A Neuroinflammation Inhibitor, Hypoxylon xanthone A, from Soil Fungus Hypoxylon sp.

2020 ◽  
Vol 17 (2) ◽  
pp. 116-120
Author(s):  
Ying Xiao ◽  
Bing Xu ◽  
You Kang ◽  
Yuedi Li ◽  
Yong Cui ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Nmr Spectra ◽  
Soil Fungus ◽  
2D Nmr ◽  
Inhibitory Effect ◽  
No Production ◽  
Dependent Manner ◽  
Solid Culture ◽  
2D Nmr Spectra ◽  
Dose Dependent

: Hypoxylon sp. was used to ferment at 25°C for 45 days. The solid culture of Hypoxylon sp. was extracted with 75% EtOH under ultrasonic for twice. And the dried combined extracts were then suspended in H2O and partitioned with ethyl acetate. EtOAc extracts were subjected to a silica gel column and eluted with petroleum ether - acetone to a.ord seven fractions. Sephadex LH-20 and RPHPLC were used subsequently to yield a novel xanthone metabolite (Hypoxylon xanthone A). Its structure was elucidated based on HR-ESI-MS, 1D-, 2D-NMR spectra, and the comparison of the experimental and calculated ECD spectra. The anti-neuroinflammatory assay of Hypoxylon xanthone A, as manifested by the inhibitory effect on LPS-induced NO production in BV-2 microglial cells, indicated almost the same inhibitory effect as minocycline in a dose-dependent manner within the concentration of 1-50 μM, suggesting that Hypoxylon xanthone A could be a new potential neuroinflammation inhibitor.

scholarly journals A New Megastigmane Glucoside and Other Constituents from Desmodium gangeticum

2020 ◽  
Vol 2020 ◽  
pp. 1-4
Author(s):  
Hau Viet Dang ◽  
Giang Hoang Do ◽  
Phuong Thi Ngo ◽  
Tien Dat Nguyen ◽  
Ha Minh Le
Keyword(s):  
Nmr Spectra ◽  
Aerial Part ◽  
2D Nmr ◽  
Inhibitory Effect ◽  
Methyl Benzoate ◽  
Raw264.7 Cells ◽  
No Production ◽  
2D Nmr Spectra ◽  
Ic50 Values ◽  
Megastigmane Glucoside

A new megastigmane glycoside, gangeticoside (1), and three known compounds leonuriside A (2), methyl benzoate 2-O-β-D-glucopyranoside (3), and tortoside A (4) were isolated from the aerial part of Desmodium gangeticum. Their structures were determined by 1D and 2D NMR spectra. The isolated compounds were evaluated for their inhibitory effect on NO production in LPS-stimulated RAW264.7 cells. Among them, compounds 1, 2, and 3 exhibited strong effect with the IC50 values of 22.3, 15.6, 7.3 μM, respectively.

scholarly journals Chemical constituents from the ethyl acetate and n-butanol extracts of the stems of Buchanania lucida Blume (Anacardiaceae)

2018 ◽  
Vol 1 (T5) ◽  
pp. 167-171
Author(s):  
Tung Thanh Nguyen ◽  
Thuong Thi Nguyen ◽  
Phu Hoang Dang ◽  
Trong Nguyen Huu Phan ◽  
Nhan Trung Nguyen
Keyword(s):  
Phenolic Compounds ◽  
Methyl Ester ◽  
Ethyl Acetate ◽  
Nmr Spectra ◽  
Chemical Structure ◽  
Chemical Constituents ◽  
2D Nmr ◽  
Published Data ◽  
2D Nmr Spectra ◽  
Aloe Emodin

There is no research on the chemical constituents investigation and bioactivity evaluation of Buchanania lucida Blume (Anacardiaceae). From the stems of Buchanania lucida collected at Dong Nai province, the ethyl acetate and n-butanol extracts were prepared. Four phenolic compounds: protocatechuic methyl ester (1), aloe-emodin (2), naringenin (3), and glucosyringic acid (4) were isolated from these extracts. The chemical structure of these compounds were elucidated by 1D and 2D NMR spectra and comparison with published data. These compounds were first reported in Buchanania lucida.

scholarly journals Zizaane-Type Sesquiterpenoids and Their Rearranged Derivatives from Agarwood of an Aquilaria Plant

Molecules ◽  
2021 ◽  
Vol 27 (1) ◽  
pp. 198
Author(s):  
Jing-Zhe Yuan ◽  
Yi-Ling Yang ◽  
Wei Li ◽  
Li Yang ◽  
Hao-Fu Dai ◽  
...  
Keyword(s):  
Absolute Configuration ◽  
Ethyl Ether ◽  
Nmr Spectra ◽  
2D Nmr ◽  
Raw264.7 Cells ◽  
No Production ◽  
Ether Extract ◽  
Ic50 Value ◽  
2D Nmr Spectra

Nine new sesquiterpenoids (1–9) were isolated from ethyl ether extract of agarwood originated from Aquilaria sp., including three novel sesquiterpenoids (1–3) derived from zizaane, together with six zizaane-type sesquiterpenoids (4–9). All structures were unambiguously elucidated based on 1D and 2D NMR spectra as well as by HRESIMS data. The absolute configuration of sesquiterpenoids was determined by comparison of the experimental and computed ECD spectra. In vitro anti-inflammatory assessment showed that compound 9 exhibited inhibition of NO production in LPS-stimulated RAW264.7 cells with an IC50 value of 62.22 ± 1.27 μM.

scholarly journals CONTRIBUTE TO STUDY ON CHEMICAL CONSTITUENTS OF DESMODIUM GANGETICUM (L.) DC. OF VIETNAM

2019 ◽  
Vol 57 (1) ◽  
pp. 1
Author(s):  
Le Minh Ha ◽  
Ngo Thi Phuong ◽  
Do Thi Thanh Huyen ◽  
Duong Bich Ngoc ◽  
Nguyen Minh Nguyet ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Nmr Spectra ◽  
Ethyl Acetate Extract ◽  
Chemical Constituents ◽  
2D Nmr ◽  
2D Nmr Spectra ◽  
First Time

From the ethyl acetate extract of the leaves of Desmodium gangeticum collected in Me Linh, Ha Noi, we isolated 5 compounds including luteolin (1), luteolin tetramethyl ether (2),  N,N-dimethyl tetradecane-1-amin (3), D-pinitol (4)  and stigmasterol (5). In which, luteolin (1) was isolated from Desmodium gangeticum for the first time, luteolin tetramethyl ether (2) and  N,N-dimethyl tetradecane-1-amin (3) were first isolated from genus Desmodium. Their structures were determined by 1D and 2D NMR spectra.

Synthesis and Assessment of Novel Anti-chlamydial Benzylidene Acylhydrazides Derivatives

2018 ◽  
Vol 15 (1) ◽  
pp. 31-36 ◽  
Author(s):  
Xiaofeng Bao ◽  
Ying Xue ◽  
Chao Xia ◽  
Yin Lu ◽  
Ningjing Yang ◽  
...  
Keyword(s):  
Inhibitory Effect ◽  
Dependent Manner ◽  
Iron Starvation ◽  
Hydrochloride Salt ◽  
Obligate Intracellular ◽  
Biphasic Life Cycle ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Dose Dependent ◽  
Better Than

Background: Chlamydiae, characterized by a unique biphasic life cycle, are a group of Gram-negative obligate intracellular bacterial pathogens responsible for diseases in a range of hosts including humans. Benzylidene acylhydrazide CF0001 could inhibit chlamydiae independent of iron starvation and T3SS inhibition. This finding promoted us to design and synthesize more benzylidene acylhydrazides to find novel anti-chlamydial agents. Methods: The carboxylic acids 1a-1d were coupled with Boc-hydrazide inpresence of EDCI and DMAP to obtain the intermediate 2a-2d in 60-62% yields. N-Boc deprotections were performed to obtain hydrazide hydrochloride salt 3a-3d. Nextly, the hydrazides were subjected to condensation with aldehydes to obtain benzylidene acylhydrazides 4a-4g in 30-52% yields in two steps. Results: Compound 4d exhibited best inhibitory effect on the formation and growth of chlamydial inclusions. The IC50 value of compound 4d for infectious progenies was 3.55 µM, better than 7.30 µM of CF0001. Conclusion: To find novel anti-chlamydial agents, we have designed and synthesized benzylidene acylhydrazides 4a-4g. Compounds 4a, 4d, 4g showed inhibitory activity on C. muridarum with the IC50 values from 3.55-12 µM. The 3,5-dibromo-4-hydroxyl substitutes on ring B are critical to keep their anti-chlamydial activity. Compound 4d inhibited C. muridarum in a dose-dependent manner without apparent cytotoxicity.

A Cytotoxic Natural Product from Patrinia villosa Juss

2019 ◽  
Vol 19 (11) ◽  
pp. 1399-1404 ◽  
Author(s):  
Yangcheng Liu ◽  
Wei Liu ◽  
Changlan Chen ◽  
Zheng Xiang ◽  
Hongwei Liu
Keyword(s):  
Cell Cycle ◽  
Cell Lines ◽  
Silica Gel ◽  
Column Chromatography ◽  
Bioactive Compound ◽  
Antitumor Agent ◽  
2D Nmr ◽  
Preparative Hplc ◽  
Dependent Manner ◽  
2D Nmr Spectra

Background and Purpose:: Patrinia villosa Juss is an important Chinese herbal medicine widely used for thousands of years, but few reports on the ingredients of the herb have been presented. In this study, we aim to isolate the bioactive compound from the plant. Material and Methods:: The air-dried leaves of P. villosa (15kg) were extracted three times with 70% EtOH under reflux. The condensed extract was suspended in H2O and partitioned with light petroleum, dichloromethane and n-BuOH. The dichloromethane portion was then subjected to normal-phase silica gel column chromatography, ODS silica gel column chromatography and semi-preparative HPLC to yield compound 1. Cytotoxicities of 1 were assayed on HepG2, A549 and A2780 cell lines. The mechanism of apoptosis and cell cycle on A549 was confirmed subsequently. Results: A new impecylone (Impecylone A) was isolated from the leaves of Patrinia villosa Juss, and its structures were established using 1D, 2D-NMR spectra and HR-ESI-MS. Impecylone A could selectivity inhibit HepG2 and A549 cell lines. The compound could induce apoptosis of A549 and arrest the cell cycle at G2/M phase in a dose-dependent manner. Conclusion: Impecylone A is a novel compound from Patrinia villosa Juss and could be a potential antitumor agent especially in the cell lines of A549.

scholarly journals In vitro study on the effect of cornin on the activity of cytochrome P450 enzymes

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Qun Zhang ◽  
Zengqiang Qu ◽  
Yanqing Zhou ◽  
Jin Zhou ◽  
Junwei Yang ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interaction ◽  
Liver Microsomes ◽  
In Vitro Study ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Cytochrome P450 Enzymes ◽  
Drug Drug Interaction ◽  
Dose Dependent

Abstract Background Cornin is a commonly used herb in cardiology for its cardioprotective effect. The effect of herbs on the activity of cytochrome P450 enzymes (CYP450s) can induce adverse drug-drug interaction even treatment failure. Therefore, it is necessary to investigate the effect of cornin on the activity of CYP450s, which can provide more guidance for the clinical application of cornin. Methods Cornin (100 μM) was incubated with eight isoforms of CYP450s, including CYP1A2, 2A6, 3A4, 2C8, 2C9, 2C19, 2D6, and 2E1, in pooled human liver microsomes. The inhibition model and corresponding parameters were also investigated. Results Cornin exerted significant inhibitory effect on the activity of CYP3A4, 2C9, and 2E1 in a dose-dependent manner with the IC50 values of 9.20, 22.91, and 14.28 μM, respectively (p < 0.05). Cornin inhibited the activity of CYP3A4 non-competitively with the Ki value of 4.69 μM, while the inhibition of CYP2C9 and 2E1 by cornin was competitive with the Ki value of 11.31 and 6.54 μM, respectively. Additionally, the inhibition of CYP3A4 by cornin was found to be time-dependent with the KI/Kinact value of 6.40/0.055 min− 1·μM− 1. Conclusions The inhibitory effect of cornin on the activity of CYP3A4, 2C9, and 2E1 indicated the potential drug-drug interaction between cornin and drugs metabolized by these CYP450s, which needs further investigation and validation.

Differential Analysis of 2D NMR Spectra: New Natural Products from a Pilot-Scale Fungal Extract Library

2007 ◽  
Vol 46 (6) ◽  
pp. 901-904 ◽  
Author(s):  
Frank C. Schroeder ◽  
Donna M. Gibson ◽  
Alice C. L. Churchill ◽  
Punchapat Sojikul ◽  
Eric J. Wursthorn ◽  
...  
Keyword(s):  
Natural Products ◽  
Nmr Spectra ◽  
2D Nmr ◽  
Pilot Scale ◽  
Differential Analysis ◽  
Fungal Extract ◽  
2D Nmr Spectra

Immunomodulatory activities of whey fractions in efferent prefemoral lymph of sheep

1996 ◽  
Vol 63 (2) ◽  
pp. 257-267 ◽  
Author(s):  
Chun W. Wong ◽  
Geoffrey O. Regester ◽  
Geoffrey L. Francis ◽  
Dennis L. Watson
Keyword(s):  
Immune Responses ◽  
Bovine Milk ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Milk Whey ◽  
Significant Difference ◽  
Lymphocyte Phenotypes ◽  
Dose Dependent

SummaryStudies on the immunomodulatory activities of ruminant milk and colostral whey fractions were undertaken. By comparing with boiled colostral whey in a preliminary experiment, a putative heat-labile immunostimulatory factor for antibody responses was found to be present in ovine colostral whey. Studies were then undertaken in sheep in which the efferent prefemoral lymphatic ducts were cannulated bilaterally, and immune responses in the node were measured following subcutaneous injection in the flank fold of whey protein preparations of various purities. A significant sustained decline of efferent lymphocyte output was observed following injection with autologous crude milk whey or colostral whey preparations, but no changes were observed in interferon-gamma levels in lymph plasma. Two bovine milk whey fractions (lactoperoxidase and lactoferrin) of high purity were compared in bilaterally cannulated sheep. A transient decline over the first 6 h was seen in the efferent lymphocyte output and lymph flow rate after injection of both fractions. A significant difference was seen between the two fractions in interferongamma levels in lymph at 6 h after injection. However, no significant changes in the proportion of the various efferent lymphocyte phenotypes were seen following either treatment. Whereas both fractions showed a significant inhibitory effect in a dose-dependent manner on the proliferative response of T lymphocytes, but not B lymphocytes, to mitogenic stimulation in vitro, no similar changes were seen following in vivo stimulation with these two fractions.

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