scholarly journals Cytotoxic and Anti-inflammatory Constituents from Juncus effusus

2017 ◽  
Vol 60 (2) ◽  
Author(s):  
Ma Wei ◽  
Liu Feng ◽  
Zhang Yue ◽  
Li Ning
Keyword(s):  
Spectroscopic Analysis ◽  
Human Cancer ◽  
Juncus Effusus ◽  
Inhibitory Effects ◽  
1H And 13C Nmr ◽  
Human Cancer Cell Lines ◽  
Raw264.7 Macrophages ◽  
Ic50 Values ◽  
New Compounds ◽  
Mcf 7

<p>A new sesquilignan effususin E (1) and a new long chain fatty enamide effususin F (2), together with eight known compounds were isolated from the medullae of <em>Juncus effusus</em>. The structures of 1 and 2 were elucidated by detailed spectroscopic analysis including 1H and 13C NMR, COSY, HSQC, HMBC, and HRMS, while the struc-tures of the known compounds were deduced from comparison of their spectral data with those in the literature. The new compounds 1 and 2 were evaluated against five human cancer cell lines (SHSY-5Y, SMMC-7721, HepG-2, Hela, and MCF-7) by CCK-8 assay, but only 1 exhibited weak cytotoxic activity against SMMC-7721 with IC50 val-ue of 57.5 μM. Inhibitory effects of 1 and 2 on nitric oxide (NO) pro-duction in lipopolysaccharide-induced RAW264.7 macrophages were also evaluated, and they were found to exhibit good inhibitory activities with IC50 values of 8.59 and 13.73 μM, respectively.</p>

scholarly journals Cytotoxic Polyketides from the Marine Sponge-Derived Fungus Pestalotiopsis heterocornis XWS03F09

Molecules ◽  
2019 ◽  
Vol 24 (14) ◽  
pp. 2655 ◽  
Author(s):  
Lei ◽  
Lei ◽  
Zhou ◽  
Hu ◽  
Niu ◽  
...  
Keyword(s):  
Marine Sponge ◽  
Spectroscopic Analysis ◽  
Fermentation Broth ◽  
Human Cancer ◽  
Optical Rotation ◽  
Cytotoxic Activities ◽  
Human Cancer Cell Lines ◽  
Chemical Structures ◽  
Ic50 Values ◽  
New Compounds

Four new compounds, including two new polyketides, heterocornols M and N (1, 2), and a pair of epimers, heterocornols O and P (3, 4), were isolated from the fermentation broth of the marine sponge-derived fungus Pestalotiopsis heterocornis XWS03F09, together with three known compounds (5–7). The new chemical structures were established on the basis of a spectroscopic analysis, optical rotation, experimental and calculated electronic circular dichroism (ECD). All of the compounds (1–7) were evaluated for their cytotoxic activities, and heterocornols M-P (1–4) exhibited cytotoxicities against four human cancer cell lines with IC50 values of 20.4–94.2 μM.

Three New Cytotoxic Monoterpenoid Bisindole Alkaloids from Tabernaemontana bufalina

Planta Medica ◽  
2018 ◽  
Vol 84 (15) ◽  
pp. 1127-1133 ◽  
Author(s):  
Si-Yuan Zhou ◽  
Ting-Lan Zhou ◽  
Guofu Qiu ◽  
Xiajuan Huan ◽  
Ze-Hong Miao ◽  
...  
Keyword(s):  
Human Cancer ◽  
Spectroscopic Methods ◽  
Human Cancer Cell ◽  
Inhibitory Effects ◽  
Human Cancer Cell Lines ◽  
Human Cancer Cells ◽  
Aerial Parts ◽  
Ic50 Values ◽  
Circular Dichroic ◽  
Mcf 7

AbstractThree new bisindole alkaloids, 3′-(2-oxopropyl)-19,20-dihydrotabernamine (1), 3′-(2-oxopropyl)-ervahanine B (2), 19,20-dihydrovobparicine (3), and 20 known compounds were isolated from the aerial parts of Tabernaemontana bufalina. The structures of these alkaloids were elucidated using spectroscopic methods. The absolute configurations of 1–3 were determined by the circular dichroic exciton chirality method. Compounds 1–23 were screened for their cytotoxicity against two human cancer cell lines, A-549 and MCF-7. Ten compounds (1–3, 10, 14, 16, 17, 19, 22, and 23) exhibited inhibitory effects against the two human cancer cells with IC50 values of 1.19 ~ 6.13 µM.

scholarly journals Synthesis of Novel Benzamide- piperazine-sulfonamide Hybrids as Potential Anticancer Agents

2019 ◽  
Vol 92 (3) ◽  
pp. 393-402
Author(s):  
B. Ramalingeswara Rao ◽  
Mohana Rao Katiki ◽  
Dileep Kommula ◽  
SaiShyam Narayanan ◽  
Ruby John Anto ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Sensitive Cell Line ◽  
Human Cancer Cell Lines ◽  
Ic50 Values ◽  
Different Origins ◽  
New Compounds ◽  
A549 Lung

The synthesis of a series of substituted hippuric acid (2-benzamidoacetic acid) derivatives containing arylsulfonylpiperazine nucleus (3a–j, 4a–j) is described. The compounds were synthesized by coupling hippuric/4-fluorohippuric acid with various arylsulfonylpiperazines using N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (EDCI). The structures of all the new compounds were confirmed by IR, NMR and MS spectral data. All the synthesized compounds have been evaluated for their in vitro cytotoxicity towards five human cancer cell lines of different origins viz. HeLa (Cervical), A549 (Lung), A375 (Skin), MD-AMB-231(Breast) and T98G (brain) and their IC50 values were determined. Among the compounds tested, 3b, 3d, 3g, 4c and 4e displayed significant cytotoxic activity (IC50 = 24.2–38.2 µM). T98G was the most sensitive cell line towards the compounds studied followed by HeLa, A375, A549 and MD-AMB-231.

scholarly journals Two New Cytotoxic Steroidal Alkaloids from Sarcococca Hookeriana

Molecules ◽  
2018 ◽  
Vol 24 (1) ◽  
pp. 11 ◽  
Author(s):  
Shaojie Huo ◽  
Jichun Wu ◽  
Xicheng He ◽  
Lutai Pan ◽  
Jiang Du
Keyword(s):  
Cell Lines ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Steroidal Alkaloids ◽  
X Ray ◽  
Human Cancer Cell Lines ◽  
X Ray Crystallography ◽  
Ic50 Values ◽  
Mcf 7

Two new steroidal alkaloids, named hookerianine A (1) and hookerianine B (2) were isolated from the stems and roots of Sarcococca hookeriana Baill., along with two known compounds, sarcorucinine G (3) and epipachysamine D (4). On the basis of spectroscopic methods and by comparison with literature data, their structures were determined. As well as X-ray crystallography was performed to confirm compound 4. To identify novel antitumor inhibitors, all compounds were performed a CCK-8 assay against five human cancer cell lines SW480, SMMC-7721, PC3, MCF-7 and K562 in vitro. Compound 2 exhibited moderate cytotoxic activities to all cell lines with IC50 values in the range of 5.97–19.44 μM. Compound 3 was the most effective one against SW480 and K562 cell lines with IC50 values of 5.77 and 6.29 μM, respectively.

scholarly journals Ochroborbone, A New Cytotoxic Indole Alkaloid from Ochrosia borbonica

2017 ◽  
Vol 12 (4) ◽  
pp. 1934578X1701200
Author(s):  
Yan-Ping Liu ◽  
A-Hong Chen ◽  
Ruo-Heng Li ◽  
Hui-Wen Yang ◽  
Hai-Nan Bao ◽  
...  
Keyword(s):  
Human Cancer ◽  
Indole Alkaloid ◽  
Spectroscopic Methods ◽  
Inhibitory Effects ◽  
Human Cancer Cell Lines ◽  
Stems And Leaves ◽  
Monoterpenoid Indole Alkaloid ◽  
First Time ◽  
Mcf 7

A new monoterpenoid indole alkaloid, ochroborbone (1), along with five known alkaloids (2–6), were isolated from the stems and leaves of Ochrosia borbonica. Among them, ochroborbone (1) is a rare C17-nor monoterpenoid indole alkaloid, and the known compounds (2-6) were isolated from Ochrosia for the first time. These structures were established on the basis of extensive spectroscopic methods. All isolated compounds were evaluated for their cytotoxicities against five human cancer cell lines: HL-60, SMMC-7721, A-549, MCF-7 and SW480 in vitro. Compounds 1 and 2 exhibited inhibitory effects with IC50 values comparable with those of cisplatin.

scholarly journals Molecular Structure, In Vitro Anticancer Study and Molecular Docking of New Phosphate Derivatives of Betulin

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 737
Author(s):  
Elwira Chrobak ◽  
Maria Jastrzębska ◽  
Ewa Bębenek ◽  
Monika Kadela-Tomanek ◽  
Krzysztof Marciniec ◽  
...  
Keyword(s):  
Molecular Structure ◽  
Cell Lines ◽  
Human Cancer ◽  
Amelanotic Melanoma ◽  
Human Cancer Cell Lines ◽  
Ic50 Values ◽  
C 32 ◽  
New Compounds ◽  
Derivatives Of

A series of 30-diethylphosphate derivatives of betulin were synthesized and evaluated for their in vitro cytotoxic activity against human cancer cell lines, such as amelanotic melanoma (C-32), glioblastoma (SNB-19), and two lines of breast cancer (T47D, MDA-MB-231). The molecular structure and activities of the new compounds were also compared with their 29-phosphonate analogs. Compounds 7a and 7b showed the highest activity against C-32 and SNB-19 cell lines. The IC50 values for 7a were 2.15 and 0.91 μM, and, for 7b, they were 0.76 and 0.8 μM for the C-32 and SNB-19 lines, respectively. The most potent compounds, 7a and 7b, were tested for their effects on markers of apoptosis, such as H3, TP53, BAX, and BCL-2. For the whole series of phosphate derivatives, a lipophilicity study was performed, and the ADME parameters were calculated. The most active products were docked to the active site of the EGFR protein. The relative binding affinity of selected phosphate betulin derivatives toward EGFR was compared with standard erlotinib on the basis of ChemScore and KDEEP score. Positively, all derivatives docked inside the cavity and showed significant interactions. Moreover, a molecular dynamics study also reveals that ligands 7a,b form stable complexes and the plateau phase started after 7 ns.

Novel Artemisinin-Derived Dimers: Synthesis and Evaluation of Anti-cancer Activities

2016 ◽  
Vol 14 (1) ◽  
pp. 102-111 ◽  
Author(s):  
Vu Tuan Kien ◽  
Le Huy Binh ◽  
Phan Hai Phong ◽  
Doan Thi Hien ◽  
Nguyen Thi Thuy My ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Anticancer Compounds ◽  
Human Cancer Cell Lines ◽  
Ic50 Values ◽  
Mcf 7

In continuation of our study on anticancer compounds, a series of novel artemisinin dimers have been synthesized and evaluated for their cytotoxic effects against three human cancer cell lines, including HepG2 (liver cancer), MCF-7(breast cancer) and HL-60 (leukemia cancer). The assay results showed that most of the compounds displayed inhibitory effects against all three human cancer cell lines tested, and seemed to be more cytotoxic toward the blood cancer cells (HL-60) than liver (HepG2), and breast (MCF-7) cancer cells. Among the synthesized artemisinin dimers, the compound 10d with a double bond bridge exhibited the most potent cytotoxicity with IC50 values of 5.08, 4.82 and 1.32 µg/mL against the HepG2, MCF-7, and HL-60 cell lines, respectively.

scholarly journals Synthesis and Characterization of New Series of 1,3-5-Triazine Hydrazone Derivatives with Promising Antiproliferative Activity

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2708 ◽  
Author(s):  
Hessa H. Al Rasheed ◽  
Azizah M. Malebari ◽  
Kholood A. Dahlous ◽  
Ayman El-Faham
Keyword(s):  
Cell Lines ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Human Cancer Cell Lines ◽  
Triazine Derivatives ◽  
Ic50 Values ◽  
Hct 116 ◽  
Benzaldehyde Derivatives ◽  
Mcf 7

A new series of s-triazine hydrazone derivatives was prepared based on the reaction of 6-hydrazino-2,4-disubstituted-s-triazine with p-substituted benzaldehyde derivatives using a straightforward synthetic pathway. The antiproliferative activity of all synthesized compounds was evaluated against two human cancer cell lines; breast cancer MCF-7 and colon carcinoma HCT-116 using MTT assay. Among all, 11 compounds have shown strong to moderate antiproliferative activity with IC50 values in the range 1.01–18.20 µM in MCF-7 and 0.97–19.51 µM in HCT-116. The best results were obtained with 4,4’-(6-(2-(pyridin-2-ylmethylene)hydrazinyl)-1,3,5-triazine-2,4-diyl) dimorpholine 11 (IC50 = 1.0 µM and 0.98 µM in MCF-7 and HCT-116 cell lines, respectively). The substituents on the s-triazine core as well as the substituent at the benzylidene moiety have a great effect on the antiproliferative activity. Whereas compounds containing dimorpholino-s-triazine derivatives 8a–e showed more potent antiproliferative in MCF-7 compared to their analogs 7a–f (compounds containing two-piperidine rings), compounds containing one piperidine and one morpholine ring 9a–f showed better IC50 values in the range 10.4–22.2 µM. On the other hand, compounds containing two-piperidine rings 7a–f showed more potent antiproliferative in HCT-116 (IC50 values in the range 8.8–19.5 µM) than their analogs 8a–e and 9a–f.

Design, Synthesis and Anticancer Evaluation of Acetamides Comprising 1,2,3-triazole, 1,3,4-thiadiazole and Isothiazolo[4,3-b]pyridine Rings

2020 ◽  
Vol 17 (11) ◽  
pp. 864-871 ◽  
Author(s):  
Shaik Shahinshavali ◽  
Nuthalapati Poojith ◽  
Venkat Rao Guttikonda ◽  
Reddymasu Sreenivasulu ◽  
Mandava Venkata Basaveswara Rao
Keyword(s):  
Breast Cancer ◽  
Human Cancer ◽  
Positive Control ◽  
Pyridine Derivatives ◽  
Anticancer Activities ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Ic50 Values ◽  
A549 Lung ◽  
Mcf 7

We have synthesized a library of new 1,2,3-triazole incorporated 1,3,4-thiadiazoleisothiazolo[ 4,3-b]pyridine derivatives 12a-j and have screened these products for their anticancer activities against four human cancer cell lines such as MCF-7 (breast cancer), A549 (lung cancer), DU-145 (prostate cancer), and MDA MB-231 (breast cancer) using MTT assay with etoposide as a positive control. Among them, compound 12e has shown excellent activities against MCF-7, A549, DU-145, and MDA-MB-231 with IC50 values of 0.53±0.055 μM, 0.18±0.077 μM, 0.10±0.082 μM, and 0.92±0.041 μM, respectively.

Synthesis of New Zerumbone Hydrazones and Their In vitro Anticancer Activity

2020 ◽  
Vol 16 ◽  
Author(s):  
Vu Van Vu ◽  
Tran Khac Vu
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Cytotoxic Effects ◽  
Human Cancer Cell Lines ◽  
Ic50 Values ◽  
Bioassay Result ◽  
Mcf 7

Background: A series of new zerumbone hydrazones 5a-f and 9a-f have been synthesized via an in situ procedure in high yields. The structure of synthesized compounds has been confirmed using 1H, 13C NMR and HR-MS. The bioassay result showed that several compounds exhibited cytotoxic effects against three human cancer cell lines including HepG-2, SK-LU-1 and MCF-7. Compound 9a showed the best cytotoxic effect against HepG-2, SK-LU-1 and MCF-7 with IC50 values of 8.20, 6.66 and 9.35 µM, respectively. Objective: This study aims at developing new zerumbone hydrazones as anticancer agents based on zerumbone, a natural compound wildly growing in Vietnam. Method: A series of new zerumbone hydrazones was designed, synthesized and evaluated for cytotoxicity against three human cancer cell lines, including HepG-2, MCF-7 and SKLu-1 using MTT method. Results: The bioassay result showed that several compounds exhibited cytotoxic effects against three human cancer cell lines including HepG-2, SK-LU-1 and MCF-7. Especially, compound 9a displayed the best cytotoxic effect against HepG-2, SK-LU-1 and MCF-7 with IC50 values of 8.20, 6.66 and 9.35 µM, respectively. Results: The bioassay result showed that several compounds exhibited cytotoxic effects against three human cancer cell lines including HepG-2, SK-LU-1 and MCF-7. Especially, compound 9a displayed the best cytotoxic effect against HepG-2, SK-LU-1 and MCF-7 with IC50 values of 8.20, 6.66 and 9.35 µM, respectively. Conclusion: The research results suggest that some compounds could be considered as a lead for future design of zerumbone hydrazones in which bio-isosteric replacements in ortho position of the phenyl ring could be performed to improve the cytotoxic activity.

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