Celastrol in cancer therapy: Recent developments, challenges and prospects

Lim, Hannah Ying; Ong, Pei Shi; Wang, Lingzhi; Goel, Anjana; Ding, Ling-Wen; Wong, Andrea Li‐Ann; Ho, Paul C.; Sethi, Gautam; Xiang, Xiaoqiang; Goh, Boon Cher

doi:10.1016/j.canlet.2021.08.030

Cited by 64 publications

(27 citation statements)

References 91 publications

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“…Furthermore, initial PT2385 administration to a patient suffering metastatic renal carcinoma (ccRCC), followed by a Phase I clinical trial in patients with advanced ccRCC, PT2385 showed promising efficacy and tolerability as monotherapy [ 220 , 221 ]. Consistently, a recent meta-analysis of nine previous studies showed an inverse correlation between circulating and dietary vitamin D levels and the occurrence of ccRCC [ 222 ], suggesting that a combination of HIF inhibitors (including natural compounds such as flavonoids, celastrol, and resveratrol [ 223 , 224 , 225 ]) and calcitriol could be a potential anticancer strategy to treat ccRCC.…”

Section: Cancer–hypoxia–vitamin Dmentioning

confidence: 60%

Vitamin D and Hypoxia: Points of Interplay in Cancer

Gkotinakou

Mylonis

Tsakalof

2022

Cancers

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Vitamin D is a hormone that, through its action, elicits a broad spectrum of physiological responses ranging from classic to nonclassical actions such as bone morphogenesis and immune function. In parallel, many studies describe the antiproliferative, proapoptotic, antiangiogenic effects of calcitriol (the active hormonal form) that contribute to its anticancer activity. Additionally, epidemiological data signify the inverse correlation between vitamin D levels and cancer risk. On the contrary, tumors possess several adaptive mechanisms that enable them to evade the anticancer effects of calcitriol. Such maladaptive processes are often a characteristic of the cancer microenvironment, which in solid tumors is frequently hypoxic and elicits the overexpression of Hypoxia-Inducible Factors (HIFs). HIF-mediated signaling not only contributes to cancer cell survival and proliferation but also confers resistance to anticancer agents. Taking into consideration that calcitriol intertwines with signaling events elicited by the hypoxic status cells, this review examines their interplay in cellular signaling to give the opportunity to better understand their relationship in cancer development and their prospect for the treatment of cancer.

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Section: Cancer–hypoxia–vitamin Dmentioning

confidence: 60%

Vitamin D and Hypoxia: Points of Interplay in Cancer

Gkotinakou

Mylonis

Tsakalof

2022

Cancers

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“…Among the triterpenoid, Celastrol is currently the most extensively studied component-its structural formula displaying in Figure 2 . Besides the anti-tumor effect ( Lim et al, 2021 ), it can regulate lipid metabolism and is an effective anti-obesity agent ( Feng et al, 2019 ). It also has the potential in central nervous system diseases’ treatment ( Schiavone et al, 2021 ).…”

Section: Introductionmentioning

confidence: 99%

Applications and Mechanisms of Tripterygium Wilfordii Hook. F. and its Preparations in Kidney Diseases

Xue

Qiao

Yang³

et al. 2022

Front. Pharmacol.

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Tripterygium wilfordii Hook. f. (TwHF) is a Chinese botanical drug containing a large number of metabolites. The discovered and recognized anti-inflammatory and immune-regulating effects have made it attract more and more attentions in trials and clinical researches. The extraction and processing of TwHF for pharmaceuticals is a manifestation of the role of traditional Chinese medicine. However, TwHF is toxic. Optimization of TwHF preparations has become a requirement for the development of TwHF pharmaceuticals. Our article introduces the main preparations of TwHF on the Chinese market and their characteristics. In particular, we summarize the clinical applications and influential mechanisms of TwHF and its preparations in kidney diseases. Considering that nephropathy is closely related to immune inflammation and TwHF is a botanical drug with a high number of metabolites, the application of TwHF in kidney diseases may be much more complicated. By revealing the role and mechanisms of TwHF in kidney diseases, this study aims to provide more insights to basic and clinical studies about nephropathy.

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“…It is also known to tackle bioavailability issues when loaded into a nanocarrier and has proved to be a safer compound. These phytochemicals have expanded their use due to their safer toxicity windows and multifactorial effects [ 29 ].…”

Section: Introductionmentioning

confidence: 99%

Thymoquinone-Enriched Naringenin-Loaded Nanostructured Lipid Carrier for Brain Delivery via Nasal Route: In Vitro Prospect and In Vivo Therapeutic Efficacy for the Treatment of Depression

et al. 2022

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In the current research, a thymoquinone-enriched naringenin (NGN)-loaded nanostructured lipid carrier (NLC) was developed and delivered via the nasal route for depression. Thymoquinone (TQ) oil was used as the liquid lipid and provided synergistic effects. A TQ- and NGN-enriched NLC was developed via the ultrasonication technique and optimized using a central composite rotatable design (CCRD). The optimized NLC exhibited the following properties: droplet size, 84.17 to 86.71 nm; PDI, 0.258 to 0.271; zeta potential, −8.15 to −8.21 mV; and % EE, 87.58 to 88.21%. The in vitro drug release profile showed the supremacy of the TQ-NGN-NLC in comparison to the NGN suspension, with a cumulative drug release of 82.42 ± 1.88% from the NLC and 38.20 ± 0.82% from the drug suspension. Ex vivo permeation study displayed a 2.21-fold increase in nasal permeation of NGN from the NLC compared to the NGN suspension. DPPH study showed the better antioxidant potential of the TQ-NGN-NLC in comparison to NGN alone due to the synergistic effect of NGN and TQ oil. CLSM images revealed deeper permeation of the NGN-NLC (39.9 µm) through the nasal mucosa in comparison to the NGN suspension (20 µm). Pharmacodynamic studies, such as the forced swim test and the locomotor activity test, were assessed in the depressed rat model, which revealed the remarkable antidepressant effect of the TQ-NGN-NLC in comparison to the NGN suspension and the marketed formulation. The results signify the potential of the TQ-enriched NGN-NLC in enhancing brain delivery and the therapeutic effect of NGN for depression treatment.

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Celastrol in cancer therapy: Recent developments, challenges and prospects

Cited by 64 publications

References 91 publications

Vitamin D and Hypoxia: Points of Interplay in Cancer

Vitamin D and Hypoxia: Points of Interplay in Cancer

Applications and Mechanisms of Tripterygium Wilfordii Hook. F. and its Preparations in Kidney Diseases

Thymoquinone-Enriched Naringenin-Loaded Nanostructured Lipid Carrier for Brain Delivery via Nasal Route: In Vitro Prospect and In Vivo Therapeutic Efficacy for the Treatment of Depression

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