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.

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 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 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.

Synthesis and Investigation of the Role of Benzopyran Dihydropyrimidinone Hybrids in Cell Proliferation, Migration and Tumor Growth

2019 ◽  
Vol 19 (2) ◽  
pp. 276-288 ◽  
Author(s):  
Ashutosh K. Dash ◽  
Debasis Nayak ◽  
Nazar Hussain ◽  
Mubashir J. Mintoo ◽  
Sumera Bano ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Tumor Growth ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Cancer Cell Proliferation ◽  
Human Cancer Cell Lines ◽  
Cell Scattering ◽  
Ic50 Values

Background: Cancer is the second leading cause of mortality worldwide after heart diseases, and lung cancer is the topmost cause of all cancer-related deaths in both sexes. Dihydropyrimidinones (DHPMs) are medicinally important class of molecules with diverse pharmacological activities including anticancer activity. The present study focuses on the molecular hybridization of novel Benzopyran with Dihydropyrimidinone and evaluation of the resulting hybrids for cancer cell proliferation, migration and tumor growth. Methods: We have synthesized a focused library of dihydropyrimidinone benzopyran hybrids (compounds 1-11) by joining the aromatic as well as pyran portions of the benzopyran core with dihydropyrimidinone. All the synthesized hybrid molecules were evaluated for their cytotoxic activities against a panel of four human cancer cell lines of diverse tissue origin, viz: A549 (lung carcinoma), MCF7 (mammary gland adenocarcinoma), HCT-116 (colorectal carcinoma), and PANC-1 (pancreatic duct carcinoma) with the help of MTT cell viability assay. A structure-activity relationship was made on the basis of IC50 values of different hybrids. Effect on cell proliferation was examined through colony formation assay, reactive oxygen species generation and mitochondrial membrane potential studies. Wound healing assays and cell scattering assays were employed to check the effect on cell migration. Western blotting experiments were performed to find out the molecular mechanism of action and anti-tumor studies were carried out to evaluate the in vivo efficacy of the selected lead molecule. Results: Two types of novel hybrids were synthesized efficiently from benzopyran aldehydes, ethylacetoacetate and urea under heteropolyacid catalysis. Compound 3 was found to be the most potent hybrid among the synthesized compounds with consistent cytotoxic activities against four human cancer cell lines (IC50 values: 0.139 - 2.32 μM). Compound 3 strongly inhibited proliferation abilities of A549 cells in colony formation assay. Compound 3 exerted oxidative stress-mediated mitochondrial dysfunction, in which mitochondrial reactive oxygen species (ROS) generation as a mechanism of its anti-proliferative effects was analysed. Further, the molecule abrogated migration and cell scattering properties of aggressive PANC-1 cells. Mechanistic studies revealed that compound 3 modulated NF-kB expression and its downstream oncogenic proteins involved in cancer cell proliferation and invasion. Finally, compound 3 confirmed its in vivo anti-tumor efficacy; there observed 41.87% tumor growth inhibition at a dose of 30 mg/kg/body weight against a mouse model of Ehrlich solid tumor. Conclusion: Our study unravels a potential anticancer lead (compound 3) from DHPMs that have opened up new research avenues for the development of promising anticancer therapeutic agents.

Antarones A and B, Two Polyketides from an Endophytic Penicillium antarcticum

2008 ◽  
Vol 63 (7) ◽  
pp. 909-914 ◽  
Author(s):  
Yoshihito Shiono ◽  
Yumi Seino ◽  
Takuya Koseki ◽  
Tetsuya Murayama ◽  
Ken-ichi Kimura
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Endophytic Fungus ◽  
Brine Shrimp ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Spectroscopic Methods ◽  
Human Cancer Cell ◽  
Brine Shrimp Lethality ◽  
Human Cancer Cell Lines

Two new polyketides, antarones A and B, were isolated from the endophytic fungus Penicillium antarcticum. Their structures were determined by spectroscopic methods. Their general toxicity and cytotoxicity were evaluated, respectively, by brine shrimp lethality and cytotoxicity assay with human cancer cell lines. Neither antarones A nor B exhibited activity at the concentration of 100 μM.

New Sulfoxide-Containing Derivatives from the Resin of Ferula sinkiangensis

Planta Medica ◽  
2021 ◽  
Author(s):  
Junchi Wang ◽  
Haoli Yan ◽  
Xiaoshuang Huo ◽  
Lingyu Li ◽  
Huijuan Wang ◽  
...  
Keyword(s):  
Human Cancer ◽  
Cytotoxic Activities ◽  
Spectroscopic Methods ◽  
Human Cancer Cell ◽  
Addition Compound ◽  
Human Cancer Cell Lines ◽  
Nitric Oxide Release ◽  
Tnf Α ◽  
Ic50 Values ◽  
Ferula Sinkiangensis

AbstractFour undescribed sulfoxide-containing derivatives, sinkiangenoxides A and B, (2Z, 4E)-sinkiangenoxide C, and (2E, 4E)-sinkiangenoxide C (1 – 4), and one known compound, 1-(methylthio)propyl (E)-1-propenyl disulfide (5), were isolated from the resin of Ferula sinkiangensis. Their structures were determined based on spectroscopic methods, including IR, UV, HRESIMS, NMR, and CD analysis. Compounds 2 – 4 showed moderate cytotoxic activities against four human cancer cell lines with IC50 values ranging from 15.0 to 40.3 µM. Sinkiangenoxide B (2) was shown to induce apoptosis in HepG2 cells. In addition, compound 5 effectively attenuated lipopolysaccharide-induced nitric oxide release and TNF-α, IL-1β, IL-6, and IL-10 expression.

scholarly journals Phytochemical, antioxidant, brine shrimp lethality and antiproliferative analyses of Solanum dasyphyllum schum. & thonn. leaf and fruit extracts [Solanaceae]

2019 ◽  
pp. 13-17
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Brine Shrimp ◽  
Colorimetric Assay ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Brine Shrimp Lethality ◽  
Human Cancer Cell Lines ◽  
Fruit Extracts

Introduction: Solanum dasyphyllum is an edible egg plant belonging to Solanaceae family. The fruit and leaf of S. dasyphyllum are traditionally used to relief swellings and oedema. In this study, we investigated the phytochemical constituents, DPPH antioxidant activity, brine shrimp lethality and cytotoxicity on human cancer cell lines of the leaf and fruit extracts of S. dasyphyllum. Methods: The leaf and fruit extracts of S. dasyphyllum were subjected to phytochemical screening, in vitro antioxidant assay using DPPH, brine shrimp lethality (BSL) bioassay and MTT colorimetric assay using human cancer cell lines. Results: The leaf and fruit of S. dasyphyllum tested positive for the presence of alkaloids, tannins, saponins and cardiac glycosides. Extract of the leaf (IC50 of 274.6±2.45 and LC50 of 406.0±7.41) and fruit (278.2±2.68 µg/mL and 766.7±9.14 µg/mL) displayed weak DPPH radical scavenging activity and brine shrimp lethality (BSL) compared to ascorbic acid (IC50=20.2±0.36 µg/mL) and cyclophosphamide (LC50 of 98.76±0.15 µg/mL) respectively. Compared to the fruits extracts, the leaf extract was found to be more cytotoxic with CC50 of 28.46±1.42, 2.99±0.15 and 23.33±2.7 µg/mL on the human cancer cell lines Rd, Hep-2c and the normal cell line, Vero, respectively in the MTT colorimetric assay. Significance: The leaf and fruit extracts of S. dasyphyllum had weak DPPH activity and elicited mild cytotoxicity in BSL assay. However, the leaf extract of displayed a higher cytotoxicity than the fruit extract on human cancer line used in the study.

scholarly journals Mollicellins O–R, Four New Depsidones Isolated from the Endophytic Fungus Chaetomium sp. Eef-10

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3218 ◽  
Author(s):  
Jinkui Ouyang ◽  
Ziling Mao ◽  
Hui Guo ◽  
Yunying Xie ◽  
Zehua Cui ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Radical Scavenging ◽  
Antibacterial Activities ◽  
Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Ic50 Values

Four new depsidones, mollicellins O–R (compounds 1–4), along with three known compounds 5–7, were isolated from cultures of the fungus Chaetomium sp. Eef-10, an endophyte isolated from Eucalyptus exserta. The structures of the new compounds were elucidated by analysis of the 1D and 2D NMR and HR-ESI-MS spectra. The known compounds were identified by comparison of their spectral data with published values. Compounds 1–7 were evaluated for antibacterial activities against Staphylococcus aureus (sensitive and resistant strains), Escherichia coli, Agrobacterium tumefaciens, Salmonella typhimurium, Pseudomonas lachrymans, Ralstonia solanacearum, Xanthomonas vesicatoria and cytotoxic activities against two human cancer cell lines (HepG2 and Hela). Mollicellin H (6) displayed best antibacterial activity, with IC50 values of 5.14 µg/mL against S. aureus ATCC29213 and 6.21 µg/mL against S. aureus N50, MRSA, respectively. Mollicellin O (1) and mollicellin I (7) also exhibited antibacterial activities against S. aureus ATCC29213 and S. aureus N50. Mollicellin G (5) was active against both two human cancer cell lines, with IC50 values of 19.64 and 13.97 µg/mL while compounds 6 and 7 only showed cytotoxic activity against one cell line. In addition, mollicellin O (1) showed antioxidant activity based on DPPH radical scavenging, with an IC50 value of 71.92 µg/mL.

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.  

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