Synthesis, anticancer activity and potential application of diosgenin modified cancer chemotherapeutic agent cytarabine

Liao, Ai‐Mei; Cai, Bangrong; Huang, Jihong; Hui, Ming; Lee, Kyung-Ku; Lee, Kwang Youl; Chun, ChangJu

doi:10.1016/j.fct.2020.111920

Cited by 13 publications

(7 citation statements)

References 39 publications

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“…Tai investigated curcumin‐loaded liposomes with different ratios of SPC/HSPC; two endothermic peaks were also observed, corresponding to two phase transitions, except that the temperatures were a little higher, possibly due to the amounts of lecithin and cholesterol 29 . After encapsulation, only one peak at 37 °C was found at a similar position, possibly due to the increase in cooperativity of the phospholipid acyl chains with cholesterol 42,43 . At higher temperature, a much stronger endothermic peak was found, for un‐L at 140.39 °C and L‐VE‐βC at 147.76 °C, responding to their melting temperature, respectively 40 .…”

Section: Resultsmentioning

confidence: 95%

“…29 After encapsulation, only one peak at 37 °C was found at a similar position, possibly due to the increase in cooperativity of the phospholipid acyl chains with cholesterol. 42,43 At higher temperature, a much stronger endothermic peak was found, for un-L at 140.39 °C and L-VE-⊎C at 147.76 °C, responding to their melting temperature, respectively. 40 The melting temperature increased after encapsulation, indicating the improvement in the thermal stability of the liposomes, and a sharper peak of L-VE-⊎C liposome was observed, implying the formation of a more ordered arrangement in the bilayer membrane.…”

Section: Differential Scanning Calorimetrymentioning

confidence: 96%

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Physicochemical properties, antioxidant activities and in vitro sustained release behaviour of co‐encapsulated liposomes as vehicle for vitamin E and β‐carotene

Zhang

Cheng

et al. 2022

J Sci Food Agric

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BACKGROUND In this study the potential of liposomes as a vitamin E (VE) and β‐carotene (βC) delivery system was examined. The co‐encapsulated liposomes of βC and VE (L‐VE‐βC) were prepared and characterized. Their antioxidant properties were evaluated by free radical scavenging activities of 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH), 2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulfonic acid (ABTS), hydroxyl radical and lipid peroxidation assay. The in vitro sustained release behaviour was then investigated and discussed. RESULTS VE and βC were co‐encapsulated in liposomes with high encapsulation efficiency, up to 92.49% and 86.16% for βC and VE, respectively. The antioxidant activities of L‐VE‐βC samples were significantly higher than that of single loaded liposome. Among different ratios of VE/βC, L‐VE‐βC at 5:3 exhibited the highest radical scavenging rates, with 66.80%, 56.58% and 34.39% for DPPH, ABTS and OH radical, respectively. L‐VE‐βC samples also had a good ability to inhibit lipid peroxidation, especially the sample with ratios of VE/βC at 5:3 and 3:1. In simulated gastrointestinal release, L‐VE‐βC exhibited an excellent sustained release behaviour in SGF with the accumulated rate at about 20%, while the release rate in SIF increased to over 80%, where they should be absorbed. The release kinetics analysis indicated that βC was released in the Higuchi model in stomach, and the Korsmeyr–Peppas model in intestine. CONCLUSION Compared to single loaded liposomes, the combined‐loaded liposomes exhibited higher antioxidant activity and bioavailability, suggesting the potential applications in functional foods. © 2022 Society of Chemical Industry.

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Section: Resultsmentioning

confidence: 95%

Section: Differential Scanning Calorimetrymentioning

confidence: 96%

Physicochemical properties, antioxidant activities and in vitro sustained release behaviour of co‐encapsulated liposomes as vehicle for vitamin E and β‐carotene

Zhang

Cheng

et al. 2022

J Sci Food Agric

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“…The TCM option alone as a palliative treatment is suitable for patients who cannot tolerate surgical treatment or radiotherapy and chemotherapy. The main characteristic of TCM treatment is syndrome differentiation and treatment, while the main characteristic of Western medicine treatment is evidence-based differentiations [ 10 , 23 ]. The combination of both not only considers the patient's overall condition but also targets the specific lesions of patients' disease conditions.…”

Section: Discussionmentioning

confidence: 99%

Study on the Mechanism of Diosgenin Targeting STAT3 to Inhibit Colon Cancer Proliferation and Migration

et al. 2022

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To elucidate regulatory effects and molecular mechanisms of diosgenin on colon cancer, this study administered diosgenin at concentrations of 10 (low), 50 (medium), and 100 μmol/L (high concentration group) at the cell level, respectively. EdU, colony formation, and Transwell assays were implemented to determine SW480 cellular proliferation and migration. Assays of flow cytometry and TUNEL were employed to estimate cell apoptosis. Additionally, nude mouse tumorigenesis assay was used to further verify the regulatory function of diosgenin on colon cancer. The target protein of diosgenin was predicted via molecular docking. The results showed that all three concentrations of diosgenin could reduce colon cancer cellular proliferation and migration, and after diosgenin treatment, colon cancer cellular apoptosis was markedly increased, and the 100 μmol/L diosgenin group produced the most satisfactory inhibition on colon cancer cell proliferation. Ki67 expression was markedly reduced whereas those of Bax and caspase3 were greatly increased after diosgenin treatment. The nude mouse tumorigenesis assay indicated that the parameters of tumorous volume and mass of diosgenin treatment group were greatly decreased as compared to control, and as the concentration of diosgenin increased, the inhibitory effect was more significant. Molecular docking indicated that STAT3 served as a target protein of diosgenin. Moreover, after diosgenin treatment on colon cancer cells, the STAT3 expression was markedly reduced. The STAT3 overexpression would counteract the inhibitory effect of 50 μmol/L diosgenin in both suppressing colon cancer cellular proliferation and migration and promoting apoptosis. Taken together, all our outcomes demonstrated the diosgenin effects in not only inhibiting colon cancer cellular proliferation and migration but also promoting cancerous cellular apoptosis. Diosgenin is a regulatory player in targeting and regulating STAT3.

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“…One of these compounds: diosgenyl α-L-rhamnopyranosyl-(1→2)-[α-L-arabinopyranosyl-(1→4)]-α-L-arabinopyranoside, induces apoptosis in A549 cells via caspase-8 mediated exogenous pathway and caspase-9 mediated endogenous pathway (Wang et al, 2012). Another study reported that diosgenin altered the biofilm affinity of cytarabine (Ara-C) during liposome preparation to exert anti-tumor activity, and DG-Ara-C liposomes showed superior anti-tumor activity than free DG and Ara-C liposomes against leukemia cells and solid tumor cells (Liao et al, 2021). Furthermore, (Meng et al, 2019) synthesized an additional fluorophore derivative of diosgenin (GND) from diosgenin and glucosamine hydrochloride in 7-10 steps.…”

Section: Diosgenin Glycosylated Derivativesmentioning

confidence: 99%

Diosgenin: an important natural pharmaceutical active ingredient

Huang

et al. 2022

Food Sci. Technol

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Diosgenin is a steroidal saponin isolated from dioscorea opposita, which has been proven to have anti-cancer, anti-inflammatory, anti-thrombotic and immune system modulating effects in a large number of pharmacological tests. Diosgenin is also one of the important raw materials for the synthesis of steroidal drugs, and structural modification of diosgenin to obtain diosgenin derivatives can not only improve the solubility and dissolution, but also enhance their pharmacological effects. This paper reviews the synthetic reactions, pharmacological effects of diosgenin and its derivatives, aiming to provide detailed information for the further development and application of diosgenin, which is important to improve the utilization value of diosgenin.

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Synthesis, anticancer activity and potential application of diosgenin modified cancer chemotherapeutic agent cytarabine

Cited by 13 publications

References 39 publications

Physicochemical properties, antioxidant activities and in vitro sustained release behaviour of co‐encapsulated liposomes as vehicle for vitamin E and β‐carotene

Physicochemical properties, antioxidant activities and in vitro sustained release behaviour of co‐encapsulated liposomes as vehicle for vitamin E and β‐carotene

Study on the Mechanism of Diosgenin Targeting STAT3 to Inhibit Colon Cancer Proliferation and Migration

Diosgenin: an important natural pharmaceutical active ingredient

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