Cytochalasan Alkaloids as TRAIL Sensitizers from an Endophytic Fungus Chaetomium sp.

Planta Medica ◽  
2021 ◽  
Author(s):  
Hanli Ruan ◽  
Ying Gao ◽  
Ruihua Mao ◽  
Ye Liu ◽  
Ming Zhou

Two new cytochalasans with a rare 6/6/5/5/7 pentacyclic ring system, named chaetoconvosins C−D (1−2), together with two known congeners (3−4), were isolated from the fermentation of an endophytic fungus, Chaetomium sp. SG-01, harbored in the fibrous roots of Schisandra glaucescens Diels. Their structures including the absolute configuration were elucidated by extensive spectroscopic (HRESIMS, NMR, and ECD) and X-ray crystallographic analyses. The TRAIL sensitivity of 1–4 in a TRAIL-resistant HT29 colorectal cancer cell line was evaluated, which revealed that co-treatment of 1–4 at 50 µM with TRAIL (150 ng/mL) reduced the HT29 cell viability by 19.0%, 24.1%, 17.9%, and 15.5%, respectively, compared to treatment with 1–4 alone.

2014 ◽  
Vol 10 ◽  
pp. 2677-2682 ◽  
Author(s):  
Zhi Kai Guo ◽  
Rong Wang ◽  
Wei Huang ◽  
Xiao Nian Li ◽  
Rong Jiang ◽  
...  

An unusual C18 norditerpenoid, aspergiloid I (1), was isolated from the culture broth of Aspergillus sp. YXf3, an endophytic fungus derived from Ginkgo biloba. Its structure was unambiguously established by analysis of HRMS–ESI and spectroscopic data, and the absolute configuration was determined by low-temperature (100 K) single crystal X-ray diffraction with Cu Kα radiation. This compound is structurally characterized by a new carbon skeleton with an unprecedented 6/5/6 tricyclic ring system bearing an α,β-unsaturated spirolactone moiety in ring B, and represents a new subclass of norditerpenoid, the skeleton of which is named aspergilane. The hypothetical biosynthetic pathway for 1 was also proposed. The cytotoxic, antimicrobial, anti-oxidant and enzyme inhibitory activities of 1 were evaluated.


2020 ◽  
Author(s):  
Md. Nur Alam ◽  
Mohammad Moni ◽  
Jun Yu ◽  
Philip Beale ◽  
Peter Turner ◽  
...  

Abstract Due to similar coordination chemistry of palladium and platinum, a large number of palladium compounds too have been investigated for their anticancer activity. In the present study we describe synthesis, characterization and anticancer activity of palladium complex [Bis(1,8-quinolato)palladium (II)], coded as NH3 against seven different cancer cell lines. NH3 is found to have higher antitumour activity than cisplatin against both parent ovarian A2780 cell line and cisplatin-resistant cell lines. Also, NH3 has the lowest IC50 value against HT-29 colorectal cancer cell line. The higher antitumour activity of NH3 is due to the presence of bulky 8-hydroxy-quinoline ligand thus reducing its reactivity. Proteomic study has identified significantly expressed proteins which have been validated through bioinformatics. NH3 has been found to be less toxic than cisplatin at 2.5 mg/kg and 5 mg/kg dosages on mice models. Binary combinations of NH3 with curcumin and epigallocatechin gallate (EGCG) have demonstrated dose and sequence dependent synergism in ovarian and colorectal cancer models. All of the preclinical studies indicate promising therapeutic potentiality of NH3 [Bis(1,8-quinolato)palladium (II) ] as an anticancer drug.


2021 ◽  
Vol 8 (1) ◽  
Author(s):  
Dany Muhammad Daffa ◽  
Muhammad Hasan Bashari ◽  
Eko Fuji Ariyanto ◽  
Tenny Putri ◽  
Nurul Qomarilla

Background: Colorectal cancer is the second leading cause of mortality and the most prevalent cancer worldwide. Most patients, who come with late-stage, have ineffective treatments and some side effects in chemotherapy. Aaptos suberitoides has potential anti-cancer effects due to its bioactive compounds such as aptamine. This study aimed to evaluate the migration inhibition effect of Aaptos suberitoides fraction in HCT-116 cell line.Methods: This study was an experimental study. Aaptos suberitoides specimen was taken in Tinjil Island and fractionated with ethyl acetate. HCT-116 cell line was added with Aaptos suberitoides fraction and cellular migration activity was observed in 48 hours of which the scratch assay was performed. The gap closure area was determined with ImageJ software.Results: The data showed that a low concentration of Aaptos suberitoides fraction inhibited migration activity in HCT-116 cell line as follow; 1 and 5 mg/L Aaptos suberitoides fraction inhibit 3-4 % cancer cell migration in 24 hours, and 10-11% inhibition in 48 hours, respectively. However, 10 mg/L fraction concentration only inhibited 7-14% of the migration effect.Conclusion: Aaptos suberitoides fraction suggests insignificant migration inhibition in colorectal cancer cells and only inhibits less than 15 % HCT-116 cell line.


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