scholarly journals α-Glucosidase and 15-Lipoxygenase Inhibitory Activities of Phytochemicals from Calophyllum symingtonianum

2015 ◽  
Vol 10 (9) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Nurul Iman Aminudin ◽  
Farediah Ahmad ◽  
Muhammad Taher ◽  
Razauden Mohamed Zulkifli
Keyword(s):  
Positive Result ◽  
Inhibitory Activity ◽  
Spectroscopic Analysis ◽  
Chemical Structures ◽  
Crude Extracts ◽  
Phytochemical Investigation ◽  
Lipoxygenase Inhibition ◽  
Inhibitory Activities

A phytochemical investigation of the crude extracts of the bark and leaves of Calophyllum symingtonianum has resulted in the isolation of inophyllum D, inophyllum H, calanone, isocordato-oblongic acid, amentoflavone, carpachromene and lupenone. Their chemical structures were elucidated and confirmed by spectroscopic analysis. All flavonoids and coumarins showed significant α-glucosidase inhibitory activity, while amentoflavone gave a positive result against 15-lipoxygenase inhibition.

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.

scholarly journals Phenolic compounds from the lichen Parmotrema tinctorum

2021 ◽  
Vol 24 (1) ◽  
pp. 1842-1846
Author(s):  
Huynh Bui Linh Chi ◽  
Van Muoi Bui ◽  
Thi Quynh Nhu Phan ◽  
Kim Phi Phung Nguyen
Keyword(s):  
Inhibitory Activity ◽  
Spectroscopic Analysis ◽  
Published Data ◽  
Anticancer Activities ◽  
Chemical Structures ◽  
Diphenyl Ethers ◽  
Pure Compounds ◽  
First Time ◽  
Parmotrema Tinctorum ◽  
Gyrophoric Acid

Introduction: The metabolites of lichens concentrated depsidones, depsides, and diphenyl ethers were possessed antibiotic, antifungal, antiviral, antitumor, and anticancer activities. Parmotrema tinctorum (Despr. ex Nyl.) Hale, a species of foliose lichen, is widely distributed in Lam Dong province, Vietnam. Herein, this paper describes the isolation and structure elucidation of seven compounds isolated from this lichen. Methods: Phytochemical investigations of the ethyl acetate extract of the lichen P. tinctorum led to the isolation of seven pure compounds. Their chemical structures were elucidated by extensive HR-ESI-MS and NMR spectroscopic analysis and comparison with previously published data. Results: Seven compounds, namely orcinol (1), orsellinic acid (2), methyl orsellinate (3), methyl heamatomate (4), lecanorin (5), lecanoric acid (6), and gyrophoric acid (7). These compounds were determined the α-glucosidase inhibitory activity. Conclusions: Compound 7 was determined for the first time in P. tinctorum, and this was also the first time these compounds were determined the α-glucosidase inhibitory activity.

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 Quassinoids from the Roots of Eurycoma longifolia and Their Anti-Proliferation Activities

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5939
Author(s):  
Wei-Qun Yang ◽  
Wei Tang ◽  
Xiao-Jun Huang ◽  
Jian-Guo Song ◽  
Yue-Yue Li ◽  
...  
Keyword(s):  
Spectroscopic Analysis ◽  
Hydroxyl Group ◽  
Human Leukemia ◽  
In Vitro Proliferation ◽  
X Ray ◽  
Eurycoma Longifolia ◽  
Chemical Structures ◽  
Phytochemical Investigation ◽  
Ic50 Values

A phytochemical investigation on the roots of medicinal plant Eurycoma longifolia resulted in the isolation of 10 new highly oxygenated C20 quassinoids longifolactones G‒P (1–10), along with four known ones (11–14). Their chemical structures and absolute configurations were unambiguously elucidated on the basis of comprehensive spectroscopic analysis and X-ray crystallographic data. Notably, compound 1 is a rare pentacyclic C20 quassinoid featuring a densely functionalized 2,5-dioxatricyclo[5.2.2.04,8]undecane core. Compound 4 represents the first example of quassinoids containing a 14,15-epoxy functionality, and 7 features an unusual α-oriented hydroxyl group at C-14. All isolated compounds were evaluated for their anti-proliferation activities on human leukemia cells. Among the isolates, compounds 5, 12, 13, and 14 potently inhibited the in vitro proliferation of K562 and HL-60 cells with IC50 values ranging from 2.90 to 8.20 μM.

α-Glucosidase Inhibitory Activity of the Extracts and Major Phytochemical Components of Smilax glabra Roxb

2020 ◽  
Vol 10 (1) ◽  
pp. 26-32
Author(s):  
Phuong T.M. Nguyen ◽  
Quang V. Ngo ◽  
Minh T.H. Nguyen ◽  
Alan T. Maccarone ◽  
Stephen G. Pyne
Keyword(s):  
Inhibitory Activity ◽  
In Vitro Cytotoxicity ◽  
Antidiabetic Activity ◽  
Ca 125 ◽  
Chemical Structures ◽  
Glucosidase Inhibitors ◽  
Ic50 Values ◽  
Inhibitory Activities ◽  
Phytochemical Components

Background: A therapeutic approach to treat diabetes is to decrease postprandial hyperglycemia. α-Glucosidase inhibitors from plant sources offer an attractive strategy for the control of hyperglycemia. Smilax glabra Roxb is a medicinal plant found in Asia, including Vietnam, which is used in the treatment of chronic diseases. However, the antidiabetic activity and the identification of α-glucosidase inhibitors from this plant have not been intensively investigated. This research was carried out to determine the α-glucosidase inhibitory activity of the extracts and that of the major phytochemical components of Smilax glabra Roxb. This could lead to further studies on the role of these compounds in hyperglycemia control, as well as identify their potential future applications. Methods: Column chromatography combined with crystallization procedures were used to isolate active fractions and two major compounds. The chemical structures of these compounds were determined by analysis of their NMR spectroscopic data, as well as MS data and comparisons made with the literature data. The α-glucosidase inhibitory activity was determined spectrophotometrically using p-nitrophenyl α-D-glucopyranoside as a substrate. The in vitro cytotoxicity of the isolated compounds and fractions was determined using the MTT assay. Results: The two major compounds, astilbin and 5-O-caffeoylshikimic acid together with two very active fractions, F7 and F8, were isolated from the rhizome. The two major compounds had α- glucosidase inhibitory activities with IC50 values of ca. 125 µg/mL and 38 µg/mL, respectively which are about 4 and 13 folds higher activity than the reference compound acarbose (IC50 of ca. 525 µg/mL). Fractions F7 and F8 showed very promising inhibitory activities towards α-glucosidase with IC50 values of 5.5 and 5.8 µg/mL, respectively. Cytotoxicity data on mouse fibroblast NIH3T3 cells indicated that the active compounds and fractions were not toxic at concentrations that are greater than their respective IC50 values. The α-glucosidase inhibitory activity of 5-Ocaffeoylshikimic acid and that of the two active fractions are reported here for the first time. Conclusion: The two major isolated compounds and fractions, F7 and F8, significantly contribute to the α-glucosidase inhibitory activity of S. glabra Roxb extract. Further work is needed to clarify their modes of action and potential application.

scholarly journals Five New Pregnane Glycosides from Gymnema sylvestre and Their α-Glucosidase and α-Amylase Inhibitory Activities

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2525 ◽  
Author(s):  
Phan Van Kiem ◽  
Duong Thi Hai Yen ◽  
Nguyen Van Hung ◽  
Nguyen Xuan Nhiem ◽  
Bui Huu Tai ◽  
...  
Keyword(s):  
Medicinal Plant ◽  
Traditional Medicine ◽  
Oleanolic Acid ◽  
Inhibitory Activity ◽  
Gymnema Sylvestre ◽  
Spectroscopic Evidence ◽  
Phytochemical Investigation ◽  
Ic50 Values ◽  
Treatment Of Diabetes ◽  
Inhibitory Activities

Gymnema sylvestre, a medicinal plant, has been used in Indian ayurvedic traditional medicine for the treatment of diabetes. Phytochemical investigation of Gymnema sylvestre led to the isolation of five new pregnane glycosides, gymsylosides A–E (1–5) and four known oleanane saponins, 3β-O-β-D-glucopyranosyl (1→6)-β-D-glucopyranosyl oleanolic acid 28-O-β-D-glucopyranosyl ester (6), gymnemoside-W1 (7), 3β-O-β-D-xylopyranosyl-(1→6)-β-D- glucopyranosyl-(1→6)-β-D-glucopyranosyl oleanolic acid 28-O-β-D-glucopyranosyl ester (8), and alternoside XIX (9). Their structures were identified based on spectroscopic evidence and comparison with those reported in the literature. All compounds were evaluated for their α-glucosidase and α-amylase inhibitory activities. Compounds 2–4 showed significant α-amylase inhibitory activity, with IC50 values ranging from 113.0 to 176.2 µM.

Isolation of New Glycosides from Anemarrhena Asphodeloides Rhizome and Screening of their Anticancer Activity

2019 ◽  
Vol 16 (6) ◽  
pp. 474-477 ◽  
Author(s):  
Pham Van Khang ◽  
Nguyen Thi Hien Lan ◽  
Le Quang Truong ◽  
Mai Thi Minh Chau ◽  
Mai Xuan Truong ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Spectral Data ◽  
Cell Lines ◽  
Cancer Cell ◽  
Spectroscopic Analysis ◽  
2D Nmr ◽  
Ic50 Values ◽  
Nmr Techniques ◽  
Inhibitory Activities ◽  
Anemarrhena Asphodeloides

In this report, two new steroidal glycosides were isolated and determined from n-butanol fraction of A.asphodeloides. The structures were confirmed in comparison with the spectral data of known compounds by using different spectroscopic analysis approaches including 1D & 2D-NMR techniques and HRMS. The anti-proliferation screening against cancer cell lines A549 and HeLa indicated that compound 1 exhibited good inhibitory activities with IC50 values of 0.79 and 0.55 µg/mL, respectively.

The Development of Tyrosyl-DNA Phosphodyesterase 1 (TDP1) Inhibitors Based on the Amines Combining Aromatic/Heteroaromatic and Monoterpenoid Moieties

2019 ◽  
Vol 16 (5) ◽  
pp. 597-605 ◽  
Author(s):  
Evgenii Mozhaitsev ◽  
Evgenii Suslov ◽  
Yuliya Demidova ◽  
Dina Korchagina ◽  
Konstantin Volcho ◽  
...  
Keyword(s):  
Dna Repair ◽  
Tumor Cell ◽  
13C Nmr ◽  
Inhibitory Activity ◽  
Secondary Amines ◽  
Repair Enzyme ◽  
1H And 13C Nmr ◽  
Chemical Structures ◽  
Natural Substances ◽  
Micromolar Range

Background: Inhibition of the DNA repair enzyme, tyrosyl-DNA phosphodiesterase 1 (TDP1), may increase the efficacy of cancer drugs that cause damage to tumor cell DNA. Among the known TDP1 inhibitors, there are compounds containing moieties of natural substances, e.g., monoterpenoids. In this work, we synthesized several compounds containing aromatic/ heteroaromatic amines and monoterpenoid groups and assessed their TDP1 inhibition potential. Methods: Structures of all the synthesized compounds were confirmed by 1H and 13C NMR as well as HRMS. The TDP1 inhibitory activity of the amines was determined by real-time fluorescence oligonucleotide biosensor. Results: The synthesized secondary amines had TDP1 inhibitory activity IC50 in the range of 0.79-9.2 µM. The highest activity was found for (–)-myrtenal derivatives containing p-bromoaniline or m-(trifluoromethyl)aniline residue. Conclusion: We synthesized 22 secondary amines; of these, 17 amines are novel chemical structures. Many of the amines inhibit TDP1 activity in the low micromolar range. Therefore, these compounds are promising for further study of their antiproliferative activity in conjunction with DNA damaging drugs.

scholarly journals Massiliamide, a cyclic tetrapeptide with potent tyrosinase inhibitory properties from the Gram-negative bacterium Massilia albidiflava DSM 17472T

2020 ◽  
Author(s):  
Andri Frediansyah ◽  
Jan Straetener ◽  
Heike Brötz-Oesterhelt ◽  
Harald Gross
Keyword(s):  
Absolute Configuration ◽  
Inhibitory Activity ◽  
Liquid Culture ◽  
Spectroscopic Analysis ◽  
2D Nmr ◽  
Negative Bacterium ◽  
Gram Negative ◽  
The Absolute ◽  
Potent Inhibitory Activity ◽  
Cyclic Tetrapeptide

AbstractA cyclic tetrapeptide, designated massiliamide, was isolated from the liquid culture of the Gram-negative bacterium Massilia albidiflava DSM 17472T. The structure was elucidated through extensive spectroscopic analysis, including HR-MS and 1D and 2D NMR experiments. The absolute configuration was determined using the Marfey´s method. Massiliamide showed potent inhibitory activity towards tyrosinase with an IC50 value of 1.15 µM and no cytotoxicity.

scholarly journals Highly Oxygenated Triterpenoids and Diterpenoids from Fructus Rubi (Rubus Chingii Hu) and Their NF-kappa B Inhibitory Effects

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 1911
Author(s):  
Jiang Wan ◽  
Xiao-Juan Wang ◽  
Nan Guo ◽  
Xi-Ying Wu ◽  
Juan Xiong ◽  
...  
Keyword(s):  
Inhibitory Effects ◽  
Nf Kappa B ◽  
Pentacyclic Triterpenoids ◽  
Chemical Structures ◽  
Phytochemical Investigation ◽  
Ic50 Values ◽  
Rubus Chingii ◽  
Rubus Chingii Hu ◽  
Type 3

During a phytochemical investigation of the unripe fruits of Rubus chingii Hu (i.e., Fructus Rubi, a traditional Chinese medicine named “Fu-Pen-Zi”), a number of highly oxygenated terpenoids were isolated and characterized. These included nine ursane-type (1, 2, and 4–10), five oleanane-type (3, 11–14), and six cucurbitane-type (15–20) triterpenoids, together with five ent-kaurane-type diterpenoids (21–25). Among them, (4R,5R,8R,9R,10R,14S,17S,18S,19R,20R)-2,19α,23-trihydroxy-3-oxo-urs-1,12-dien-28-oic acid (rubusacid A, 1), (2R*,4S*,5R*,8R*,9R*,10R*,14S*,17S*, 18S*,19R*,20R*)-2α,19α,24-trihydroxy-3-oxo-urs-12-en-28-oic acid (rubusacid B, 2), (5R,8R,9R,10R, 14S,17R,18S,19S)-2,19α-dihydroxy-olean-1,12-dien-28-oic acid (rubusacid C, 3), and (3S,5S,8S,9R, 10S,13R,16R)-3α,16α,17-trihydroxy-ent-kaur-2-one (rubusone, 21) were previously undescribed. Their chemical structures and absolute configurations were elucidated on the basis of spectroscopic data and electronic circular dichroism (ECD) analyses. Compounds 1 and 3 are rare naturally occurring pentacyclic triterpenoids featuring a special α,β-unsaturated keto-enol (diosphenol) unit in ring A. Cucurbitacin B (15), cucurbitacin D (16), and 3α,16α,20(R),25-tetrahydroxy-cucurbita-5,23- dien-2,11,22-trione (17) were found to have remarkable inhibitory effects against NF-κB, with IC50 values of 0.08, 0.61, and 1.60 μM, respectively.

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