavanone A (3). Compounds 1–3 showed strong antimalarial activity against 3D7 strain of P. falciparum with IC50 values of 0.52, 0.36, and 3.65μM, respectively. This result indicates that stem bark of E. poeppigiana is a promising source of antimalarial agents, and merits further investigation.

scholarly journals Identification of Dipeptidyl Peptidase-4 and α-Amylase Inhibitors from Melicope glabra (Blume) T. G. Hartley (Rutaceae) Using Liquid Chromatography Tandem Mass Spectrometry, In Vitro and In Silico Methods

Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 1
Author(s):  
Alexandra Quek ◽  
Nur Kartinee Kassim ◽  
Amin Ismail ◽  
Muhammad Alif Mohammad Latif ◽  
Khozirah Shaari ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Computational Study ◽  
Stem Bark ◽  
Dipeptidyl Peptidase ◽  
Chloroform Extract ◽  
Dipeptidyl Peptidase 4 ◽  
Bioassay Guided Fractionation ◽  
Liquid Chromatography Tandem Mass ◽  
Amylase Inhibitors

The present study investigated the antidiabetic properties of the extracts and fractions from leaves and stem bark of M. glabra based on dipeptidyl peptidase-4 (DPP-4) and α-Amylase inhibitory activity assays. The chloroform extract of the leaves was found to be most active towards inhibition of DPP-4 and α-Amylase with IC50 of 169.40 μg/mL and 303.64 μg/mL, respectively. Bioassay-guided fractionation of the leaves’ chloroform extract revealed fraction 4 (CF4) as the most active fraction (DPP-4 IC50: 128.35 μg/mL; α-Amylase IC50: 170.19 μg/mL). LC-MS/MS investigation of CF4 led to the identification of trans-decursidinol (1), swermirin (2), methyl 3,4,5-trimethoxycinnamate (3), renifolin (4), 4′,5,6,7-tetramethoxy-flavone (5), isorhamnetin (6), quercetagetin-3,4′-dimethyl ether (7), 5,3′,4′-trihydroxy-6,7-dimethoxy-flavone (8), and 2-methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one (9) as the major components. The computational study suggested that (8) and (7) were the most potent DPP-4 and α-Amylase inhibitors based on their lower binding affinities and extensive interactions with critical amino acid residues of the respective enzymes. The binding affinity of (8) with DPP-4 (−8.1 kcal/mol) was comparable to that of sitagliptin (−8.6 kcal/mol) while the binding affinity of (7) with α-Amylase (−8.6 kcal/mol) was better than acarbose (−6.9 kcal/mol). These findings highlight the phytochemical profile and potential antidiabetic compounds from M. glabra that may work as an alternative treatment for diabetes.

In vitro and computational studies on the antiglycation activity of compounds isolated from antidiabetic Tetracera alnifolia stem bark

2021 ◽  
pp. 1-10
Author(s):  
Kelly Oriakhi ◽  
Collins U. Ibeji ◽  
Emmanuel E. Essien ◽  
Nkeiruka Eluehike ◽  
Kissinger Orumwensodia ◽  
...  
Keyword(s):  
Stem Bark ◽  
Computational Studies ◽  
Tetracera Alnifolia

scholarly journals Nontargeted Metabolomics by High-Resolution Mass Spectrometry to Study the In Vitro Metabolism of a Dual Inverse Agonist of Estrogen-Related Receptors β and γ, DN203368

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 776
Author(s):  
Sin-Eun Kim ◽  
Seung-Bae Ji ◽  
Euihyeon Kim ◽  
Minseon Jeong ◽  
Jina Kim ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
High Resolution ◽  
Human Liver ◽  
High Resolution Mass Spectrometry ◽  
Liver Microsomes ◽  
Human Liver Microsomes ◽  
Rat Liver Microsomes ◽  
High Resolution Mass ◽  
Resolution Mass

DN203368 ((E)-3-[1-(4-[4-isopropylpiperazine-1-yl]phenyl) 3-methyl-2-phenylbut-1-en-1-yl] phenol) is a 4-hydroxy tamoxifen analog that is a dual inverse agonist of estrogen-related receptor β/γ (ERRβ/γ). ERRγ is an orphan nuclear receptor that plays an important role in development and homeostasis and holds potential as a novel therapeutic target in metabolic diseases such as diabetes mellitus, obesity, and cancer. ERRβ is also one of the orphan nuclear receptors critical for many biological processes, such as development. We investigated the in vitro metabolism of DN203368 by conventional and metabolomic approaches using high-resolution mass spectrometry. The compound (100 μM) was incubated with rat and human liver microsomes in the presence of NADPH. In the metabolomic approach, the m/z value and retention time information obtained from the sample and heat-inactivated control group were statistically evaluated using principal component analysis and orthogonal partial least-squares discriminant analysis. Significant features responsible for group separation were then identified using tandem mass spectra. Seven metabolites of DN203368 were identified in rat liver microsomes and the metabolic pathways include hydroxylation (M1-3), N-oxidation (M4), N-deisopropylation (M5), N,N-dealkylation (M6), and oxidation and dehydrogenation (M7). Only five metabolites (M2, M3, and M5-M7) were detected in human liver microsomes. In the conventional approach using extracted ion monitoring for values of mass increase or decrease by known metabolic reactions, only five metabolites (M1-M5) were found in rat liver microsomes, whereas three metabolites (M2, M3, and M5) were found in human liver microsomes. This study revealed that nontargeted metabolomics combined with high-resolution mass spectrometry and multivariate analysis could be a more efficient tool for drug metabolite identification than the conventional approach. These results might also be useful for understanding the pharmacokinetics and metabolism of DN203368 in animals and humans.

scholarly journals Macrophagic Inflammatory Response Next to Dental Implants with Different Macro- and Micro-Structure: An In Vitro Study

2021 ◽  
Vol 11 (12) ◽  
pp. 5324
Author(s):  
Maria Menini ◽  
Francesca Delucchi ◽  
Domenico Baldi ◽  
Francesco Pera ◽  
Francesco Bagnasco ◽  
...  
Keyword(s):  
Inflammatory Response ◽  
Dental Implants ◽  
In Vitro Study ◽  
Titanium Implants ◽  
Implant Surface ◽  
Bone Implant ◽  
Optimal Outcomes ◽  
Negative Controls ◽  
Inflammatory Effect

(1) Background: Intrinsic characteristics of the implant surface and the possible presence of endotoxins may affect the bone–implant interface and cause an inflammatory response. This study aims to evaluate the possible inflammatory response induced in vitro in macrophages in contact with five different commercially available dental implants. (2) Methods: one zirconia implant NobelPearl® (Nobel Biocare) and four titanium implants, Syra® (Sweden & Martina), Prama® (Sweden & Martina), 3iT3® (Biomet 3i) and Shard® (Mech & Human), were evaluated. After 4 h of contact of murine macrophage cells J774a.1 with the implants, the total RNA was extracted, transcribed to cDNA and the gene expression of the macrophages was evaluated by quantitative PCR (qPCR) in relation to the following genes: GAPDH, YWHAZ, IL1β, IL6, TNFα, NOS2, MMP-9, MMP-8 and TIMP3. The results were statistically analyzed and compared with negative controls. (3) Results: No implant triggered a significant inflammatory response in macrophages, although 3iT3 exhibited a slight pro-inflammatory effect compared to other samples. (4) Conclusions: All the samples showed optimal outcomes without any inflammatory stimulus on the examined macrophagic cells.

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