Characterization of NVX-207, a novel betulinic acid-derived anti-cancer compound

2009 ◽  
Vol 39 (5) ◽  
pp. 384-394 ◽  
Author(s):  
M. Willmann ◽  
V. Wacheck ◽  
J. Buckley ◽  
K. Nagy ◽  
J. Thalhammer ◽  
...  
Keyword(s):  
Betulinic Acid ◽  
Anti Cancer

scholarly journals Synthesis, Characterization of Liposomes Modified with Biosurfactant MEL-A Loading Betulinic Acid and Its Anticancer Effect in HepG2 Cell

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3939 ◽  
Author(s):  
Qin Shu ◽  
Jianan Wu ◽  
Qihe Chen
Keyword(s):  
Betulinic Acid ◽  
Hepg2 Cells ◽  
Lipid A ◽  
Clinical Applications ◽  
Dose Effect ◽  
Anticancer Effect ◽  
Mannosylerythritol Lipid ◽  
Anti Cancer ◽  
Effect Relation

As a novel natural compound delivery system, liposomes are capable of incorporating lipophilic bioactive compounds with enhanced compound solubility, stability and bioavailability, and have been successfully translated into real-time clinical applications. To construct the soy phosphatidylcholine (SPC)–cholesterol (Chol) liposome system, the optimal formulation was investigated as 3:1 of SPC to Chol, 10% mannosylerythritol lipid-A (MEL-A) and 1% betulinic acid. Results show that liposomes with or without betulinic acid or MEL-A are able to inhibit the proliferation of HepG2 cells with a dose-effect relation remarkably. In addition, the modification of MEL-A in liposomes can significantly promote cell apoptosis and strengthen the destruction of mitochondrial membrane potential in HepG2 cells. Liposomes containing MEL-A and betulinic acid have exhibited excellent anticancer activity, which provide factual basis for the development of MEL-A in the anti-cancer applications. These results provide a design thought to develop delivery liposome systems carrying betulinic acid with enhanced functional and pharmaceutical attributes.

scholarly journals Discovery and Mechanistic Characterization of a Select Modulator of AhR-regulated Transcription (SMAhRT) with Anti-cancer Effects

APOPTOSIS ◽  
2021 ◽  
Author(s):  
Edmond Francis O’Donnell ◽  
Hyo Sang Jang ◽  
Daniel F Liefwalker ◽  
Nancy I Kerkvliet ◽  
Siva Kumar Kolluri
Keyword(s):  
Anti Cancer

scholarly journals Molecular and Pharmacological Characterization of the Interaction between Human Geranylgeranyltransferase Type I and Ras-Related Protein Rap1B

2021 ◽  
Vol 22 (5) ◽  
pp. 2501
Author(s):  
Sonja Hinz ◽  
Dominik Jung ◽  
Dorota Hauert ◽  
Hagen S. Bachmann
Keyword(s):  
Protein Function ◽  
Tumor Development ◽  
Cysteine Residue ◽  
Type I ◽  
Pharmacological Characterization ◽  
Anti Cancer ◽  
And Function ◽  
Caax Motif ◽  
Important Drug

Geranylgeranyltransferase type-I (GGTase-I) represents an important drug target since it contributes to the function of many proteins that are involved in tumor development and metastasis. This led to the development of GGTase-I inhibitors as anti-cancer drugs blocking the protein function and membrane association of e.g., Rap subfamilies that are involved in cell differentiation and cell growth. In the present study, we developed a new NanoBiT assay to monitor the interaction of human GGTase-I and its substrate Rap1B. Different Rap1B prenylation-deficient mutants (C181G, C181S, and ΔCQLL) were designed and investigated for their interaction with GGTase-I. While the Rap1B mutants C181G and C181S still exhibited interaction with human GGTase-I, mutant ΔCQLL, lacking the entire CAAX motif (defined by a cysteine residue, two aliphatic residues, and the C-terminal residue), showed reduced interaction. Moreover, a specific, peptidomimetic and competitive CAAX inhibitor was able to block the interaction of Rap1B with GGTase-I. Furthermore, activation of both Gαs-coupled human adenosine receptors, A2A (A2AAR) and A2B (A2BAR), increased the interaction between GGTase-I and Rap1B, probably representing a way to modulate prenylation and function of Rap1B. Thus, A2AAR and A2BAR antagonists might be promising candidates for therapeutic intervention for different types of cancer that overexpress Rap1B. Finally, the NanoBiT assay provides a tool to investigate the pharmacology of GGTase-I inhibitors.

Synthesis and characterization of fluorescent chitosan–ZnSe/ZnS nanoparticles for potential drug carriers

RSC Advances ◽  
2015 ◽  
Vol 5 (49) ◽  
pp. 38810-38817 ◽  
Author(s):  
Yeping Li ◽  
Jingbo Xu ◽  
Yun Xu ◽  
Liying Huang ◽  
Junli Wang ◽  
...  
Keyword(s):  
Quantum Dots ◽  
Drug Carrier ◽  
Drug Carriers ◽  
Cancer Drug ◽  
Synthesis And Characterization ◽  
Potential Drug ◽  
Zns Nanoparticles ◽  
New Approach ◽  
Anti Cancer

The objective of the study is to describe a new approach of combining quantum dots into chitosan as an anti-cancer drug carrier.

A review on phyto-pharmacology of Oxalis corniculata

2021 ◽  
Vol 24 ◽  
Author(s):  
Iqra Sarfraz ◽  
Azhar Rasul ◽  
Ghulam Hussain ◽  
Muhammad Ajmal Shah ◽  
Bushra Nageen ◽  
...  
Keyword(s):  
Clinical Trials ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Current Effort ◽  
Isolation And Characterization ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Anti Fungal ◽  
Warm Temperate

: Oxalis corniculata (Oxalidaceae) is a small decumbent and delicate appearing medicinal herb flourishing in warm temperate and tropical domains such as Pakistan and India. Main bioactive chemical constituents of Oxalis plant include several alkaloids, flavonoids, terpenoids, cardiac glycosides, saponins, phlobatannins along with steroids. Due to its polyphenolic, glycosides and flavonoid profile, it is proved to be protective in numerous ailments and exhibit various biological activities such as anti-fungal, anti-cancer, anti-oxidant, anti-bacterial, anti-diabetic, and cardioprotective. Moreover, bioactive phytochemicals from this plant possess significant wound healing potential. Our current effort intends to emphasize on the immense significance of this plant species, which have not been the subject matter of clinical trials and effective pharmacological studies, even though its favored usage has been stated. This review proposes that Oxalis corniculata possess potential for the cure of various diseases, however, further researches on isolation and characterization of bioactive compounds along with pre-clinical trials are compulsory to figure out its pharmacological applications.

Characterization of cannabinoid receptors expressed in Ewing sarcoma TC-71 and A-673 cells as potential targets for anti-cancer drug development

Life Sciences ◽  
2021 ◽  
Vol 285 ◽  
pp. 119993
Author(s):  
Amal M. Shoeib ◽  
Azure L. Yarbrough ◽  
Benjamin M. Ford ◽  
Lirit N. Franks ◽  
Alicja Urbaniak ◽  
...  
Keyword(s):  
Drug Development ◽  
Ewing Sarcoma ◽  
Cannabinoid Receptors ◽  
Cancer Drug ◽  
Anti Cancer

scholarly journals Tyrosine Kinase ROR1 as a Target for Anti-Cancer Therapies

2021 ◽  
Vol 11 ◽  
Author(s):  
Yuming Zhao ◽  
Dengyang Zhang ◽  
Yao Guo ◽  
Bo Lu ◽  
Zhizhuang Joe Zhao ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Malignant Tumors ◽  
Wnt Signaling Pathway ◽  
Cancer Therapies ◽  
Anti Cancer ◽  
Functional Features ◽  
Survival Signaling ◽  
Preclinical And Clinical Studies ◽  
Canonical Wnt

Receptor tyrosine kinase ROR1 plays an essential role in embryogenesis and is overexpressed in many types of malignant tumors. Studies have demonstrated that it plays an important role in oncogenesis by activating cell survival signaling events, particularly the non-canonical WNT signaling pathway. Antibody-based immunotherapies targeting ROR1 have been developed and evaluated in preclinical and clinical studies with promising outcomes. However, small molecule inhibitors targeting ROR1 are underappreciated because of the initial characterization of ROR1 as a peusdokinase. The function of ROR1 as a tyrosine kinase remains poorly understood, although accumulating evidence have demonstrated its intrinsic tyrosine kinase activity. In this review, we analyzed the structural and functional features of ROR1 and discussed therapeutic strategies targeting this kinase.

Characterization of the anti-cancer-cell parasporal proteins of aBacillus thuringiensisisolate

2000 ◽  
Vol 46 (10) ◽  
pp. 913-919 ◽  
Author(s):  
Satoko Yamashita ◽  
Tetsuyuki Akao ◽  
Eiichi Mizuki ◽  
Hiroyuki Saitoh ◽  
Kazuhiko Higuchi ◽  
...  
Keyword(s):  
Bacillus Thuringiensis ◽  
Cancer Cell ◽  
Human Cancer ◽  
Proteolytic Processing ◽  
Proteinase K ◽  
Major Protein ◽  
Human Cancer Cell ◽  
Soil Isolate ◽  
Anti Cancer

An unusual activity, associated with non-insecticidal and non-haemolytic parasporal inclusion proteins of a Bacillus thuringiensis soil isolate, designated 89-T-26-17, was characterized. The parasporal inclusion of this isolate was bipyramidal, rounded at both ends, containing proteins of 180, 150, 120, 100, and 88 kDa. No homologies with the Cry and Cyt proteins of B. thuringiensis were detected based on N-terminal sequences. Proteolytic processing of the inclusion proteins by proteinase K, trypsin, and chymotrypsin produced a major protein of 64 kDa exhibiting cytocidal activity against human leukaemic T cells and uterus cervix cancer (HeLa) cells. The protease-activated proteins showed no cytotoxicity to normal T cells.Key words: Bacillus thuringiensis parasporal inclusion, non-insecticidal, non-haemolytic, cytocidal activity, human cancer cell.

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