Delving into the Latest Updates on EF-40 with Synapse

Overview

Basic Info

Drug Type

Unknown

Synonyms

Target-

Mechanism

Osteogenesis stimulants

Therapeutic Areas

Endocrinology and Metabolic DiseaseSkin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Osteoporosis, Postmenopausal

Originator Organization

Scotia Holdings Plc

Active Organization-

Inactive Organization

Scotia Holdings Plc

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Helicteres angustifolia L. (Helicteres angustifolia) has been commonly used in folk medicine to treat cancer; however, its mechanisms of action remain obscure. In our earlier work, we reported that aqueous extract of H. angustifolia root (AQHAR) possesses attractive anticancer properties. In the present study, we isolated five ethanol fractions from AQHAR and investigated their therapeutic efficacy in human non-small cell lung cancer (NSCLC) cells. The results showed that among the five fractions, the 40% ethanol fraction (EF40) containing multiple bioactive compounds exhibited the best selective killing effect on NSCLC cells with no obvious toxicity to normal human fibroblasts. Mechanistically, EF40 reduced the expression of nuclear factor-E2-related factor 2 (Nrf2), which is constitutively expressed at high levels in many types of cancers. As a result, Nrf2-dependent cellular defense responses are suppressed, leading to the intracellular accumulation of reactive oxygen species (ROS). Extensive biochemical analyses revealed that EF40 caused cell cycle arrest and apoptosis through activation of the ROS-mediated DNA damage response. Furthermore, treatment with EF40 compromised NSCLC cell migration, as evidenced by the downregulation of matrix metalloproteinases (MMPs) and heterogeneous nuclear ribonucleoprotein K (hnRNP-K). In vivo studies using A549 xenografts in nude mice also revealed significant suppression of tumor growth and lung metastasis in the treated group. We propose that EF40 may serve as a potential natural anti-NSCLC drug that warrants further mechanistic and clinical attention.

100 Deals associated with EF-40

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Osteoporosis, Postmenopausal	Phase 2	GB	Scotia Holdings Plc	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASCO2021	Not Applicable	Colorectal Cancer	7	CoupledCAR technology (CoupledCAR-T cells)	(nxajpioyhz) = vmnxhezhmh crtpxflttr (tseqhgbggp ) View more	Positive	28 May 2021