Antiproliferative Activity of Triterpenoid and Steroid Compounds from Ethyl Acetate Extract of Calotropis gigantea Root Bark against P388 Murine Leukemia Cell Lines

Calotropis gigantea has been known to produce bioactive secondary metabolites with antiproliferative activities against cancer cells. Herein, we extracted the secondary metabolites using ethyl acetate from its root bark and further tested its antiproliferative activities against P388 murine leukemia cell lines. The subfractions from the ethyl acetate extract was obtained from Vacuum Liquid Column Chromatography (VLCC), and followed by Gravity Column Chromatography (GCC). The subfraction C2 and D1 were identified to contain triterpenoids and steroids with the most potent cytotoxicity against Brine Shrimp Lethality Test (BSLT). A 3-(4,5-dimethylthiazol-2-yl) -2-5 diphenyl tetrazolium bromide (MTT) assay suggested that ethyl acetate extract has the highest antiproliferative activities against P388 murine leukemia cell lines (IC50 = 21.79 μg/mL), as opposed to subfraction C2 (IC50 = 50.64 µg/mL) and subfraction D1 (IC50 = 49.33 µg/mL). The compound identified in subfraction C2 and D1 are taraxerol acetate and calotropone, respectively. Though taraxerol acetate and calotropone were active in inhibiting the leukemic cell lines, their IC50s were lower than the ethyl acetate extract, which is probably due to the synergism of the secondary metabolites.

Antioxidant effects and in vitro cytotoxicity on human cancer cell lines of flavonoid-rich Flamboyant (Delonix regia (Bojer) Raf.) flower extract

Background: Cancer is a noncommunicable disease with increasing incidence and mortality rates both worldwide and in Thailand. Its apparent lack of effective treatments is posing challenging public health issues. Introduction: Encouraging research results indicating probable anti-cancer properties of the Delonix regia flower extract (DRE) have prompted us to evaluate the feasibility of developing a type of product for future cancer prevention or treatment. Methods and Results: In the present report, using High Performance Liquid Chromatography (HPLC), we demonstrate in the DRE, the presence of high concentrations of three identifiable flavonoids, namely rutin 4.15±0.30 % w/w, isoquercitrin 3.04±0.02 %w/w, and myricetin 2.61±0.01 % w/w respectively while the IC50 of DPPH and ABTS assay antioxidation activity was 66.88±6.30 µg/ml and 53.65±7.24 µg/ml respectively. Discussion: Our cancer cell line studies using the MTT assay demonstrated DREs potent and dose dependent inhibition of murine leukemia cell line (P-388: 35.28±4.07% of cell viability remaining), as well as of human breast adenocarcinoma (MCF-7), human cervical carcinoma (HeLa), human oral cavity carcinoma (KB), and human colon carcinoma (HT-29) cell lines in that order of magnitude. Conclusion: Three identifiable flavonoids (rutin, isoquercitrin and myricetin) with high antioxidation activity and potent and dose dependent inhibition of murine leukemia cell line and five other cancer cell lines were documented in the DRE. The extract’s lack of cytotoxicity in 3 normal cell lines is a rare advantage not usually seen in current antineoplastic agents. Yet another challenge of the DRE was its low dissolution rate and long-term storage stability, issues to be resolved before a future product can be formulated.

Triterpenoids from the Bark of Aglaia glabrata and their In vitro Effects on P-388 Murine Leukemia Cells

Four dammarane-type triterpenoids, dammardienon (1), aglaiabbreviatin E (2), dammar-20,25-dien-3b,24-diol (3) and dammar-24-en-3b,20-diol (4) were isolated from methanolic extract of the bark of Aglaia glabrata. The structures of all triterpenoids were elucidated by 1D-, 2D-NMR, and comparison with previously reported data. All triterpenoids were applied into in vitro bioassay against P-388 murine leukemia cell. Dammar-24-en-3b,20-diol (4) has cytotoxic activity with IC50 value of 9.45 mM towards P-388 murine leukemia cell lines.

Potensi antitumor dari beberapa spons laut asal teluk Manado

Screening of antitumor for the extract and fraction from the marine sponges ofManado Gulf, Aaptos sp., Acervochalina sp., Gelliodes sp., Theonella sp., and orangeboring sponge have been done by use P388 murine leukemia cell. Activity test resultshowed IC50 of the extract and fraction from Aaptos sp were: MeOH extract 5938ng/mL and BuOH extract 125000 ng/mL; Acervochalina sp: EtOH extract 125000ng/mL, PE extract 125000 ng/mL, EtOAc extract 4251 ng/mL, BuOH extract125000 ng/mL; Gelliodes sp: EtOH extract 125000 ng/mL; Theonella sp: EtOHextract 125000 ng/mL, PE extract 9282 ng/mL, EtOAc extract 3273 ng/mL, BuOHextract 125000 ng/mL; orange boring sponge: MeOH extract 1422 ng/mL. Based onthe IC50 value, it could be concluded that MeOH extract of Aaptos sp., EtOAc extractof boring sponge could be a sources for cytotoxic compounds.

CYTOTOXIC BIOACTIVE COMPOUNDS FROM CALOTROPIS GIGANTEA STEM BARK

<p><strong>Objective: </strong>The present study deals with the cytotoxic activity of n-hexane and ethyl acetate extracts of <em>Calotropis gigantea</em> L. stem bark and its fractions such as A, B, C, D and E fractions on murine leukemia cell line P388.</p><p><strong>Methods: </strong>The crude extracts of <em>C. gigantea</em> stem bark were prepared using n-hexane and ethyl acetate solvents. The plant extracts were subjected to vacuum liquid chromatography followed by TLC. According to the similarity of stain patterns, the fractions were combined. The extracts and its combined fractions were then subjected for the phytochemical test. Cytotoxic activity of those extracts and its combined fractions were tested using MTT assay. Fraction D was subjected to gravity column chromatography followed by TLC. Then, fractions A, B, and D2 were crystallized and subjected to GC-MS.</p><p><strong>Results: </strong>The qualitative screening of n-hexane extract of <em>Calotropis gigantea</em> L. stem bark for secondary metabolites showed the presence of terpenoid, flavonoids, phenolics and coumarins. While the ethyl acetate extract contained phenolics, steroids, flavonoids, saponins and coumarins compounds. IC₅₀values for n-hexane extract and E fraction are 76.29 µg/ml and 18.48 µg/ml, respectively. In the ethyl acetate extract and C fraction obtained IC₅₀ values 57.05 µg/ml and 52.58 µg/ml.</p><p><strong>Conclusion: </strong>Cytotoxic activity from E fraction of n-hexane extract of <em>C. gigantea</em> stem bark is the most potent and containing flavonoids, phenolics and coumarins. The main components from several compounds of n-hexane extract of <em>C. gigantea</em> are germacrane-A, (-)-globulol, urs-12-ene and veridiflorol. </p>

7α-Hydroxyfriedelan-3-one-26-ol-29-oic acid and other Constituents from Pileostegia viburnoides var. glabrescens

Phytochemical investigation of the roots and rhizomes of Pileostegia viburnoides var. glabrescens led to the isolation and identification of 31 compounds (1-31), 25 of which (1-2, 4-7, 9-12, 15-18, 21-31) were isolated from the Pileostegia genus for the first time. 7α-Hydroxyfriedelan-3-one-26-ol-29-oic acid (1) is a new friedelane-type triterpene. The structure of n-butyl-β-D-fructopyranoside (2) was determined by single-crystal X-ray diffraction. Compounds 4 and 12 displayed marginal cytotoxicity against the P388 murine leukemia cell line with IC50 values of 13.4 μM and 25.0 μM, respectively. Compound 23 exhibited marginal anti-inflammatory activity by the inhibition of lipopolysaccharide induced nitric oxide production in RAW 264.7 macrophage cells, with an IC50 value of 32.0 μM. Compounds 3, 8-10, 25, and 27 were phytotoxic to the dicot Lactuca sativa (lettuce) and/or the monocot Agrostis stolonifera (bentgrass).