Cytotoxic Cardenolides from the Leaves of Calotropis gigantea

Seeka, Chonticha; Sutthivaiyakit, Somyote

doi:10.1248/cpb.58.725

Cited by 38 publications

(26 citation statements)

References 18 publications

(15 reference statements)

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“…The compound was extracted from the leaves that has cytotoxic activity on MCF-7 cancer cells, KB (skin cancer cells) and NCL-H18 (lung cancer cells) (Saeka & Sutthivaiyakit, S., 2010). Dichloromethane extract from the leaves also has cytotoxic activity on many cancer cells, such as MCF-7, MDA-MB-231, HeLa cells, HT-29, SKOV-3, and Hep-G2 (Wong et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Comparison of Ethanol Extract from Roots, Leaves, and Flowers of Calotropis gigantea as Anticancer on T47D Breast Cancer Cell Lines

Mutiah¹,

Sukardiman²,

Widyawaruyanti³

et al. 2018

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This research aims to find out the anticancer activity of ethanol extract from the roots, leaves, and flowers of Calotropis gigantea. This experiment was conducted by MTT method on T47D breast cancer cell line. The result showed that the root of Calotropis gigantea was more cytotoxic (IC50 89.76 μg/mL) on T47D breast cancer cell line than the leaves (IC50 459.51 μg/mL) and the flowers (IC50>1000). Based on the result, roots are potent to be chemotherapeutic agent, especially in breast cancer.

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Section: Introductionmentioning

confidence: 99%

Comparison of Ethanol Extract from Roots, Leaves, and Flowers of Calotropis gigantea as Anticancer on T47D Breast Cancer Cell Lines

Mutiah¹,

Sukardiman²,

Widyawaruyanti³

et al. 2018

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“…Natural products derived from plants, such as cardenolides, flavonoids, and terpenes, have diverse pharmacological properties, and they may potentially be used to treat cancer [24][25][26]. ToxH was extracted from the seeds of Antiaris toxicaria (Pers.)…”

Section: Discussionmentioning

confidence: 99%

Toxicarioside H induces drug-resistant mitophagy via promoting expression of sirtuin-3 in lung cancer cells

Huang¹,

Sun²,

Yang³

et al. 2018

Oncotarget

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Cardenolides may have anticancer effects and toxicarioside H (ToxH), which we isolated, may have similar activity but its underlying mechanism against tumors is not clear. Herein, we report that ToxH treatment inhibited cell proliferation and induced mitochondrion-dependent apoptosis and mitophagy in human A549 and H460 lung cancer cells. ToxH treatment increased the expression of Sirt3, and inhibited Sirt3 expression via RNA interference against Sirt3 (siSirt3) suppressed mitophagy in ToxH-treated lung cancer cells. Stronger inhibition of cell proliferation and induction of apoptosis occurred when ToxH-mediated mitophagy was blocked by siSirt3. In addition, ToxH treatment redistributed hexokinase II from the mitochondria to the cytosol in A549 and H460 lung cancer cells, and decreased interaction of hexokinase II with VDAC1 was accompanied by the increased interaction of VDAC1 with parkin. Moreover, the disruption of Sirt3 by siSirt3 decreased the association of VDAC1 with parkin. Thus, ToxH induces drug-resistant mitophagy by enhancing the expression of Sirt3, which leads to the dissociation of hexokinase II from VDAC1 and increased binding of VDAC1 with parkin. Adding ToxH to a mitophagy inhibitor may thus be an effective strategy for treating lung cancer.

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“…From the leaves of C. gigantea, 16α-hydroxycardenolide, calotropagenin, calotoxin, frugoside and 12β-hydroxycoroglaucigenin showed cytotoxic activity against KB, MCF7 and NCI-H187 human cancer cells [32]. Calotoxin displayed strong activity against KB cells while frugoside had good overall activity.…”

Section: Calotropis Giganteamentioning

confidence: 97%

Cytotoxic Cardenolides from Calotropis Species: A Short Review

Chan¹,

Sweidan²,

Wong³

et al. 2017

Rec.Nat.Prod.

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Abstract:From different plant parts of Calotropis species (C. gigantea and C. procera), various classes of compounds such as oxypregnanes, terpenoids, sterols, cardenolides and flavonoids have been isolated. Of these compounds, the cardenolides stand out as many of them have anticancer properties. Cardenolides are C 23 steroids with a five-membered unsaturated butyrolactone ring consisting of a steroid nucleus, a lactone moiety at C-17 and a sugar moiety at C-3. The roles of cardenolides in the treatment of human cancer have been established as they can induce apoptosis and inhibit the growth of cancer cells. Structure-activity relationship analyses have yielded some interesting findings on their cytotoxicity. Compounds with six-membered ring sugar groups generally have significantly stronger inhibitory activity than those with five-membered ring sugar groups. A formyl or methyl-hydroxyl group at C-10 enhances cytotoxicity while the presence of a 4´-OH or 16-OH group decreases cytotoxicity. Chemical modification of 2"-oxovoruscharin, a novel cardenolide extracted from the root bark of C. procera, has led to the synthesis of UNBS1450. The compound is characterized by more potent antiproliferative activity, lower toxicity, and is a strong sodium pump inhibitor and inducer of non-apoptotic cell death. UNBS1450 is currently in Phase I clinical trials.

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Cytotoxic Cardenolides from the Leaves of Calotropis gigantea

Cited by 38 publications

References 18 publications

Comparison of Ethanol Extract from Roots, Leaves, and Flowers of Calotropis gigantea as Anticancer on T47D Breast Cancer Cell Lines

Comparison of Ethanol Extract from Roots, Leaves, and Flowers of Calotropis gigantea as Anticancer on T47D Breast Cancer Cell Lines

Toxicarioside H induces drug-resistant mitophagy via promoting expression of sirtuin-3 in lung cancer cells

Cytotoxic Cardenolides from Calotropis Species: A Short Review

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