scholarly journals Secondary Metabolites with α-Glucosidase Inhibitory Activity from Mangrove Endophytic Fungus Talaromyces sp. CY-3

Marine Drugs ◽  
2021 ◽  
Vol 19 (9) ◽  
pp. 492
Author(s):  
Wencong Yang ◽  
Qi Tan ◽  
Yihao Yin ◽  
Yan Chen ◽  
Yi Zhang ◽  
...  

Eight new compounds, including two sambutoxin derivatives (1–2), two highly oxygenated cyclopentenones (7–8), four highly oxygenated cyclohexenones (9–12), together with four known sambutoxin derivatives (3–6), were isolated from semimangrove endophytic fungus Talaromyces sp. CY-3, under the guidance of molecular networking. The structures of new isolates were elucidated by analysis of detailed spectroscopic data, ECD spectra, chemical hydrolysis, 13C NMR calculation, and DP4+ analysis. In bioassays, compounds 1–5 displayed better α-glucosidase inhibitory activity than the positive control 1-deoxynojirimycin (IC50 = 80.8 ± 0.3 μM), and the IC50 value was in the range of 12.6 ± 0.9 to 57.3 ± 1.3 μM.

2018 ◽  
Vol 17 (3) ◽  
pp. 134-139
Author(s):  
R.M. Perez-Gutierrez

Methanol extract from Lippia graveolens (Mexican oregano) was studied in order to identify inhibitory bioactives for protein tyrosine phosphatase 1B (PTP1B). Known flavone as lutein (1), and another flavone glycoside such as lutein-7-o-glucoside (2), 6-hydroxy-lutein-7-ohexoside (3) and lutein-7-o-ramnoide (4) were isolated from methanol extract of aerial parts of the Lippia graveolens. All isolates were identified based on extensive spectroscopic data analysis, including UV, IR, NMR, MS and compared with spectroscopic data previously reported. These flavones were evaluated for PTP1B inhibitory activity. Among them, compounds 1 and 3 displayed potential inhibitory activity against PTP1B with IC50 values of 7.01 ± 1.25 μg/ml and 18.4 μg/ml, respectively. In addition, compound 2 and 4 showed moderate inhibitory activity with an IC50 value of 23.8 ± 6.21 and 67.8 ± 5.80 μg/ml respectively. Among the four compounds, luteolin was found to be the most potent PTP1B inhibitor compared to the positive control ursolic acid, with an IC50 value of 8.12 ± 1.06 μg/ml. These results indicate that flavonoids constituents contained in Lippia graveolens can be considered as a natural source for the treatment of type 2 diabetes.


Marine Drugs ◽  
2021 ◽  
Vol 19 (4) ◽  
pp. 224
Author(s):  
Cui-Ping Xing ◽  
Dan Chen ◽  
Chun-Lan Xie ◽  
Qingmei Liu ◽  
Tian-Hua Zhong ◽  
...  

Ten new (1–10) and 26 known (11–36) compounds were isolated from Penicillium griseofulvum MCCC 3A00225, a deep sea-derived fungus. The structures of the new compounds were determined by detailed analysis of the NMR and HRESIMS spectroscopic data. The absolute configurations were established by X-ray crystallography, Marfey’s method, and the ICD method. All isolates were tested for in vitro anti-food allergic bioactivities in immunoglobulin (Ig) E-mediated rat basophilic leukemia (RBL)-2H3 cells. Compound 13 significantly decreased the degranulation release with an IC50 value of 60.3 μM, compared to that of 91.6 μM of the positive control, loratadine.


Plants ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 385
Author(s):  
May Thazin Thant ◽  
Boonchoo Sritularak ◽  
Nutputsorn Chatsumpun ◽  
Wanwimon Mekboonsonglarp ◽  
Yanyong Punpreuk ◽  
...  

A phytochemical investigation on the whole plants of Aerides multiflora revealed the presence of three new biphenanthrene derivatives named aerimultins A–C (1–3) and a new natural phenylpropanoid ester dihydrosinapyl dihydroferulate (4), together with six known compounds (5–10). The structures of the new compounds were elucidated by analysis of their spectroscopic data. All of the isolates were evaluated for their α-glucosidase inhibitory activity. Aerimultin C (3) showed the most potent activity. The other compounds, except for compound 4, also exhibited stronger activity than the positive control acarbose. Compound 3 showed non-competitive inhibition of the enzyme as determined from a Lineweaver–Burk plot. This study is the first phytochemical and biological investigation of A. multiflora.


Marine Drugs ◽  
2021 ◽  
Vol 20 (1) ◽  
pp. 5
Author(s):  
Xiaoya Qin ◽  
Jiguo Huang ◽  
Dexiong Zhou ◽  
Wenxiu Zhang ◽  
Yanjun Zhang ◽  
...  

Four undescribed compounds, guhypoxylonols A (1), B (2), C (3), and D (4), were isolated from the mangrove endophytic fungus Aspergillus sp. GXNU-Y45, together with seven previously reported metabolites. The structures of 1–4 were elucidated based on analysis of HRESIMS and NMR spectroscopic data. The absolute configurations of the stereogenic carbons in 1–3 were established through a combination of spectroscopic data and electronic circular dichroism (ECD). Compounds 1–11 were evaluated for their anti-inflammatory activity. Compounds 1, 3, 4, and 6 showed an inhibitory activity against the production of nitric oxide (NO), with the IC50 values of 14.42 ± 0.11, 18.03 ± 0.14, 16.66 ± 0.21, and 21.05 ± 0.13 μM, respectively.


2021 ◽  
Vol 63 (4) ◽  
pp. 42-46
Author(s):  
Thi-My-Linh Lam ◽  
◽  
Minh-Tuan Le ◽  
Manh-Ha Bui ◽  
◽  
...  

A study on the α-glucosidase inhibitory activity of 40 kinds of vegetables, tubers, and fruits found in the An Giang province was conducted. The results indicated that all 40 extracted samples displayed α-glucosidase inhibitory activity at a concentration of 250 μg ml-1, 36 extracted samples showed an inhibition rate greater than 50% at 250 μg ml-1, 25 extracted samples had over 50% at 100 μg ml-1, 17 extracted samples possessed more than 50% at 50 μg ml-1, 7 extracted samples sampled showed over 50% at 25 μg ml-1, 5 extracted samples were greater than 50% at 10 μg ml-1, and 1 extracted sample was greater than 50% at 1 μg ml-1. Among the 40 samples, those taken from the seeds of Areca catechu, the fruits of Cassia grandis, the fruits of Syzygium cumini, the seeds of Glycine max,andthe stems of Enydra fluctuansexhibited the strongest α-glucosidase inhibitory activity in methanol, with IC50 values of 0.15, 2.54, 4.05, 5.17 and 8.68 μg ml-1, respectively, which were stronger than the positive control acarbose with an IC50 value of 214.5 μg ml-1


Marine Drugs ◽  
2020 ◽  
Vol 18 (3) ◽  
pp. 164 ◽  
Author(s):  
Zhongbin Cheng ◽  
Wan Liu ◽  
Runzhu Fan ◽  
Shouye Han ◽  
Yuanli Li ◽  
...  

A chemical study of the ethyl acetate (EtOAc) extract from the deep-sea-derived fungus Penicillium thomii YPGA3 led to the isolation of a new austalide meroterpenoid (1) and seven known analogues (2−8), two new labdane-type diterpenoids (9 and 10) and a known derivative (11). The structures of new compounds 1, 9, and 10 were determined by comprehensive analyses via nuclear magnetic resonance (NMR) and mass spectroscopy (MS) data. The absolute configurations of 1, 9, and 10 were determined by comparisons of experimental electronic circular dichroism (ECD) with the calculated ECD spectra. Compound 1 represented the third example of austalides bearing a hydroxyl group at C-5 instead of the conserved methoxy in other known analogues. To our knowledge, diterpenoids belonging to the labdane-type were discovered from species of Penicillium for the first time. Compound 1 showed cytotoxicity toward MDA-MB-468 cells with an IC50 value of 38.9 μM. Compounds 2 and 11 exhibited inhibition against α-glucosidase with IC50 values of 910 and 525 μM, respectively, being more active than the positive control acarbose (1.33 mM).


Author(s):  
Kai-Liang Ma ◽  
Shi-Hui Dong ◽  
Hang-Ying Li ◽  
Wen-Jun Wei ◽  
Yong-Qiang Tu ◽  
...  

Abstract Three previously undescribed cytochalasins, named xylariasins A‒C (1‒3), together with six known ones (4‒9) were isolated from Xylaria sp. CFL5, an endophytic fungus of Cephalotaxus fortunei. The chemical structures of all new compounds were elucidated on the basis of extensive spectroscopic data analyses and electronic circular dichroism calculation, as well as optical rotation calculation. Biological activities of compounds 1, 4‒9 were evaluated, including cytotoxic, LAG3/MHC II binding inhibition and LAG3/FGL1 binding inhibition activities. Compounds 6 and 9 possessed cytotoxicity against AGS cells at 5 μM, with inhibition rates of 94% and 64%, respectively. In addition, all tested isolates, except compound 6, exhibited obvious inhibitory activity against the interaction of both LAG3/MHC II and LAG3/FGL1. Compounds 1, 5, 7, and 8 inhibited LAG3/MHC II with IC50 values ranging from 2.37 to 4.74 μM. Meanwhile, the IC50 values of compounds 1, 7, and 8 against LAG3/FGL1 were 11.78, 4.39, and 7.45 μM, respectively. Graphic Abstract


Planta Medica ◽  
2017 ◽  
Vol 84 (05) ◽  
pp. 336-343 ◽  
Author(s):  
Yifan Wang ◽  
Liangjin Xu ◽  
Wen Gao ◽  
Lixin Niu ◽  
Chunyue Huang ◽  
...  

AbstractThree new Diels-Alder adducts, macrourins E – G (1–3), one new 2-arylbenzofuran, macrourin H (4), and eight known Diels-Alder adducts (5–12) were isolated from Morus macroura. Their structures were elucidated through extensive analysis of spectroscopic data. The 1H NMR and ECD trends in the determination of the configurations of these Diels-Alder adducts were summarized. The tyrosinase inhibitory activities of all compounds isolated were evaluated, and the new compounds (1–4) as well as the eight known compounds (5–12) were found to be potent with IC50 values ranging from 0.39 to 4.54 µM. Among them, 1 showed the best tyrosinase inhibitory activity with an IC50 value of 0.39 µM, approximately 50 times stronger than the positive control, kojic acid.


2021 ◽  
Vol 8 (1) ◽  
pp. 65
Author(s):  
Rezqi Handayani ◽  
Nurul Qamariah ◽  
Muhammad Izmiansyah

Saluang Belum (Luvunga sarmentosa Kurz) adalah tumbuhan yang dikenal sebagai obat tradisional di Kalimantan Tengah. Batang L. sarmentosa Kurz dipercayai memiliki manfaat secara empiris sebagai antioksidan yang dimanfaatkan sebagai anti-aging (anti penuaan dini). Batang L. sarmentosa Kurz mengandung metabolit sekunder yaitu tanin, saponin, steroid dan flavonoid yang diduga memiliki aktivitas sebagai antibakteri. Berdasarkan khasiat empiris dan kandungan metabolit sekunder yang ada dalam tumbuhan L. sarmentosa Kurz, maka dilakukan penelitian tentang aktivitas daya hambat ekstrak etanol tumbuhan ini terhadap bakteri P. acnes yang merupakan salah satu bakteri penyebab jerawat. Tujuan dari penelitian ini adalah untuk mengetahui aktivitas daya hambat ekstrak etanol batang L. sarmentosa Kurz terhadap bakteri P.acnes. Metode penelitian yang dilakukan pada penelitian ini dimulai dari pengambilan simplisia, pembuatan ekstrak etanol dengan metode perkolasi dan uji daya hambat dengan menggunakan metode Disk Difusion yang menggunakan kontrol positif antibiotik klindamicin. Analisis data dilakukan dengan membandingkan lebar zona hambat dari ekstrak etanol batang L. sarmentosa Kurz  dengan kategori penghambatan antimikroba klindamisin berdasarkan diameter zona hambat dari Clinical and Laboratory Standards Institute.  Hasil uji daya hambat didapatkan zona hambat ekstrak etanol batang Saluang Belum pada semua konsentrasi 0,5%, 1%, 5%, 10% dan 15% secara berturut-turut yaitu  Intermediate, Resistant, Intermediate, Susceptible dan Susceptible dan hasil dari zona hambat klindamicin pada semua konsentrasi 0,5%,1%,5%,10%,dan 15% adalah susceptible. Simpulan dari penelitian ini adalah ekstrak etanol batang L. sarmentosa Kurz mempunyai kemampuan dalam menghambat pertumbuhan bakteri P.acnes.           Kata Kunci: Obat Tradisional, Jerawat, Uji Daya Hambat, Propionibacterium acnes, Batang Saluang Belum Saluang belum (Luvunga sarmentosa Kurz) is one of traditional medicine in Central Kalimantan. The stem of L. sarmentosa Kurz is believed to have empirical benefits as an antioxidant which is used as anti-ageing (anti-ageing). The stem of L. sarmentosa Kurz contains secondary metabolites, namely tannins, saponins, steroids and flavonoids which are thought to have antibacterial activity. Based on the empirical properties and the content of secondary metabolites in L. sarmentosa Kurz, a study was conducted on the inhibitory activity of this plant's ethanol extract against P. acnes, which is one of the bacteria that causes acne. The purpose of this study was to determine the inhibitory activity of the ethanol extract of L. sarmentosa Kurz stem against P.acnes bacteria. The research method carried out in this study started from taking simplicia, making ethanol extract using the percolation method and the inhibition test using the disk diffusion method which used a positive control of the clindamycin antibiotic. Data analysis was performed by comparing the inhibition zone width of the ethanol extract of L. sarmentosa Kurz stem with the clindamycin antimicrobial inhibition category based on the inhibition zone diameter of the Clinical and Laboratory Standards Institute. The results of the inhibition test obtained the inhibition zone of Saluang Belum stem ethanol extract at all concentrations of 0.5%, 1%, 5%, 10% and 15% respectively, Intermediate, Resistant, Intermediate, Susceptible and Susceptible and the results of the inhibition zone. Clindamycin at all concentrations of 0.5%, 1%, 5%, 10%, and 15% are susceptible. This research concludes that the ethanol extract of L. sarmentosa Kurz stem can inhibit the growth of P.acnes bacteria.


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