scholarly journals Structures, Chemical Conversions, and Cytotoxicity of Tricholopardins C and D, Two Tricholoma Triterpenoids from the Wild Mushroom Tricholoma pardinum

2021 ◽  
Author(s):  
Chen Shi ◽  
Yue-Ling Peng ◽  
Juan He ◽  
Zheng-Hui Li ◽  
Ji-Kai Liu ◽  
...  
Keyword(s):  
Hela Cell ◽  
Single Crystal ◽  
Cell Lines ◽  
Cell Apoptosis ◽  
Spectroscopic Methods ◽  
Wild Mushroom ◽  
X Ray Diffraction ◽  
X Ray ◽  
Hela Cell Lines ◽  
Mcf 7

AbstractTwo undescribed Tricholoma triterpenoids, namely tricholopardins C (1) and D (2), were isolated from the wild mushroom Tricholoma pardinum. Their structures with absolute configurations were elucidated by spectroscopic methods, as well as the single crystal X-ray diffraction. Compounds 1 and 2 were further obtained by chemical conversions from the known analogues. Compound 1 showed significant cytotoxicity to MCF-7 and Hela cell lines with IC50 values of 4.7 μM and 9.7 μM, respectively. Its mechanism of inducing MCF-7 cell apoptosis was studied briefly. Graphical Abstract

scholarly journals 5α,8α-Epidioxysterols from a Formosan Sponge, Axinyssa sp

2013 ◽  
Vol 8 (11) ◽  
pp. 1934578X1300801
Author(s):  
Tzu-Rong Su ◽  
Kai-Ju Liang ◽  
Michael Y. Chiang ◽  
Mei-Chin Lu ◽  
Yu-Jen Wu ◽  
...  
Keyword(s):  
Single Crystal ◽  
Diffraction Analysis ◽  
Cell Lines ◽  
Cancer Cell ◽  
Absolute Configuration ◽  
Cancer Cell Lines ◽  
Spectroscopic Methods ◽  
X Ray Diffraction ◽  
X Ray ◽  
First Time

One new 5α,8α-epidioxysterol, 3-acetylaxinysterol (1), along with one known sterol, axinysterol (2), were isolated from a Formosan sponge, Axinyssa sp.. The structures of the compounds were determined by spectroscopic methods and the absolute configuration of 2 was further confirmed by single-crystal X-ray diffraction analysis for the first time. Compound 2 exhibited significant cytotoxicity against K562 and Molt 4 cancer cell lines.

scholarly journals Synthesis and Anti-Proliferative Assessment of Triazolo-Thiadiazepine and Triazolo-Thiadiazine Scaffolds

Molecules ◽  
2019 ◽  
Vol 24 (24) ◽  
pp. 4471 ◽  
Author(s):  
Ahmed T. A. Boraei ◽  
Hazem A. Ghabbour ◽  
Mohamed S. Gomaa ◽  
El Sayed H. El Ashry ◽  
Assem Barakat
Keyword(s):  
Single Crystal ◽  
Cell Lines ◽  
Cancer Cell ◽  
2D Nmr ◽  
Cancer Cell Lines ◽  
Docking Studies ◽  
X Ray ◽  
Cytotoxicity Activity ◽  
Human Liver Cancer ◽  
Mcf 7

A series of triazolo-thiadiazepines 4a–k were synthesized with excellent yields using dehydrated PTSA as a catalyst in toluene. Two triazolo-thiadiazines were obtained; 8a was formed directly by reflux in ethanol, whereas, PTSA promoted the formation of 8b. The molecular structure of the formed triazolo-thiadiazepines is identical to the imine-form 4a–k and not the enamine-tautomer 6a–k. The structures of the newly synthesized triazolo-thiadiazepines 4a–k and triazolo-thiadiazines 8a–b were elucidated using NMR (1H, and 13C), 2D NMR, HRMS, and X-ray single crystal. Furthermore, 4a was deduced using X-ray single crystal diffraction analysis. These new thiadiazepine hits represent an optimized series of previously synthesized indole-triazole derivatives for the inhibition of EGFR. The cytotoxicity activity against two cancer cell lines including human liver cancer (HEPG-2) and breast cancer (MCF-7) was promising, with IC50 between 12.9 to 44.6 µg/mL and 14.7 to 48.7 µg/mL for the tested cancer cell lines respectively, compared to doxorubicin (IC50 4.0 µg/mL). Docking studies revealed that the thiadiazepine scaffold presented a suitable anchor, allowing good interaction of the various binding groups with the enzyme binding regions and sub-pockets.

Synthese und Molekülstruktur des [α-(Dichlormethylsilyl)ethyl]- dichlorboran-dimethylsulfid / Synthesis and Molecular Structure of [α-(Dichloromethylsilyl)ethyl]- dichloroborane-dimethylsulfide

1999 ◽  
Vol 54 (5) ◽  
pp. 624-626 ◽  
Author(s):  
Lutz Ruwisch ◽  
Ralf Riedel ◽  
Uwe Klingebiel ◽  
Mathias Noltemeyer
Keyword(s):  
Molecular Structure ◽  
Single Crystal ◽  
Spectroscopic Methods ◽  
X Ray Diffraction ◽  
X Ray ◽  
Markovnikov Rule

[α-(Dichloromethylsilyl)ethyl]-dichloroborane-dimethylsulfide has been synthesized by the reaction of dichloromethylvinylsilane with dichloroborane-dimethylsulfide and its molecular structure determined by single crystal X-ray diffraction and by spectroscopic methods. Following the Markovnikov rule, a chiral methine group is formed as a bridge between silicon and boron.

Isolation, Characterization and Crystal Structure of Natural Eremophilenolide from Ligularia sagitta

2004 ◽  
Vol 59 (8) ◽  
pp. 921-924 ◽  
Author(s):  
Lyi Li ◽  
Li-Wen Xu ◽  
Yan-Feng Jiang ◽  
Chan-Juan Xi ◽  
Han-Qing Wang ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Single Crystal ◽  
Spectroscopic Methods ◽  
X Ray Diffraction ◽  
X Ray ◽  
Aerial Parts

AbstractA new eremophilenolide 1β ,10β -epoxy-6β -acetoxy-3β -angeloyloxy-8β -hydrox y-eremophil- 7(11)-en-8,12α-olide (1), together with liguhodgsonal (2), esculetin (3) and β -sitosterol (4), was isolated from the aerial parts of Ligularia sagitta. The structure of the new constituent (1) was elucidated by spectroscopic methods and confirmed by single-crystal X-ray diffraction.

scholarly journals Unexpected Synthesis, Single-Crystal X-ray Structure, Anticancer Activity, and Molecular Docking Studies of Certain 2–((Imidazole/Benzimidazol–2–yl)thio)–1–arylethanones

Crystals ◽  
2020 ◽  
Vol 10 (6) ◽  
pp. 446
Author(s):  
Tarfah Al-Warhi ◽  
Mohamed Said ◽  
Mahmoud El Hassab ◽  
Nada Aljaeed ◽  
Hazem Ghabour ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Molecular Docking ◽  
Single Crystal ◽  
Cell Lines ◽  
Docking Study ◽  
Anticancer Activities ◽  
Molecular Docking Study ◽  
X Ray ◽  
Mcf 7

In connection with our research program concerning development of novel effective benzimidazole-based anticancer candidates, herein we describe a new unexpected synthetic route to obtain a series of 2–((imidazole/benzimidazol2–yl)thio)1–arylethanones endowed with promising anti-breast cancer and Cyclin-dependent kinase 2 (CDK2) inhibitory activities. Contrary to expectations, products for the reaction of 2–mercaptoimidazole/benzimidazole 2a,b with β–keto esters 6a–c were unambiguously assigned as 2–((imidazol/benzimidazol2–yl)thio)1–arylethanones 10a–f based on NMR spectroscopy and single-crystal X-ray crystallographic analyses. In vitro anticancer activities for herein reported imidazole/benzimidazoles 10a–f were assessed through a cell-based assay against human breast cancer T4–7D and MCF–7 cell lines. Benzimidazoles 10d–f exerted better anti-proliferative action towards T4–7D and MCF–7 cell lines than their corresponding imidazole counterparts 10a–c. Furthermore, a molecular docking study suggested CDK2 kinase as a potential enzymatic target for benzimidazoles 10d–f, and investigated their possible binding pattern and interactions within CDK2 active site. Thereafter, benzimidazoles 10d–f were in vitro examined for their CDK2 inhibitory action, where they exerted good activity. Finally, several key ADME and druglikeness properties were predicted by the SwissADME online tool. Interestingly, benzimidazoles 10d–f were found to have no violations in all druglikeness rules (Veber, Lipinski, Ghose, Muegge, and Egan). In addition, they had neither PAINS nor structural alerts (Brenks). In conclusion, benzimidazoles 10d–f demonstrated not only a promising anticancer activities but also an acceptable ADME and physicochemical properties especially benzimidazole 10e.

Radiation dose rate affects the radiosensitization of MCF-7 and HeLa cell lines to X-rays induced by dextran-coated iron oxide nanoparticles

2017 ◽  
Vol 93 (8) ◽  
pp. 757-763 ◽  
Author(s):  
Karim Khoshgard ◽  
Parvaneh Kiani ◽  
Abbas Haghparast ◽  
Leila Hosseinzadeh ◽  
Mohammad Taghi Eivazi
Keyword(s):  
Iron Oxide ◽  
Radiation Dose ◽  
Hela Cell ◽  
Dose Rate ◽  
Cell Lines ◽  
Oxide Nanoparticles ◽  
X Rays ◽  
Radiation Dose Rate ◽  
Hela Cell Lines ◽  
Mcf 7

scholarly journals Jatroidaine A: a New Tetranortirucallane Type Triterpene from Jatropha multifida

2021 ◽  
Vol 15 (5) ◽  
pp. 408-413
Author(s):  
Fei Li ◽  
Liang Ma ◽  
Jinyuan Zhang ◽  
Xueling Qiao ◽  
Dingshan Zhang ◽  
...  
Keyword(s):  
Single Crystal ◽  
Diffraction Analysis ◽  
Absolute Configuration ◽  
Thioredoxin Reductase ◽  
Spectroscopic Methods ◽  
Significant Activity ◽  
X Ray Diffraction ◽  
X Ray ◽  
Inhibitory Activities ◽  
Jatropha Multifida

Jatroidaine A (1), a new tetranortirucallane-type triterpene, and two known analogues (2−3) were isolated from the leaves and branches of Jatropha multifida. Their structures were fully elucidated by extensive spectroscopic methods and comparison to known compounds. The absolute configuration of 1 was assigned by single-crystal X-ray diffraction analysis. All compounds were evaluated for their anti-inflammatory and thioredoxin reductase (TrxR) inhibitory activities. Unfortunately, no significant activity was observed.

scholarly journals In Vitro, Evaluation of Anticancer and Anti-dermatophytes Activities of Some Egyptian Medicinal Plants 

2020 ◽  
Author(s):  
Esraa Ahmed Mohamed El-Bondkly ◽  
Mervat Morsy El-Gendy ◽  
Aya Ahmed Mohamed El-Bondkly ◽  
Fareed Shawky El-Shenawy ◽  
Alaa Ahmed Mohamed El-Bondkly
Keyword(s):  
Hela Cell ◽  
Cell Lines ◽  
Methanolic Extract ◽  
Acetone Extract ◽  
Microsporum Canis ◽  
Microsporum Gypseum ◽  
Hela Cell Lines ◽  
Trichophyton Soudanense ◽  
Hct 116 ◽  
Mcf 7

Abstract In this investigation three ancient Egyptian medical plants; Plantago albicans L., Thymelaea hirsuta (L.) Endl. and Urginea maritima (L.) were chosen to explore their biochemical properties, anticancer and antimycotic activities against clinical dermatophytes. Growing of Trichophyton soudanense, Trichophyton erinacei, Microsporum audouinii, Microsporum gypseum, Microsporum gallinae, Microsporum ferrogenium, Microsporum cookie, Microsporum racemosum, Microsporum persicolor and Microsporum canis were totally inhibited by the 100 µg/mL of P. albicans methanolic extract. Whereas the growth of T. soudanense, T. erinacei, Trichophyton rubrum, Trichophyton tonsurance and Trichophyton mentagrophytes and Epidermophyton floccosum were 100% inhibited by the methanolic extract of T. hirsiuta at 100 µg/mL concentration, however its acetone extract was more active against Microsporum species. The highest fungi toxicity against all dermatophytic fungi was detected in both methanol and acetone extract of U. maritima at a concentration ranged between 50 to 100 µg/mL. Methanolic extract of P. albicans inhibited the viability of HCT-116, HepG-2, MCF-7 and HeLa cell lines by (41%, 40%, 80% and 81%); (30%, 20%, 66% and 70%); (19%, 0%, 49% and 57%); (5%, 0%, 35% and 45%) and (0%, 0%, 21% and 40%) at 25, 50, 100, 200 and 300 µg/mL, respectively. Moreover, the cells death after treatment with the same concentrations of T. hirsuta methanol extract were (10%, 20%, 23% and 60%); (16%, 40%, 58% and 80%); (40%, 50%, 80% and 100%); (51%, 65%, 100% and 100%) and (49%, 82%, 100% and 100%) in HCT-116, HepG-2, MCF-7 and HeLa cells, respectively. Viability of HCT-116, MCF-7 and HepG-2 cell lines was totally suppressed with 100 µg/mL whereas the HeLa cell growth was reduced to 10% and totally killed at 100 and 200 µg/mL, respectively of U. maritima methanolic extract. All data approve the significance of Egyptian ethnomedical plants as potent source of diverse bioactive pharmaceutical metabolites.

scholarly journals A Novel Azaphilone Muyophilone A From the Endophytic Fungus Muyocopron laterale 0307-2

2021 ◽  
Vol 9 ◽  
Author(s):  
Chao Yuan ◽  
Yuhua Guo ◽  
Ke Wang ◽  
Zhunian Wang ◽  
Longfei Li ◽  
...  
Keyword(s):  
Circular Dichroism ◽  
Nmr Spectroscopy ◽  
Single Crystal ◽  
Endophytic Fungus ◽  
Vibrational Circular Dichroism ◽  
Spectroscopic Methods ◽  
X Ray Diffraction ◽  
X Ray ◽  
Spectroscopic Analyses ◽  
Circular Dichroïsm

Two known azaphilone derivatives, 4,6-dimethylcurvulinic acid (1) and austdiol (2), and their novel heterotrimer, muyophilone A (3), were isolated and identified from an endophytic fungus, Muyocopron laterale 0307-2. Their structures and stereochemistry were established by extensive spectroscopic analyses including HRMS, NMR spectroscopy, electronic circular dichroism (ECD) and vibrational circular dichroism (VCD) spectroscopic methods, as well as single crystal X-ray diffraction. In the structure of 3, two compound 2-derived azaphilone units were connected through an unprecedented five-membered carbon bridge which was proposed to be originated from compound 1. Compound 3 represents the first example of azaphilone heterotrimers.

Sign in / Sign up

Export Citation Format

Share Document