Kahweol inhibits proliferation and induces apoptosis by suppressing fatty acid synthase in HER2-overexpressing cancer cells

Oh, Suck Hoon; Hwang, Yong Pil; Choi, Jae Ho; Jin, Sun Woo; Lee, Gi Ho; Han, Eun Hee; Chung, Young‐Ho; Chung, Young Chul; Jeong, Hye Gwang

doi:10.1016/j.fct.2018.09.008

Cited by 32 publications

(25 citation statements)

References 45 publications

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“…Studies on various tumor cells have confirmed that kahweol-induced apoptosis is related with caspase 3 activation, cytochrome c releasing from mitochondria to cytoplasm and down-regulating anti-apoptotic proteins and cyclins [58,59,60,61,62]. Kahweol plays anti-cancer effects by regulating Sp1, Akt, ERK/JNK pathways with multiple targets [58,61,62,63,64,65]. In addition to the above mechanism, Kim et al [65] also reported that kahweol inhibited proliferation and promoted apoptosis in A549 cells in a positively correlation with treated time (24–48 h) and dose (10–40 μM).…”

Section: Biological and Pharmacological Activities Of Cafestol Andmentioning

confidence: 99%

Cafestol and Kahweol: A Review on Their Bioactivities and Pharmacological Properties

Ren

Wang

et al. 2019

IJMS

121

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Cafestol and kahweol are natural diterpenes extracted from coffee beans. In addition to the effect of raising serum lipid, in vitro and in vivo experimental results have revealed that the two diterpenes demonstrate multiple potential pharmacological actions such as anti-inflammation, hepatoprotective, anti-cancer, anti-diabetic, and anti-osteoclastogenesis activities. The most relevant mechanisms involved are down-regulating inflammation mediators, increasing glutathione (GSH), inducing apoptosis of tumor cells and anti-angiogenesis. Cafestol and kahweol show similar biological activities but not exactly the same, which might due to the presence of one conjugated double bond on the furan ring of the latter. This review aims to summarize the pharmacological properties and the underlying mechanisms of cafestol-type diterpenoids, which show their potential as functional food and multi-target alternative medicine.

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Section: Biological and Pharmacological Activities Of Cafestol Andmentioning

confidence: 99%

Cafestol and Kahweol: A Review on Their Bioactivities and Pharmacological Properties

Ren

Wang

et al. 2019

IJMS

121

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“…Among them is kahweol, an anti-inflammatory diterpene that remains in unfiltered coffee beverages including espresso, Scandinavian boiled, and Turkish coffees [19]. Aside from the well-established anti-carcinogenic property [20,21,22,23,24,25,26], studies on human neuroblastoma and dopaminergic neurons have suggested a neuroprotective function of kahweol [27,28]. In addition, kahweol has been shown to reduce LPS-induced macrophages proinflammatory activation [29] and prevent hepatic injury through its anti-inflammatory property [30,31].…”

Section: Introductionmentioning

confidence: 99%

Acute Kahweol Treatment Attenuates Traumatic Brain Injury Neuroinflammation and Functional Deficits

2019

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Traumatic brain injury (TBI) affects millions worldwide with devastating long-term effects on health and cognition. Emerging data suggest that targeting the immune response may offer promising strategies to alleviate TBI outcomes; kahweol, an anti-inflammatory diterpene that remains in unfiltered coffee, has been shown to be beneficial in neuronal recovery. Here, we examined whether kahweol could alleviate brain trauma-induced injury in a mouse model of TBI and its underlying mechanisms. TBI was induced by controlled cortical impact (CCI) and various doses of kahweol were intraperitoneally administered following injury. Contusion volume, brain edema, neurobehavioral deficits, and protein expression and activity were evaluated in both short-term and long-term recovery. We found that kahweol treatments significantly reduced secondary brain injury and improved neurobehavioral outcomes in TBI mice. These changes were accompanied by the attenuation of proinflammatory cytokine secretion, decreased microglia/macrophage activation, and reduction of neutrophil and leukocyte infiltration. In addition, continuous kahweol treatment further improved short-term TBI outcomes compared to single-dosage. Collectively, our data showed that kahweol protects against TBI by reducing immune responses and may serve as a potential therapeutic intervention for TBI patients.

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“…Cacalol inhibits lipid biosynthesis and impairs tumor growth both in vivo and in vitro by downregulating FASN via Akt/SREBP pathway [226]. Piperine and kahweol have been reported to inhibit FASN activity and SREBP1c, by interfering with Akt/mTOR signaling in HER2 overexpressing cells resulting in reduced cell growth via induction of apoptosis [227,228]. [6]-Gingerol-an active component of ginger inhibits ERK1/2 and JNK MAP kinases and induces caspase-dependent apoptosis [229].…”

Section: Growth Factor Signalingmentioning

confidence: 99%

Phytochemicals targeting metabolic reprogramming in cancer: an assessment of role, mechanisms, pathways and therapeutic relevance

Khan¹,

Siddiqui²,

Husain³

et al. 2020

Preprint

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The metabolism of cancer is remarkably different from that of normal cells and confers variety of benefits including the promotion of other cancer hallmarks. As the rewired metabolism is a near-universal property of cancer cells, efforts are underway to exploit metabolic vulnerabilities for therapeutic benefit. In the continued search for a safer and effective ways of cancer treatment, structurally diverse plant-based compounds have gained substantial attention. Here, we present an extensive assessment of the role of phytocompounds in modulating cancer metabolism and make a case for the use of plant-based compounds in targeting metabolic vulnerabilities of cancer. We discuss the interactions of phytocompounds with major metabolic pathways and evaluate the role of phytochemicals in the regulation of growth signaling and transcriptional programs involved in metabolic transformation of cancer. Lastly, we examine the potential of these compounds in clinical management of cancer along with limitations and challenges

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Kahweol inhibits proliferation and induces apoptosis by suppressing fatty acid synthase in HER2-overexpressing cancer cells

Cited by 32 publications

References 45 publications

Cafestol and Kahweol: A Review on Their Bioactivities and Pharmacological Properties

Cafestol and Kahweol: A Review on Their Bioactivities and Pharmacological Properties

Acute Kahweol Treatment Attenuates Traumatic Brain Injury Neuroinflammation and Functional Deficits

Phytochemicals targeting metabolic reprogramming in cancer: an assessment of role, mechanisms, pathways and therapeutic relevance

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