scholarly journals New Unsaturated Lactones and a Meroterpenoid from Ganoderma lucidum

2019 ◽  
Vol 14 (7) ◽  
pp. 1934578X1985881
Author(s):  
Qi-Hang Xin ◽  
Qi Luo ◽  
Ze-Hong Wu ◽  
Jiao-Jiao Zhang ◽  
Li-Zhong Liu ◽  
...  
Keyword(s):  
Ganoderma Lucidum ◽  
Spectroscopic Data ◽  
Specific Rotation ◽  
Positive Control ◽  
Fruiting Bodies ◽  
Chemical Structures ◽  
Inhibitory Activities ◽  
Unsaturated Lactones

From the dried fruiting bodies of Ganoderma lucidum, 2 new unsaturated lactones, dayaolingzhilactones A and B (1 and 2), and 1 new meroterpenoid, dayaolingzhiol H (3), together with 10 known compounds (4-13), were isolated. Their chemical structures were identified by using spectroscopic data and calculated specific rotation. The inhibitory activities of compounds 1 and 2 toward acetylcholinesterase (AchE) were assessed in vitro with tacrine as the positive control. Both of them exhibited moderate AchE inhibitory activities at the concentration of 50 μM.

scholarly journals Lanostane-type Triterpenoids from Ganoderma lucidum and G. multipileum Fruiting Bodies

2018 ◽  
Vol 13 (11) ◽  
pp. 1934578X1801301
Author(s):  
Pham Thanh Binh ◽  
Nguyen Phuong Thao ◽  
Nguyen Thi Luyen ◽  
Duong Thu Trang ◽  
Phung Thi Xuan Binh ◽  
...  
Keyword(s):  
Ganoderma Lucidum ◽  
Spectroscopic Data ◽  
Fruiting Bodies

Sixteen lanostane-type triterpeneoids were isolated from the fruiting bodies of wild Ganoderma lucidum and G. multipileum. The new structures 3 S,24 S,25,26-tetrahydroxy-5α-lanost-8-en-11-one (1) and ganodermanondiol 24,25-acetonide (10) were elucidated by means of spectroscopic data and Mosher's experiments. Lanosta-7,9(11)-dien-3β-ol (9) strongly inhibited α-glucosidase with the IC50 values of 198.8 μM in compared with acarbose (IC50 712.4 μM).

scholarly journals In Vitro Selective Growth-Inhibitory Activities of Phytochemicals, Synthetic Phytochemical Analogs, and Antibiotics against Diarrheagenic/Probiotic Bacteria and Cancer/Normal Intestinal Cells

2020 ◽  
Vol 13 (9) ◽  
pp. 233
Author(s):  
Tomas Kudera ◽  
Ivo Doskocil ◽  
Hana Salmonova ◽  
Miloslav Petrtyl ◽  
Eva Skrivanova ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Selective Growth ◽  
Intestinal Cancer ◽  
Zinc Pyrithione ◽  
Chemical Structures ◽  
Growth Inhibitory ◽  
Increased Risk ◽  
Broth Microdilution Method ◽  
Inhibitory Activities

A desirable attribute of novel antimicrobial agents for bacterial diarrhea is decreased toxicity toward host intestinal microbiota. In addition, gut dysbiosis is associated with an increased risk of developing intestinal cancer. In this study, the selective growth-inhibitory activities of ten phytochemicals and their synthetic analogs (berberine, bismuth subsalicylate, ferron, 8-hydroxyquinoline, chloroxine, nitroxoline, salicylic acid, sanguinarine, tannic acid, and zinc pyrithione), as well as those of six commercial antibiotics (ceftriaxone, ciprofloxacin, chloramphenicol, metronidazole, tetracycline, and vancomycin) against 21 intestinal pathogenic/probiotic (e.g., Salmonella spp. and bifidobacteria) bacterial strains and three intestinal cancer/normal (Caco-2, HT29, and FHs 74 Int) cell lines were examined in vitro using the broth microdilution method and thiazolyl blue tetrazolium bromide assay. Chloroxine, ciprofloxacin, nitroxoline, tetracycline, and zinc pyrithione exhibited the most potent selective growth-inhibitory activity against pathogens, whereas 8-hydroxyquinoline, chloroxine, nitroxoline, sanguinarine, and zinc pyrithione exhibited the highest cytotoxic activity against cancer cells. None of the tested antibiotics were cytotoxic to normal cells, whereas 8-hydroxyquinoline and sanguinarine exhibited selective antiproliferative activity against cancer cells. These findings indicate that 8-hydroxyquinoline alkaloids and metal-pyridine derivative complexes are chemical structures derived from plants with potential bioactive properties in terms of selective antibacterial and anticancer activities against diarrheagenic bacteria and intestinal cancer cells.

Synthesis and antiproliferative activity of novel 4-azasteroidal-17-hydrazone derivatives

2019 ◽  
Vol 43 (3-4) ◽  
pp. 130-134
Author(s):  
Shao-Rui Chen ◽  
Hao Wu ◽  
Hai-Yan Zhao ◽  
Yu-Mei Zhang ◽  
Peng-Qi Li ◽  
...  
Keyword(s):  
Cell Line ◽  
Antiproliferative Activity ◽  
Normal Cell ◽  
Spectroscopic Data ◽  
Human Lung ◽  
Positive Control ◽  
Mucosal Cell ◽  
Human Gastric Adenocarcinoma ◽  
Normal Human

A new series of 4-azasteroidal-17-hydrazone derivatives have been synthesized from androstenedione. Their structures were characterized by analysis and spectroscopic data. The antiproliferative activity of synthesized compounds against three cancer cells (human lung adenocarcinoma, human oesophageal cervical cancer, human gastric adenocarcinoma) and a normal cell line (human gastric mucosal) was investigated. The studies show that the compound bearing a naphthyl group displayed the same antiproliferative activity in vitro against tested cells as cis-platin did (a positive control). Most of the compounds show very weak toxicity towards normal human gastric mucosal cell line.

scholarly journals Comparative Study of Synthesis, Structural and Antioxidant Activity In Vitro of Some New Carboxylic α,α-diaminodiesters Derivatives

2021 ◽  
Vol 2 (3) ◽  
pp. 6-13
Author(s):  
Oumaima Karai ◽  
Sara Hajib ◽  
Serigne Abdou Khadir Fall ◽  
Salaheddine Boukhssas ◽  
Khadim Dioukhane ◽  
...  
Keyword(s):  
Radical Scavenging ◽  
Reducing Power ◽  
2D Nmr ◽  
Positive Control ◽  
Alkylation Reaction ◽  
X Ray Diffraction ◽  
2D Nmr Spectroscopy ◽  
Antioxidant Power ◽  
Chemical Structures

Considering the richness of heterocyclic chemistry, and the diversity of applications it possesses, in the present work we were interested in preparing new polyfunctional α,α-diaminodiesters derived from glycine, via the N-alkylation reaction of methyl 2-azido-2-benzamidoacetate with a series of heterocyclic and non-heterocyclic carboxylic aminoesters, using different bases. The structures of the synthesized molecules were characterized by 1D and 2D NMR spectroscopy, mass spectrometry (MS-ESI) and elemental analysis. Two compounds from this series were isolated as single crystals and their chemical structures were determined by X-ray diffraction. The antioxidant effect of the synthesized compounds was tested in vitro using the free radical scavenging power (DPPH) and reducing power (FRAP) tests. The results show that the different extracts tested have a relatively high antioxidant power compared to the positive control considered, especially for the compound methyl 2-benzamido-2-(2-methoxy-2-oxo-1-phenylethyl)amino)acetate, which showed a very strong antiradical power and reducing power.

Bioactivity of Flavonoids Isolated from Lychnophora markgravii against Leishmania amazonensis Amastigotes

2009 ◽  
Vol 64 (7-8) ◽  
pp. 509-512 ◽  
Author(s):  
Marcos José Salvador ◽  
Fabiana Terezinha Sartori ◽  
Ana Claudia B. C. Sacilotto ◽  
Elizabeth M. F. Pral ◽  
Silvia Celina Alfieri ◽  
...  
Keyword(s):  
Methyl Ether ◽  
Spectroscopic Data ◽  
Leishmania Amazonensis ◽  
Active Compounds ◽  
Esi Ms ◽  
Chemical Structures ◽  
Chromatographic Techniques ◽  
Aerial Parts ◽  
Leishmania Amastigotes

The bioactivity of the flavonoids pinostrobin (1), pinocembrin (2), tectochrysin (3), galangin 3-methyl ether (4), and tiliroside (5) isolated from Lychnophora markgravii aerial parts was investigated in vitro against amastigote stages of Leishmania amazonensis. The compounds were isolated by several chromatographic techniques and their chemical structures were established by ESI-MS and NMR spectroscopic data. The flavonoids 1 and 3 were the most active compounds; they markedly reduced the viability of Leishmania amastigotes.

scholarly journals Anti-Inflammatory, Antiallergic, and COVID-19 Main Protease (Mpro) Inhibitory Activities of Butenolides from a Marine-Derived Fungus Aspergillus terreus

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3354
Author(s):  
Ibrahim Seyda Uras ◽  
Sherif S. Ebada ◽  
Michal Korinek ◽  
Amgad Albohy ◽  
Basma S. Abdulrazik ◽  
...  
Keyword(s):  
Aspergillus Terreus ◽  
2D Nmr ◽  
World Health ◽  
Chemical Structures ◽  
Main Protease ◽  
The World ◽  
Inhibitory Activities ◽  
Anti Inflammatory ◽  
Health Organization

In December 2020, the U.K. authorities reported to the World Health Organization (WHO) that a new COVID-19 variant, considered to be a variant under investigation from December 2020 (VUI-202012/01), was identified through viral genomic sequencing. Although several other mutants were previously reported, VUI-202012/01 proved to be about 70% more transmissible. Hence, the usefulness and effectiveness of the newly U.S. Food and Drug Administration (FDA)-approved COVID-19 vaccines against these new variants are doubtfully questioned. As a result of these unexpected mutants from COVID-19 and due to lack of time, much research interest is directed toward assessing secondary metabolites as potential candidates for developing lead pharmaceuticals. In this study, a marine-derived fungus Aspergillus terreus was investigated, affording two butenolide derivatives, butyrolactones I (1) and III (2), a meroterpenoid, terretonin (3), and 4-hydroxy-3-(3-methylbut-2-enyl)benzaldehyde (4). Chemical structures were unambiguously determined based on mass spectrometry and extensive 1D/2D NMR analyses experiments. Compounds (1–4) were assessed for their in vitro anti-inflammatory, antiallergic, and in silico COVID-19 main protease (Mpro) and elastase inhibitory activities. Among the tested compounds, only 1 revealed significant activities comparable to or even more potent than respective standard drugs, which makes butyrolactone I (1) a potential lead entity for developing a new remedy to treat and/or control the currently devastating and deadly effects of COVID-19 pandemic and elastase-related inflammatory complications.

scholarly journals Macrostachyols A-D, oligostilbenes from Gnetum macrostachyum inhibited in vitro human platelet aggregation

2021 ◽  
Vol 10 (3) ◽  
pp. 339-343
Author(s):  
Serm Surapinit ◽  
Nuttakorn Baisaeng
Keyword(s):  
Platelet Aggregation ◽  
Human Platelet ◽  
Adenosine Diphosphate ◽  
Positive Control ◽  
Inhibitory Effects ◽  
Aggregation Assay ◽  
Human Platelet Aggregation ◽  
Platelet Aggregation Assay ◽  
Inhibitory Activities

Introduction: Gnetum macrostachyum is a known Thai medicinal plant as a source of bioactive oligostilbenes, which possess platelet inhibitory activities. The study aimed to evaluate the in vitro human platelet aggregation inhibitory activities of macrostachyols A-D (compounds 1-4) isolated from the roots of G. macrostachyum. Methods: The in vitro human platelet aggregation assay was assayed with a 96-well microtiter plate format. The well-known aggregating agents were used to investigate the possible mechanism of inhibition, including adenosine diphosphate (ADP), arachidonic acid (AA), thromboxane A2 analog (U-46619), collagen, thrombin, and thrombin receptor-activating peptide-6 (TRAP-6). Results: Compound 1 was more potent than ibuprofen (positive control) on the adenosine diphosphate- induced platelet aggregation assay (P < 0.05). Compound 3 was more potent than 1, 2, and 4 (P < 0.05), but all active oligostilbenes were less potent than the positive control (P < 0.05) on the arachidonic acid-induced platelet aggregation assay. The oligostilbenes 1, 2, 3, and 4 also displayed the inhibitory effects on the U-46619-induced platelet aggregation. The tetrameric stilbenes 1 was the only compound that exhibited inhibitory effects on thrombin-induced platelet aggregation without TRAP-6 mediated platelet aggregation. Conclusion: The findings revealed the inhibitory effects of oligostilbenes on human platelet aggregation through a target-specific experimental design. It suggests that oligostilbenes from this plant might be applied as antiplatelet aggregation agents in platelet hyperreactivity- related diseases.

scholarly journals Bioactive Compounds from an Endophytic Fungi Nigrospora Aurantiaca

2021 ◽  
Author(s):  
Safwan Safwan ◽  
George Hsiao ◽  
Tzong-Huei Lee ◽  
Ching-Kuo Lee
Keyword(s):  
Bioactive Compounds ◽  
Endophytic Fungi ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Biological Activities ◽  
Fungal Strain ◽  
No Production ◽  
Chemical Structures ◽  
Inhibitory Activities ◽  
Melaleuca Leucadendra

Abstract Background: Many groups of fungi live as an endophyte in plants . Endophytic fungi could produce the bioactive compounds which was new or know compounds. Various biological activities of bioactive compounds from endophytic fungi had been reported, including anti-inflammatory and anticancer. Chemical investigation and biological activities of bioactive compounds from endophytic fungi from Melaleuca leucadendra Linn. have not yet been reportedResults: One new compound, namely nigaurdiol (1), together with five known compounds, xyloketal K (2), bostrycin (3), deoxybostrycin (4), xylanthraquinone (5), and ergosterol (6), were isolated from the Melaleuca leucadendra Linn. associated fungal strain Nigrospora aurantiaca #TMU062. Their chemical structures were elucidated by spectroscopic data and compared with literatures. All isolated compounds were evaluated for NO production inhibitory activity in LPS-activated microglial BV-2 cells. Conclusions: Compound 6 exhibited markedly inhibitory activities on NO production with IC50 values of 7.2 ± 1.4 µM and the survival of the cells was 90.8 ± 6.7% at the concentration of 10 µM.

scholarly journals Anti-trypanosomal, antioxidant and antimicrobial activities of the fruiting bodies of Ganoderma lucidum (W. Curt.: Fr) (Ganodermataceae) aqueous extract

2021 ◽  
Vol 18 (3) ◽  
pp. 172-181
Author(s):  
Samuel Otokpa Ede ◽  
John Chinyere Aguiyi ◽  
Simeon Omale ◽  
Rebecca Folashade Ede
Keyword(s):  
Aqueous Extract ◽  
Ganoderma Lucidum ◽  
Opportunistic Infections ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Antimicrobial Activities ◽  
Fruiting Bodies ◽  
Antioxidant And Antimicrobial Activities

Human African Trypanosomiasis (HAT) infection is caused by sub species of Trypanosoma brucei. The clinically licensed drugs have unacceptable toxicities and variable efficacies. The prognosis is influenced by the level of circulating free radicals and opportunistic infections. Many plants have been screened for activity in different models of HAT but the same is not true of mushrooms. This study screened the aqueous extract of the fruiting bodies of Ganoderma lucidum for trypanocidal, antioxidant and antimicrobial activities. Fruiting bodies of the mushroom were extracted sequentially with n – hexane, ethyl acetate, absolute ethanol and distilled water. The extracts were screened for phytochemical constituents and in vitro trypanocidal activity, the most active of which was further subjected to in vivo trypanocidal, anti-oxidant and anti-microbial screening. Alkaloids, carbohydrates, flavonoids, saponins and anthraquinones were present. In vitro trypanocidal screening showed the aqueous extract as the most active (IC50 = 14.65 μg/μl). It also dose-dependently inhibited parasitaemia and prolonged survival in parasite - infected mice (50, 100, 200 and 400 mg/kg). DPPH radical scavenging activity gave an IC50 of 131.00 ± 0.03 mg/ml. The extract demonstrated broad spectrum antimicrobial activity at 250 mg/ml. The fruiting bodies of G. lucidum is a potential source of trypanocidal compounds.

scholarly journals Charantoside L, A New Cucurbitane-Type Glycoside from Momordica charantia L. with α-Glucosidase Inhibitory Activities

2022 ◽  
Vol 17 (1) ◽  
pp. 1934578X2110689
Author(s):  
Duong Thi Hai Yen ◽  
Pham Hai Yen ◽  
Nguyen Quang Hop ◽  
Nguyen Anh Hung ◽  
Ha Thi Thu Tran ◽  
...  
Keyword(s):  
Ethanol Extract ◽  
2D Nmr ◽  
Positive Control ◽  
Momordica Charantia ◽  
Spectroscopic Methods ◽  
Inhibitory Effects ◽  
Chemical Structures ◽  
Glucosidase Activity ◽  
Inhibitory Activities ◽  
Reported Data

A new cucurbitane-type glycoside (1) and two known compounds (2-3) were isolated from the ethanol extract of the fruits of Momordica charantia L. Their chemical structures were determined as (19 S,23 E)-5 β­,19-epoxy-19-methoxycucurbita-6,23-diene-3 β,25-diol 3 -O-β-D-allopyranoside (1), goyaglycoside d (2), and (19 S,23 E)-5 β,19-epoxy-19-methoxycucurbita-6,23-diene-3 β,25-diol (3) on the basis of the extensive spectroscopic methods, including 1D, 2D NMR, HRESIMS, and in comparison with the reported data. Compounds 1 to 3 were evaluated for α-glucosidase inhibitory effects. Compounds 1 and 2 showed anti α-glucosidase activity with IC50 values of 134.12 ± 11.20 and 163.17 ± 13.71 µM, respectively, compared with the positive control, acarbose, IC50 160.99 ± 14.30 μM. Compounds 2 and 3 were first isolated from plant M. charantia growing in Vietnam.

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