scholarly journals AROMATASE INHIBITORY AND CYTOTOXIC ACTIVITIES OF CHEMICAL CONSTITUENTS FROM THE VIETNAMESE MEDICINAL PLANT BAN-CHI-LIEN (SCUTELLARIA BARBATA D. DON)

2017 ◽  
Vol 25 (2) ◽  
pp. 481-487 ◽  
Author(s):  
Do Thi Thao ◽  
Le Quang Huan ◽  
Do Khac Hieu ◽  
Nguyen Quyet Chien ◽  
Nguyen Van Hung
Keyword(s):  
Medicinal Plant ◽  
Human Cancer ◽  
Chemical Constituents ◽  
Positive Control ◽  
Cytotoxic Activities ◽  
Scutellaria Barbata ◽  
Human Cancer Cell Lines ◽  
Ic50 Value ◽  
Bioassay Guided Fractionation ◽  
Ic50 Values

Aromatase inhibitory and cytotoxic activities were determined for apigenin, luteolin and the new diterpene named scutebarbalactone VN, which were obtained by bioassay-guided fractionation and isolation from the methanol extract of the Vietnamese medicinal plant Banchi-lien (Scutellaria barbata D. Don). In the aromatase inhibition assay, an IC50 value of 3.36 mM was found for scutebarbalactone VN, while IC50  values of 7.2 mM and 7.95 mM were found for the positive controls aminoglutethimide and b-estradiol, respectively. In the cytotoxicity  assays using a panel of human cancer cell lines, scutebarbalactone VN showed promising anticancer activity with IC50  ranging from 2.15 to 8.3 mM compared with those of the positive control ellipticine ranging from 1.0 to 2.1 mM. Apigenin and luteolin were found to be inactive  in both assays.  

Six New neo-Clerodane Diterpenoids from Aerial Parts of Scutellaria barbata and Their Cytotoxic Activities

Planta Medica ◽  
2018 ◽  
Vol 84 (17) ◽  
pp. 1292-1299 ◽  
Author(s):  
Guo-Chun Yang ◽  
Jia-Hui Hu ◽  
Bing-Long Li ◽  
Huan Liu ◽  
Jia-Yue Wang ◽  
...  
Keyword(s):  
Cell Lines ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Cytotoxic Activities ◽  
Scutellaria Barbata ◽  
Human Cancer Cell Lines ◽  
Aerial Parts ◽  
Ic50 Values ◽  
Clerodane Diterpenoids

AbstractSix new neo-clerodane diterpenoids (1–6), scutebatas X – Z, A1-C1, along with twelve known ones (7–18) were obtained via the phytochemical investigation of the aerial parts of Scutellaria barbata. Their structures were established by detailed spectroscopic analysis. The absolute configurations of 1 and 2, as the representative members of this type, were identified based on a circular dichroic exciton chirality method. Moreover, in vitro cytotoxicity of compounds 1–6 were evaluated against three human cancer cell lines (SGC-7901, MCF-7, and A-549) using the MTT method. Compound 6 showed cytotoxic activities against all the three cell lines with IC50 values of 17.9, 29.9, and 35.7 µM, respectively.

scholarly journals Structurally Simple Phenanthridine Analogues Based on Nitidine and Their Antitumor Activities

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 437
Author(s):  
Shu-Qin Qin ◽  
Lian-Chun Li ◽  
Jing-Ru Song ◽  
Hai-Yun Li ◽  
Dian-Peng Li
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
A549 Cells ◽  
Anticancer Activities ◽  
Human Cancer Cell Lines ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Diphenyl Tetrazolium Bromide ◽  
Conjugated Compounds

A series of novel structurally simple analogues based on nitidine was designed and synthesized in search of potent anticancer agents. The antitumor activity against human cancer cell lines (HepG2, A549, NCI-H460, and CNE1) was performed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay in vitro. The results showed that some of them had good anticancer activities, especially derivatives with a [(dimethylamino)ethyl]amino side chain in the C-6 position. Planar conjugated compounds 15a, 15b, and 15c, with IC50 values of 1.20 μM, 1.87 μM, and 1.19 μM against CNE1 cells, respectively, were more active than nitidine chloride. Compound 15b and compound 15c with IC50 values of 1.19 μM and 1.37 μM against HepG2 cells and A549 cells demonstrated superior activities to nitidine. Besides, compound 5e which had a phenanthridinone core displayed extraordinary cytotoxicity against all test cells, particularly against CNE1 cells with the IC50 value of 1.13 μM.

scholarly journals Biological Activity and Chemical Constituents of Essential Oil and Extracts of Murraya microphylla

2015 ◽  
Vol 10 (9) ◽  
pp. 1934578X1501000
Author(s):  
Hai-Ning Lv ◽  
Ke-Wu Zeng ◽  
Bing-Yu Liu ◽  
Yun Zhang ◽  
Peng-Fei Tu ◽  
...  
Keyword(s):  
Essential Oil ◽  
Human Cancer ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Cytotoxic Activities ◽  
Active Components ◽  
Human Cancer Cell Lines ◽  
Total Oil ◽  
Promising Development ◽  
Carbazole Alkaloids

Murraya microphylla is the most closely related species to M. koenigii (Curry tree). Inspired by the traditional effects of M. koenigii, the antioxidant, anti-inflammatory, and cytotoxic activities of the essential oil and extracts of M. microphylla were evaluated for the first time. The light petroleum and chloroform extracts were found to be able to scavenge DPPH free radicals, inhibit linoleic acid peroxidation, and nitric oxide production, as well as to present cytotoxicity to the human cancer cell lines HepG2, Bel7402, Bel7403, and Hela, but the essential oil only showed moderate activities. Chemical analysis of the active extracts by LC-DAD-MSn indicated that carbazole alkaloids were the main constituents. GC-MS analysis of the essential oil resulted in identification of 91 constituents, representing 96.9% of the total oil, with ( E)-caryophyllene (18.4%) and terpinen-4-ol (12.6%) as the major constituents. These results demonstrate that M. microphylla has similar biological activities, as well as chemical constituents to M. koenigii, and the carbazole alkaloids were disclosed to be the main potential active components. A promising development as a flavor and potential therapeutic agent could thus be predicated for this plant.

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.

scholarly journals Cytotoxic Activities of Different Iranian Solanaceae and Lamiaceae Plants and Bioassay-Guided Study of an Active Extract from Salvia lachnocalyx

2017 ◽  
Vol 12 (10) ◽  
pp. 1934578X1701201 ◽  
Author(s):  
Hossein H. Mirzaei ◽  
Omidreza Firuzi ◽  
Ian T. Baldwin ◽  
Amir Reza Jassbi
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Active Species ◽  
Cytotoxic Activities ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Bioassay Guided Fractionation ◽  
Cytotoxic Compounds

Methanol (MeOH), dichloromethane (DCM) and 80% MeOH extractions of fourteen medicinal plants of the families Solanaceae and Lamiaceae collected from different area of Iran were tested for their cytotoxic potential against MOLT-4 human cancer cell lines. Cytotoxicity of the tested plants indicated that 11 plants had one or two active extracts (IC50 ≤50): MeOH extracts of the shoots of Thymus trautvetteri, Solanum luteum and stems of Lycium shawii; DCM extracts of the shoots of Thymus kotschyanus, Salvia persepolitana, Ballota aucheri, Nepeta glomerulosa, Hyoscyamus tenuicaulis, Salvia lachnocalyx, Salvia sharifii as well as the stems of Salvia verticillata and the roots of Salvia multicaulis and S. lachnocalyx; 80% MeOH extracts of the shoots of T. trautvetteri, S. luteum and the stems of L. shawii. The DCM extract of the aerial parts of S. lachnocalyx as one of the most active species was subjected to the cytotoxic bioassay-guided fractionation and purification using combination of chromatography methods. The bioassay-guided fractionation of DCM extract of the shoots of S. lachnocalyx led to the isolation of two cytotoxic compounds: (2 Z,6 Z,10 Z,14 E)-geranylfarnesol (1), a novel natural product, and spathulenol (2). Both of the isolated compounds, especially 1 (IC50 range: 9.6 −20.2 μg/mL), showed good cytotoxic effects against 3 human cancer cell lines, MOLT-4, MCF-7 and HT-29.

scholarly journals Chemical constituents and cytotoxicity of Aspidistra letreae

2020 ◽  
Vol 129 (1B) ◽  
pp. 31-39
Author(s):  
Duc Viet Ho ◽  
Hanh Nhu Thi Hoang ◽  
Khue Minh Vo ◽  
Anh Tuan Le ◽  
Hoai Thi Nguyen
Keyword(s):  
Human Cancer ◽  
Chemical Constituents ◽  
Hep G2 ◽  
Human Cancer Cell Lines ◽  
Phytochemical Investigation ◽  
Ic50 Values ◽  
Reported Data ◽  
Whole Plants ◽  
First Time

A phytochemical investigation of whole Aspidistra letreae plants led to the isolation of 2H-chromen-2-one (1), α-tocopherol (2), (E)-phytol (3), asparenydiol (4) and (25S)-spirost-1β,3α,5β-triol (5). Their structures were determined on the basis of NMR spectral evidences and in comparison with the reported data. Of these, asparenydiol (4) was isolated from the genus Aspidistra for the first time. This is also the first report on the separation and structural determination of (25S)-spirost-1β,3α,5β-triol (5) as a pure compound. The methanol extract from the whole plants of Aspidistra letreae exhibits moderate cytotoxicity against the LU-1, HeLa, MDA-MB-231, Hep-G2, and MKN-7 human cancer cell lines with IC50 values ranging from 52.58 ± 3.65 to 64.78 ± 4.89 μg/mL.

scholarly journals Cyclodepsipeptides and Sesquiterpenes from Marine-Derived Fungus Trichothecium roseum and Their Biological Functions

Marine Drugs ◽  
2018 ◽  
Vol 16 (12) ◽  
pp. 519 ◽  
Author(s):  
Yuan-Ming Zhou ◽  
Guang-Lin Ju ◽  
Lin Xiao ◽  
Xiang-Fei Zhang ◽  
Feng-Yu Du
Keyword(s):  
Brine Shrimp ◽  
Human Cancer ◽  
Crystallographic Analysis ◽  
Heterodera Avenae ◽  
Cytotoxic Activities ◽  
Brine Shrimp Lethality ◽  
Human Cancer Cell Lines ◽  
Trichothecium Roseum ◽  
Ic50 Values ◽  
Ld50 Value

On the basis of the ‘one strain, many compounds’ (OSMAC) strategy, chemical investigation of the marine-derived fungus Trichothecium roseum resulted in the isolation of trichomide cyclodepsipeptides (compounds 1–4) from PDB medium, and destruxin cyclodepsipeptides (compounds 5–7) and cyclonerodiol sesquiterpenes (compounds 8–10) from rice medium. The structures and absolute configurations of novel (compounds 1, 8, and 9) and known compounds were elucidated by extensive spectroscopic analyses, X-ray crystallographic analysis, and ECD calculations. All isolated compounds were evaluated for cytotoxic, nematicidal, and antifungal activities, as well as brine shrimp lethality. The novel compound 1 exhibited significant cytotoxic activities against the human cancer cell lines MCF-7, SW480, and HL-60, with IC50 values of 0.079, 0.107, and 0.149 μM, respectively. In addition, it also showed significant brine shrimp lethality, with an LD50 value of 0.48 μM, and moderate nematicidal activity against Heterodera avenae, with an LC50 value of 94.9 μg/mL. This study constitutes the first report on the cytotoxic and nematicidal potential of trichomide cyclodepsipeptides.

β-Dihydroagarofuran-type sesquiterpenoids from the stems of Celastrus orbiculatus with their cytotoxic activities

2021 ◽  
Vol 19 ◽  
Author(s):  
Yong Hua Lin ◽  
Bao Yan Zhang ◽  
Zhi Chao Chen ◽  
Jian Feng Wei
Keyword(s):  
Cytotoxic Activity ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Celastrus Orbiculatus ◽  
Physico Chemical ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Hct 116 ◽  
Hct 116 Cells

Abstract: A new β-dihydroagarofuran-type sesquiterpenoid named 1α,2α,5α,11-tetraacetoxy-8α-(trans-p-coumaroyl)-β-dihydroagarofuran (1), together with five known compounds (2-6) were isolated from the CHCl3-soluble extract of the stems of Celastrus orbiculatus. The structure of new compound was elucidated with spectroscopic physico-chemical analyses. All isolates were evaluated for in vitro cytotoxic activity against four human cancer lines including HepG2, MCF-7, A549 and HCT-116 cells. Among them, compounds 1 and 6 showed potent cytotoxic activities on HepG2 cells with IC50 values of 8.78 ± 2.31 and 10.28 ± 1.15 μM, respectively. In addition, compound 6 exhibited significant cytotoxic activity on HCT-116 cells with IC50 value of 6.37 ± 2.52 μM

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 Cytospyrone and Cytospomarin: Two New Polyketides Isolated from Mangrove Endophytic Fungus, Cytospora sp.

Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4224
Author(s):  
Chengwen Wei ◽  
Qin Deng ◽  
Mengyu Sun ◽  
Jing Xu
Keyword(s):  
Density Functional ◽  
Human Cancer ◽  
Optical Rotation ◽  
Cancer Cell Line ◽  
Positive Control ◽  
Functional Theory ◽  
Spectroscopic Analyses ◽  
Mangrove Endophytic Fungus ◽  
Ic50 Value ◽  
Ic50 Values

Two new polyketides, cytospyrone (1), cytospomarin (2), together with three known metabolites dimethoxyphtalide (3), integracin A (4) and integracin B (5), were isolated from the culture of Cytospora sp. from the Chinese mangrove Ceriops tagal. Their structures were elucidated by extensive spectroscopic analyses and time dependent density functional theory (TDDFT), calculation of electronic circular dichroism (ECD) and optical rotation (OR) data. Compound 2 displayed weak inhibitory activity against Escherichia coli GIM1.201 (minimum inhibitory concentration (MIC) value of 0.35 mM). Compounds 4 and 5 displayed significant cytotoxicity against human cancer cell line HepG2 (IC50 values of 5.98 ±  0.12 µM and 9.97 ± 0.06 µM, respectively), more potent than the positive control 5-fluorouracil (IC50 value of 43.50 ± 3.69 µM).

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