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Last update 08 May 2025

Cycleanine Dimethobromide

Last update 08 May 2025

Overview

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Clinical Result

Translational Medicine

Overview

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Drug Type

Small molecule drug

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Structure/Sequence

Molecular FormulaC38H42N2O6

InChIKeyANOXEUSGZWSCQL-LOYHVIPDSA-N

CAS Registry518-94-5

100 Clinical Results associated with Cycleanine Dimethobromide

100 Translational Medicine associated with Cycleanine Dimethobromide

100 Patents (Medical) associated with Cycleanine Dimethobromide

162

Literatures (Medical) associated with Cycleanine Dimethobromide

01 Dec 2023·South African Journal of Botany

Phytochemical composition and antidiabetic potential of the leaf, stem, and rhizome extracts of Cissampelos capensis L.f

Author: Reddy, Shanika ; Venter, Maryna van de ; Latolla, Nehemiah ; Hlangothi, Buyiswa

Diabetes mellitus has a growing global prevalence and complications resulting from type 2 diabetes have been recorded to lead to death.The endemic medicinal plant Cissampelos capensis L.f. has been identified as an important plant in the management of diabetes by local people in southern Africa.The current work was designed to evaluate the in vitro cytotoxic, antioxidant, and α-amylase - and α-glucosidase inhibition of C. capensis based on its believed antidiabetic potential.The phytochem. anal. was performed through qual. (HPTLC), and quant. (UV-Vis spectrophotometry and LC-MS) anal., while the in vitro MTT cytotoxicity, ORAC - and DPPH radical scavenging assays, α-glucosidase - and α-amylase inhibition potential of leaf, stem, and rhizome methanolic - (MCCL, MCCS, and MCCR) and TTA crude extracts (TTA CCL, TTA CCS, and TTA CCR) of C. capensis were accessed.Addnl., the cytotoxicity and enzymic potential of five previously reported bioactive proaporphine alkaloids (glaziovine, pronuciferine, cissamaline, cissamanine, and cissamdine) isolated from C. capensis were evaluated.The phytochem. anal. revealed the highest presence of alkaloids followed by flavonoids, phenols, and terpenes.MCCL (93.740 ± 11.634 %), TTA CCS (77,818 ± 2,590 %), and TTA CCR (60,375 ± 12,722 %) exhibited the highest cell viability at 125 μg/mL, resp., better than that of the pos. control, Melphalan (62.5 μM).Where the The ORAC - and DPPH radical scavenging assays generally exhibited strong antioxidant activity for the rhizome and stem methanolic extractsThe α-glucosidase inhibition was strongest for the rhizome and stem extracts and comparable to that of the control.However, α-amylase inhibition was stronger for the leaf and rhizome extracts, and only comparable to the control at 500 μg/mL.All the isolated proaporphine alkaloids exhibited concentration dependant cytotoxicity, with moderate α-amylase inhibition at 500 μg/mL while no α-glucosidase inhibition was observedThe potential antioxidants and enzymic inhibition combined with the moderate cytotoxicity of C. capensis and its isolated bioactive proaporphine alkaloids make it a good source of a possible new type II diabetic targets.

25 Apr 2023·ACS omega

Exploration of Phaeanthine: A Bisbenzylisoquinoline Alkaloid Induces Anticancer Effect in Cervical Cancer Cells Involving Mitochondria-Mediated Apoptosis.

Article

Author: Murali, Vishnu Priya ; Meenu, Murugan Thulasi ; Malgija, Beutline ; Valsan, Alisha ; Nisha, Prakasan ; Joseph, Anuja Gracy ; Maiti, Kaustabh Kumar ; Radhakrishnan, Kokkuvayil Vasu

Natural-product-based pharmacophores possess considerably more structural diversity, attractive physicochemical features, and relatively less toxicity than synthesized drug entities. In this context, our studies on phaeanthine, a bisbenzylisoquinoline alkaloid isolated from the rhizomes of Cyclea peltata (Lam) Hook.f & Thoms., showed selective cytotoxicity toward cervical cancer cells (HeLa) with an IC₅₀ of 8.11 ± 0.04 μM. Subsequent investigation with in silico molecular docking of phaeanthine displayed preferential binding to the antiapoptotic protein Akt as reflected by a docking score of -5.023. Interestingly, the follow-up in vitro assessment of the compound correlated with mitochondria-mediated apoptosis specifically by downregulating the expression of Akt and p-Akt, including other antiapoptotic proteins MCl-1, IGF-2, and XIAP. In the complementary in vitro assessment, mitochondrial membrane polarization and dynamics of intercellular cytochrome c validated the intrinsic mechanism of the apoptotic phenomenon. To the best of our knowledge, this is the first comprehensive anticancer profiling study of phaeanthine against HeLa cells.

01 Nov 2022·Journal of Molecular Modeling

The impact of cycleanine in cancer research: a computational study

Article

Author: Wai, Lam Kok ; Nwaefulu, Ogochukwu Ngozi ; Jayanthi, Sivaraman ; Sagineedu, Sreenivasa Rao ; Islam, Mohammad Kaisarul ; Al-Shar'i, Nizar A ; Woei, Lim Chee ; Owolabi, Josephine Omonkhelin ; Stanslas, Johnson

Cancer is imposing a global health burden because of the steady increase in new cases. Moreover, current anticancer therapeutics are associated with many drawbacks, mainly the emergence of resistance and the severe adverse effects. Therefore, there is a continuous need for developing new anticancer agents with novel mechanisms of action and lower side effects. Natural products have been a rich source of anticancer medication. Cycleanine, a natural product, was reported to exert an antiproliferative effect on ovarian cancer cells by causing apoptosis through activation of caspases 3/7 and cleavage of poly (ADP-ribose) polymerase to form poly (ADP-ribose) polymerase-1 (PARP1). It is well-established that PARP1 is associated with carcinogenesis, and different PARP1 inhibitors are approved as anticancer drugs. In this study, the cytotoxic activity of cycleanine was computationally investigated to determine whether it is a PARP1 inhibitor or a caspase activator. Molecular docking and molecular dynamics (MD) simulations were utilized for this purpose. The results showed that cycleanine has a good binding affinity to PARP1; moreover, MD simulation showed that it forms a stable complex with the enzyme. Consequently, the results showed that cycleanine is a potential inhibitor of the PARP1 enzyme.

100 Deals associated with Cycleanine Dimethobromide

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Cycleanine Dimethobromide

Overview

Basic Info

Structure/Sequence

Related

R&D Status

Clinical Result

Translational Medicine

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Core Patent

Clinical Trial

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