Small Molecule Constituents of Periplaneta americana and Their IL-6 Inhibitory Activities

2021 ◽  
Vol 16 (9) ◽  
pp. 1934578X2110331
Author(s):  
Hua-Sheng Zhang ◽  
Yong-Ming Yan ◽  
Dai-Wei Wang ◽  
Qing Lv ◽  
Yong-Xian Cheng ◽  
...  

Two new glycosides, periplanosides A (1) and B (2), 3 compounds reported from a natural source for the first time (3 − 5), and 6 known compounds 6 − 11 were isolated from the ethanol extract of Periplaneta americana (Linnaeus). Their structures, including absolute configurations, were unambiguously identified by comprehensive spectroscopic and chemical methods. Compound 3 is a racemate whose enantiomers were purified by chiral high-performance liquid chromatography . The biological evaluation results showed that compound 7 (0 − 20 μM) did not affect the viability of RAW264.7 cells and could effectively inhibit the production of interleukin-6 stimulated by lipopolysaccharide in a concentration-dependent manner, indicating the potential to develop novel agents against inflammation-related diseases.

Plants ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1311
Author(s):  
Magdalena Chmur ◽  
Andrzej Bajguz

Brassinolide (BL) represents brassinosteroids (BRs)—a group of phytohormones that are essential for plant growth and development. Brassinazole (Brz) is as a synthetic inhibitor of BRs’ biosynthesis. In the present study, the responses of Wolffia arrhiza to the treatment with BL, Brz, and the combination of BL with Brz were analyzed. The analysis of BRs and Brz was performed using LC-MS/MS. The photosynthetic pigments (chlorophylls, carotenes, and xanthophylls) levels were determined using HPLC, but protein and monosaccharides level using spectrophotometric methods. The obtained results indicated that BL and Brz influence W. arrhiza cultures in a concentration-dependent manner. The most stimulatory effects on the growth, level of BRs (BL, 24-epibrassinolide, 28-homobrassinolide, 28-norbrassinolide, catasterone, castasterone, 24-epicastasterone, typhasterol, and 6-deoxytyphasterol), and the content of pigments, protein, and monosaccharides, were observed in plants treated with 0.1 µM BL. Whereas the application of 1 µM and 10 µM Brz caused a significant decrease in duckweed weight and level of targeted compounds. Application of BL caused the mitigation of the Brz inhibitory effect and enhanced the BR level in duckweed treated with Brz. The level of BRs was reported for the first time in duckweed treated with BL and/or Brz.


Drug Research ◽  
2019 ◽  
Vol 69 (12) ◽  
pp. 665-670 ◽  
Author(s):  
Mohammad Jalili-Nik ◽  
Hamed Sabri ◽  
Ehsan Zamiri ◽  
Mohammad Soukhtanloo ◽  
Mostafa Karimi Roshan ◽  
...  

AbstractGlioblastoma multiforme (GBM) is the fatal type of astrocytic tumors with a survival rate of 12 months. The present study, for the first time, evaluated the cytotoxic impacts of Ferula latisecta (F. latisecta) hydroalcoholic extract on U87 GBM cell line. The MTT assay measured the cellular toxicity following 24- and 48 h treatment with various doses of F. latisecta (0–800 μg/mL). Apoptosis was evaluated by an Annexin V/propidium iodide (PI) staining 24 h after treatment by F. latisecta. Moreover, to determine the cellular metastasis of U87 cells, we used a gelatin zymography assay (matrix metalloproteinase [MMP]-2/-9 enzymatic activity). The outcomes showed that F. latisecta mitigated the viability of U87 cells in a concentration- and time-dependent manner with IC50 values of 145.3 and 192.3 μg/mL obtained for 24- and 48 h treatments, respectively. F. latisecta induced apoptosis in a concentration-dependent manner after 24 h. Also, MMP-9 activity was significantly decreased following 24 h after treatment concentration-dependently with no change in MMP-2 enzymatic activity. This study showed that F. latisecta induced cytotoxicity and apoptosis, and mitigated metastasis of U87 GBM cells. Hence, F. latisecta could be beneficial as a promising natural herb against GBM after further studies.


Fitoterapia ◽  
2020 ◽  
Vol 3 (3) ◽  
pp. 44-50
Author(s):  
S.M. Marchyshyn ◽  
◽  
L.V. Slobodianiuk ◽  
R.Yu. Basaraba ◽  
N.А. Hudz ◽  
...  

Keywords: amino acids; common pussytoes; yacon; stevia; golden marigolds; leaves; herb; aster family; high performance liquid chromatography. For the first time the qualitative composition was studied and the quantitative content of amino acids in the herb of common pussytoes, yacon leaves, stevia leaves, herb of golden marigolds was determined by HPLC. 17 bound and 16 free amino acids were identified in the herb of common pussytoes, in the herb of golden marigolds, yacon leaves and stevia leaves – 12 and 5, 17 and 11 and 16 and 14 amino acids, respectively. The highest content of the sum of essential and substitute amino acids is contained in the leaves of stevia; the lowest content of the sum of essential amino – in the herb of golden marigolds, the sum of essential amino acids – in the herb of common pussytoes.


Life ◽  
2021 ◽  
Vol 11 (9) ◽  
pp. 939
Author(s):  
Pia Loreto Werlinger Bravo ◽  
Hui Jin ◽  
Hyunwoo Park ◽  
Min Sang Kim ◽  
Hirofumi Matsui ◽  
...  

Cardiovascular diseases, such as stroke, are the most common causes of death in developed countries. Ischemic stroke accounts for 85% of the total cases and is caused by abnormal thrombus formation in the vessels, causing deficient blood and oxygen supply to the brain. Prophylactic treatments include the prevention of thrombus formation, of which the most used is acetylsalicylic acid (ASA); however, it is associated with a high incidence of side effects. Angelica gigas Nakai (AG) is a natural herb used to improve blood circulation via anti-platelet aggregation, one of the key processes involved in thrombus formation. We examined the antithrombotic effects of AGE 232, the ethanol extract of A. gigas Nakai. AGE 232 showed a significant reduction in death or paralysis in mice caused by collagen/epinephrine-induced thromboembolism in a dose-dependent manner and inhibition of collagen-induced human platelet aggregation in a concentration-dependent manner. Additionally, AGE 232-treated mice did not show severe bleeding in the gut compared to ASA-treated mice. AGE 232 resulted in a decrease in the number of neutrophils attached to the human umbilical vein endothelial cells (HUVECs) and lower inhibition of COX-1 in response to bleeding and damage to blood vessels, a major side effect of ASA. Therefore, AGE 232 can prevent thrombus formation and stroke.


2020 ◽  
Vol 42 (4) ◽  
pp. 564-564
Author(s):  
Ju liu Ju liu ◽  
Jun Li Jun Li ◽  
Jian tao Shi Jian tao Shi ◽  
Jie Li Jie Li ◽  
Xue chen Hao Xue chen Hao ◽  
...  

A series of novel 4-phenylaminobenzofuro[2,3-d]pyrimidine derivatives had been prepared and assessed for their in vitro antiproliferative activities against three lung cancer cell lines (A549, H460 and H1975). The bioassay results showed most of the designed compounds exhibited potential antiproliferation activities. Among them, compound 8f exhibited remarkable inhibitory activity against A549 and H460 cell lines with IC50 value of 2.54 μM and 2.68 μM, respectively, which was comparable to that of the positive control sorafenib (IC50 = 2.69 μM for A549 and 3.71 μM for H460). AO/EB staining suggests that compound 8f could induce apoptosis in A549 cells. Furthermore, cell cycle analyses show that compound 8f increased G0/G1 A549 cells arrest in a concentration-dependent manner. The preliminary structure-activity relationships (SARs) studies indicated that mono-electron-withdrawing groups (mono-EWGs) on the phenyl ring are positive on the antitumor activity.


Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2108 ◽  
Author(s):  
Chuanming Zhang ◽  
Xiaoyu Tan ◽  
Jian Feng ◽  
Ning Ding ◽  
Yongpeng Li ◽  
...  

To discover new antiproliferative agents with high efficacy and selectivity, a new series of 1-aryl-3-{4-[(pyridin-2-ylmethyl)thio]phenyl}urea derivatives (7a–7t) were designed, synthesized and evaluated for their antiproliferative activity against A549, HCT-116 and PC-3 cancer cell lines in vitro. Most of the target compounds demonstrated significant antiproliferative effects on all the selective cancer cell lines. Among them, the target compound, 1-[4-chloro-3-(trifluoromethyl)phenyl]-3-{4-{{[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methyl}thio}phenyl}urea (7i) was identified to be the most active one against three cell lines, which was more potent than the positive control with an IC50 value of 1.53 ± 0.46, 1.11 ± 0.34 and 1.98 ± 1.27 μM, respectively. Further cellular mechanism studies confirmed that compound 7i could induce the apoptosis of A549 cells in a concentration-dependent manner and elucidated compound 7i arrests cell cycle at G1 phase by flow cytometry analysis. Herein, the studies suggested that the 1-aryl-3-{4-[(pyridin-2-ylmethyl)thio]phenyl}urea skeleton might be regarded as new chemotypes for designing effective antiproliferative agents.


2019 ◽  
Vol 14 (1) ◽  
pp. 1934578X1901400
Author(s):  
Lilia Cherigo ◽  
Sergio Martínez-Luis

In our continuous search for α-glucosidase inhibitors, three active pentacyclic triterpenes were isolated from stem bark samples of the Panamanian mangrove Pelliciera rhizophorae Triana & Planchon. These compounds were identified by both spectroscopic and spectrometric analysis. Of the isolated compounds, only betulinic acid has been previously isolated from P. rhizophorae leaves while both betulin (IC50 2.09 μM) and lupeol (IC50 0.58 μM) were isolated from this plant for the first time. All three pentacyclic triterpenes inhibited the α-glucosidase enzyme in a concentration-dependent manner, and their inhibitory activity was higher than that of the antidiabetic drug acarbose (IC50 241.6 μM). Kinetic analysis established that betulin and lupeol acted as competitive inhibitors. Finally, docking analysis suggested that all three triterpenes bind at the same site as acarbose does in the human intestinal α-glucosidase (PDB: 3TOP). This work contributes further evidence similar to previous studies that point out that the aerial parts of P. rhizophorae might be potential agents in controlling hyperglycemia in diabetic persons.


1999 ◽  
Vol 54 (12) ◽  
pp. 1145-1174 ◽  
Author(s):  
Ingo Röhl ◽  
Bernd Schneider ◽  
Bettina Schmidt ◽  
Erich Zeeck

Sex pheromones, released with the coelomic fluid by male Platynereis dumerilii initiate egg release in swarming females. The egg release pheromone, isolated from the coelomic fluid of sexually mature males, was identified as ʟ-Ovothiol A, which was found in male marine invertebrates for the first time. Isolation was obtained by reversed-phase high-performance liquid chromatography in the biologically inactive disulfide form.


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