scholarly journals New 18(4→3)-Abeo-Abietanoids from Tripterygium wilfordii

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2467
Author(s):  
Lin Ni ◽  
Ying-da Zang ◽  
Jing-zhi Yang ◽  
Chuang-jun Li ◽  
Jie Ma ◽  
...  
Keyword(s):  
Spectroscopic Analysis ◽  
Crystallographic Analysis ◽  
No Production ◽  
Anomalous Scattering ◽  
Tripterygium Wilfordii ◽  
Raw 264.7 Macrophages ◽  
X Ray ◽  
Inhibitory Activities ◽  
New Compounds

Three 18(4→3)-abeo-abietanoids, a new natural product and two new compounds, named tripordolides A–C (1–3), were isolated from the leaves of Tripterygium wilfordii. Their structures were elucidated on the basis of their spectroscopic analysis, and the absolute configuration of compounds was confirmed by CD and X-ray crystallographic analysis using anomalous scattering of Cu Kα radiation. Compounds 1 and 3 showed moderate inhibitory activities against NO production in lipopolysaccharide-induced (LPS) RAW 264.7 macrophages in vitro.

scholarly journals Crassifolins Q−W: Clerodane Diterpenoids From Croton crassifolius With Anti-Inflammatory and Anti-Angiogenesis Activities

2021 ◽  
Vol 9 ◽  
Author(s):  
Canjie Li ◽  
Xin Sun ◽  
Wenjing Yin ◽  
Zhaochun Zhan ◽  
Qing Tang ◽  
...  
Keyword(s):  
Spectroscopic Analysis ◽  
Umbilical Vein ◽  
Raw 264.7 ◽  
Significant Activity ◽  
Raw 264.7 Macrophages ◽  
X Ray ◽  
X Ray Crystallography ◽  
Clerodane Diterpenoids ◽  
Umbilical Vein Endothelial Cells

Seven new clerodane diterpenoids, crassifolins Q−W (1–7), along with five known analogues (8–12), were isolated from the roots of Croton crassifolius. Their structures were identified by comprehensive spectroscopic analysis (UV, IR, NMR, and HR-ESI-MS), and their absolute configurations were determined by ECD spectra and X-ray crystallography. The activities of compounds 1–5 against inflammatory cytokines IL-6 and TNF-α levels on LPS-induced RAW 264.7 macrophages were assessed, and compound 5 showed the most significant activity with the secretion levels of IL-6 and TNF-α at 32.78 and 12.53%, respectively. Moreover, compounds 1–5 were screened for their anti-angiogenesis using a human umbilical vein endothelial cells in vitro mode; the results showed all of them exhibited obvious anti-angiogenesis activities, in particular, compound 5 showed the strongest anti-angiogenesis effect in the range of 6.25–50 μM.

scholarly journals Synthesis of New Triarylpyrazole Derivatives Possessing Terminal Sulfonamide Moiety and Their Inhibitory Effects on PGE2 and Nitric Oxide Productions in Lipopolysaccharide-Induced RAW 264.7 Macrophages

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2556 ◽  
Author(s):  
Mohammed S. Abdel-Maksoud ◽  
Mohammed I. El-Gamal ◽  
Mahmoud M. Gamal El-Din ◽  
Yunji Choi ◽  
Jungseung Choi ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Pyrazole Ring ◽  
Inhibitory Effect ◽  
No Production ◽  
Raw 264.7 ◽  
Design Synthesis ◽  
Raw 264.7 Macrophages ◽  
New Compounds ◽  
Oxide Synthase

This article describes the design, synthesis, and in vitro anti-inflammatory screening of new triarylpyrazole derivatives. A total of 34 new compounds were synthesized containing a terminal arylsulfonamide moiety and a different linker between the sulfonamide and pyridine ring at position 4 of the pyrazole ring. All the target compounds were tested for both cytotoxicity and nitric oxide (NO) production inhibition in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages. Compounds 1b, 1d, 1g, 2a, and 2c showed the highest NO inhibition percentages and the lowest cytotoxic effect. The most potent derivatives were tested for their ability to inhibit prostaglandin E2 (PGE2) in LPS-induced RAW 264.7 macrophages. The IC50 for nitric oxide inhibition, PGE2 inhibition, and cell viability were determined. In addition, 1b, 1d, 1g, 2a, and 2c were tested for their inhibitory effect on LPS-induced inducible nitric oxide synthase (iNOS) and Cyclooxygenase 2 (COX-2) protein expression as well as iNOS enzymatic activity.

scholarly journals Diketopiperazine and Diphenylether Derivatives from Marine Algae-Derived Aspergillus versicolor OUCMDZ-2738 by Epigenetic Activation

Marine Drugs ◽  
2018 ◽  
Vol 17 (1) ◽  
pp. 6 ◽  
Author(s):  
Wen Liu ◽  
Liping Wang ◽  
Bin Wang ◽  
Yanchao Xu ◽  
Guoliang Zhu ◽  
...  
Keyword(s):  
Spectroscopic Analysis ◽  
Specific Rotation ◽  
Crystallographic Analysis ◽  
Aspergillus Versicolor ◽  
X Ray ◽  
Naturally Occurring ◽  
Ic50 Values ◽  
New Compounds ◽  
First Time ◽  
Optically Pure

A chemical-epigenetic method was used to enhance the chemodiversity of a marine algicolous fungus. Apart from thirteen known compounds, (+)-brevianamide R ((+)-3), (‒)-brevianamide R ((‒)-3), (+)-brevianamide Q ((+)-4), (‒)-brevianamide Q ((‒)-4), brevianamide V ((+)-5), brevianamide W ((‒)-5), brevianamide K (6), diorcinol B (7), diorcinol C (8), diorcinol E (9), diorcinol J (10), diorcinol (11), 4-methoxycarbonyldiorcinol (12), two new compounds, (+)- and (‒)-brevianamide X ((+)- and (‒)- 2)), as well as a new naturally occurring one, 3-[6-(2-methylpropyl)-2-oxo-1H-pyrazin-3-yl]propanamide (1), were isolated from chemical-epigenetic cultures of Aspergillus versicolor OUCMDZ-2738 with 10 µM vorinostat (SAHA). Compared to cultures in the same medium without SAHA, compounds 1–4, 8, 9, 11, and 12 were solely observed under SAHA condition. The structures of these compounds were elucidated based on spectroscopic analysis, specific rotation analysis, ECD, and X-ray crystallographic analysis. (±)-3, (±)-4, and (±)-5 were further resolved into the corresponding optically pure enantiomers and their absolute configurations were determined for the first time. Compounds 11 and 12 showed selective antibacterial against Pseudomonas aeruginosa with a minimum inhibitory concentration (MIC) of 17.4 and 13.9 μM, respectively. Compound 10 exhibited better α-glucosidase inhibitory activity than the assay control acarbose with IC50 values of 117.3 and 255.3 μM, respectively.

scholarly journals Three New Compounds from the Actinomycete Actinocorallia aurantiaca

2019 ◽  
Vol 9 (5) ◽  
pp. 351-354 ◽  
Author(s):  
Kai-Yue Han ◽  
Xing Wu ◽  
Chenglin Jiang ◽  
Rong Huang ◽  
Zheng-Hui Li ◽  
...  
Keyword(s):  
Influenza A ◽  
Sika Deer ◽  
Spectroscopic Analysis ◽  
2D Nmr ◽  
No Production ◽  
Raw 264.7 ◽  
Spectroscopic Methods ◽  
Raw 264.7 Macrophages ◽  
Optical Rotations ◽  
New Compounds

Abstract Aurantiadioic acids A (1) and B (2), two new furan-containing polyketides, and aurantoic acid A (3), a new natural product, were isolated from the liquid fermentation of the sika deer dung-derived actinomycete Actinocorallia aurantiaca. The structures of the new compounds were established by extensive spectroscopic methods, including 1D & 2D NMR, HRESIMS spectroscopic analysis. The absolute configuration of 3 was assigned by comparison of the specific optical rotations with the reported derivatives. Biological activity evaluations suggested that compounds 1–3 showed weak inhibition on NO production in the murine monocytic RAW 264.7 macrophages with IC50 values of 35.8, 41.8, 45.2 μM, respectively. Compound 3 showed weak inhibition on influenza A virus (A/PuertoRico/8/1934, H1N1) with an EC50 value of 35.9 μM, and a selective index higher than 13.3.

scholarly journals Sacraoxides A–G, Bioactive Cembranoids from Gum Resin of Boswellia sacra

2021 ◽  
Vol 9 ◽  
Author(s):  
Bingyang Zhang ◽  
Di Liu ◽  
Wenyue Ji ◽  
Kouharu Otsuki ◽  
Koji Higai ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Spectroscopic Analysis ◽  
Raw264.7 Cells ◽  
No Production ◽  
X Ray Diffraction ◽  
X Ray ◽  
Inhibitory Activities ◽  
Modified Mosher’S Method ◽  
Boswellia Sacra

Seven undescribed cembranoids, sacraoxides A–G (1, 3–8) were isolated from the gum resin of Boswellia sacra. Their structures were elucidated by extensive physicochemical and spectroscopic analysis, as well as ECD calculation, modified Mosher’s method and X-ray diffraction crystallography. Compounds 6 and 7 exhibited inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide in RAW264.7 cells with IC50 values of 24.9 ± 1.7 and 36.4 ± 2.9 μM.

Salaterpene E, a eudesmane-type sesquiterpene from Salacia longipes var. camerunensis

2016 ◽  
Vol 71 (2) ◽  
pp. 87-93 ◽  
Author(s):  
Brice Mittérant Mba’ning ◽  
Bruno Lenta Ndjakou ◽  
Ferdinand Mouafo Talontsi ◽  
Alain Meli Lannang ◽  
Birger Dittrich ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Absolute Configuration ◽  
Previous Investigation ◽  
Spectroscopic Analysis ◽  
Inhibitory Concentration ◽  
Anomalous Scattering ◽  
X Ray Diffraction ◽  
Meoh Extract ◽  
X Ray

AbstractA mixture of two compounds with potent antiplasmodial activity in vitro against the W2 strain of Plasmodium falciparum (half maximal inhibitory concentration, 1.12 μg/mL) was obtained in a previous investigation of the CH2Cl2-MeOH extract of the seeds of Salacia longipes var. camerunensis. Separation by column chromatography led now to the isolation of salaterpene E (1) and (1R,2R,4S,5S,6R,7R,9S,10R)-2-acetoxy-1,6,9-tribenzoyloxy-4-hydroxy-dihydro-β-agarofuran (2). The structure of 1 was elucidated by spectroscopic analysis, and its absolute configuration was established unambiguously by means of single-crystal X-ray diffraction. Also the absolute configurations of the recently described salaterpenes A (2a) and D (2b) were determined by this method using the anomalous scattering of the oxygen atoms only.

scholarly journals In Vitro Modulator Effect of Total Extract from the Endophytic Paenibacillus polymyxa RNC-D in Leishmania (Leishmania) amazonensis and Macrophages

2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
Débora Meira Neris ◽  
Letícia Gonçalves Ortolani ◽  
Cynthia Aparecida de Castro ◽  
Ricardo de Oliveira Correia ◽  
Joice Margareth de Almeida Rodolpho ◽  
...  
Keyword(s):  
Paenibacillus Polymyxa ◽  
Leishmania Amazonensis ◽  
No Production ◽  
Raw 264.7 ◽  
Total Extract ◽  
Raw 264.7 Macrophages ◽  
Promising Target ◽  
Mediators Of Inflammation ◽  
Infected Cells

Leishmaniases are diseases with high epidemiological relevance and wide geographical distribution. In Brazil, Leishmania (Leishmania) amazonensis is related to the tegumentary form of leishmaniasis. The treatment for those diseases is problematic as the available drugs promote adverse effects in patients. Therefore, it is important to find new therapeutic targets. In this regard, one alternative is the study of biomolecules produced by endophytic microorganisms. In this study, the total extract produced by the endophytic Paenibacillus polymyxa RNC-D was used to evaluate the leishmanicidal, nitric oxide, and cytokines production using RAW 264.7 macrophages. The results showed that, in the leishmanicidal assay with L. amazonensis, EC50 values at the periods of 24 and 48 hours were 0.624 mg/mL and 0.547 mg/mL, respectively. Furthermore, the cells treated with the extract presented approximately 25% of infected cells with an average of 3 amastigotes/cell in the periods of 24 and 48 hours. Regarding the production of cytokines in RAW 264.7 macrophages infected/treated with the extract, a significant increase in TNF-α was observed at the periods of 24 and 48 hours in the treated cells. The concentrations of IFN-γ and IL-12 showed significant increase in 48 hours. A significant decrease in IL-4 was observed in all cells treated with the extract in 24 hours. It was observed in the treated cells that the NO production by RAW 264.7 macrophages increased between 48 and 72 hours. The endophytic Paenibacillus polymyxa RNC-D extract modulates the mediators of inflammation produced by RAW 264.7 macrophages promoting L. amazonensis death. The immunomodulatory effects might be a promising target to develop new immunotherapeutic and antileishmanial drugs.

scholarly journals Synthesis and anti-acetylcholinesterase activities of novel glycosyl coumarylthiazole derivatives

2020 ◽  
pp. 174751982094835
Author(s):  
You-Xian Wang ◽  
Shu-Hao Liu ◽  
Zhong-Bai Shao ◽  
Lian-Gong Cao ◽  
Kai-Jun Jiang ◽  
...  
Keyword(s):  
Electrospray Ionization ◽  
New Products ◽  
Reaction Conditions ◽  
Inhibitory Rate ◽  
Inhibitory Activities ◽  
Ellman’S Method ◽  
New Compounds ◽  
C Nmr

Eleven glycosyl coumarylthiazole derivatives are synthesized by cyclization and condensation of glycosyl thiourea with 3-bromoacetyl coumarins in ethanol. The reaction conditions are optimized and good yields of products (80%–95%) are obtained. The structures of all new products were confirmed by IR, 1H and 13C NMR, and by HRMS (electrospray ionization). The in vitro acetylcholinesterase (AChE) inhibitory activities of these new compounds are tested by Ellman’s method. Among them, N-(2-acetamido-3,4,6-tri- O-acetyl-2-deoxy-β-D-glucopyranosyl)-4-(6-nitrocoumarinyl)-1,3-thiazole-2-amine showed the best activity with an in vitro AChE inhibitory rate of 58% and an IC50 value of 12 ± 0.38 μg/mL.

scholarly journals Highly Substituted Benzophenone Aldehydes and Eremophilane Derivatives from the Deep-Sea Derived Fungus Phomopsis lithocarpus FS508

Marine Drugs ◽  
2018 ◽  
Vol 16 (9) ◽  
pp. 329 ◽  
Author(s):  
Jian-Lin Xu ◽  
Hong-Xin Liu ◽  
Yu-Chan Chen ◽  
Hai-Bo Tan ◽  
Heng Guo ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
A549 Cell ◽  
Marine Sediment ◽  
Deep Sea ◽  
Crystallographic Analysis ◽  
X Ray ◽  
Naturally Occurring ◽  
Ic50 Values ◽  
New Compounds

Five new benzophenone derivatives named tenellones D–H (1–5), sharing a rare naturally occurring aldehyde functionality in this family, and a new eremophilane derivative named lithocarin A (7), together with two known compounds (6 and 8), were isolated from the deep marine sediment-derived fungus Phomopsis lithocarpus FS508. All of the structures for these new compounds were fully characterized and established on the basis of extensive spectroscopic interpretation and X-ray crystallographic analysis. Compound 5 exhibited cytotoxic activity against HepG-2 and A549 cell lines with IC50 values of 16.0 and 17.6 μM, respectively.

scholarly journals New Alkaloids and Anti-inflammatory Constituents from the Leaves of Antidesma ghaesembilla

2017 ◽  
Vol 12 (1) ◽  
pp. 1934578X1701200
Author(s):  
Phan Van Kiem ◽  
Le Canh Viet Cuong ◽  
Do Thi Trang ◽  
Nguyen Xuan Nhiem ◽  
Hoang Le Tuan Anh ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Inhibitory Activity ◽  
No Production ◽  
Raw 264.7 ◽  
Chemical Methods ◽  
Raw 264.7 Macrophages ◽  
Chemical Structures ◽  
Bv2 Cells ◽  
Inhibitory Activities ◽  
Physical And Chemical

Using various chromatographic methods, two new alkaloids, antidesoic acids A (1) and B (2) along with fourteen known compounds (3-16) were isolated from the leaves of Antidesma ghaesembilla Gaertn. Their chemical structures were elucidated by physical and chemical methods. All the isolated compounds were evaluated for their inhibitory activity on LPS-stimulated nitric oxide (NO) production in BV2 cells and RAW 264.7 macrophages. Bisflavone 8 significantly inhibited LPS-stimulated NO production in BV2 cells and RAW 264.7 macrophages with IC50 values of 5.4 and 8.0 μM, respectively. Compounds 1–3, 7, 10, 12, 14, and 16 showed moderate inhibitory activities with IC50 values ranging from 11.7 to 77.4 μM.

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