Synthesis and potent cytotoxic activity of a novel diosgenin derivative and its phytosomes against lung cancer cells - Details

author：

Xu, L. (Xu, L..) ^[1] | Xu, D. (Xu, D..) ^[2] | Li, Z. (Li, Z..) ^[3] | Gao, Y. (Gao, Y..) ^[4] | Chen, H. (Chen, H..) ^[5]

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Scopus

Abstract：

Diosgenin　(Di),　a　steroidal　sapogenin　derived　from　plants,　has　been　shown　to　exert　anticancer　effects　in　preclinical　studies.　Using　Di　as　a　starting　material,　various　Di　derivatives　were　designed　and　synthesized,　aiming　to　discover　new　steroid-based　antitumor　agents.　In　this　work,　we　synthesized　several　Di　derivatives　and　screened　FZU-0021-194-P2　(P2),　which　showed　more　potent　cytotoxic　activities　against　human　non-small-cell　lung　cancer　A549　and　PC9　cells.　Considering　that　Di　has　a　unique　sterol　structure　similarly　to　cholesterol,　P2　phytosomes　(P2Ps)　were　prepared　to　further　improve　the　water　solubility　of　P2.　The　P2Ps　exhibited　a　particle　size　of　53.6　±　0.3　nm　with　oval　shape　and　a　zeta　potential　of　-4.0　±　0.7　mV.　P2Ps　could　inhibit　the　proliferation　of　lung　cancer　cells　more　efficiently　than　Di　phytosomes　after　72　h　of　incubation　time　by　inducing　cell　cycle　arrest　and　apoptosis.　The　results　indicated　that　P2Ps　could　be　a　promising　anticancer　formulation　for　non-small-cell　lung　cancer.　©　2019　Xu　et　al.

Keyword：

Diosgenin; Non-small-cell lung cancer; Phytosomes; Sterol structure

Community：

[ 1 ] [Xu, L.]Cancer Metastasis Alert and Prevention Center, College of Chemistry, Fuzhou University, Fuzhou, Fujian, 350116, China
[ 2 ] [Xu, L.]Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou University, Fuzhou, Fujian, 350116, China
[ 3 ] [Xu, D.]Cancer Metastasis Alert and Prevention Center, College of Chemistry, Fuzhou University, Fuzhou, Fujian, 350116, China
[ 4 ] [Xu, D.]Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou University, Fuzhou, Fujian, 350116, China
[ 5 ] [Li, Z.]Cancer Metastasis Alert and Prevention Center, College of Chemistry, Fuzhou University, Fuzhou, Fujian, 350116, China
[ 6 ] [Li, Z.]Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou University, Fuzhou, Fujian, 350116, China
[ 7 ] [Gao, Y.]Cancer Metastasis Alert and Prevention Center, College of Chemistry, Fuzhou University, Fuzhou, Fujian, 350116, China
[ 8 ] [Gao, Y.]Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou University, Fuzhou, Fujian, 350116, China
[ 9 ] [Gao, Y.]College of Chemistry, Fuzhou University, Fuzhou, Fujian, 350108, China
[ 10 ] [Chen, H.]Cancer Metastasis Alert and Prevention Center, College of Chemistry, Fuzhou University, Fuzhou, Fujian, 350116, China
[ 11 ] [Chen, H.]Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou University, Fuzhou, Fujian, 350116, China
[ 12 ] [Chen, H.]College of Chemistry, Fuzhou University, Fuzhou, Fujian, 350108, China

Reprint 's Address：

[Gao, Y.]Cancer Metastasis Alert and Prevention Center, College of Chemistry, Fuzhou UniversityChina

Email：

hellogaoyu@126.com

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Source ：

Beilstein Journal of Nanotechnology

ISSN： 2190-4286

Year： 2019

Volume： 10

Page： 1933-1942

2 . 6 1 2

JCR@2019

2 . 6 0 0

JCR@2023

ESI HC Threshold：236

JCR Journal Grade：2

CAS Journal Grade：3

Cited Count：

WoS CC Cited Count：

SCOPUS Cited Count： 39

ESI Highly Cited Papers on the List： 0 Unfold All

WanFang Cited Count：

Chinese Cited Count：

30 Days PV： 1

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