Antitumor Activity Of Extract Research Articles

Stages of Development and Solvents Determine the Anticancer Potential of Mountain Arnica (Arnica montana L.) Inflorescence Extracts

In recent years, new sources of secondary metabolites (SMs) in medicinal plants have been identified, and the introduction of these plants into field conditions has been carried out to obtain chemically diverse standardized raw material (RM). An example is mountain arnica Arnica montana L., one of Europe’s endemic endangered medicinal plant species, commonly used in pharmacy, cosmetics, and medicine. Its inflorescences (Arnicae flos) are characterized by anti-inflammatory, antiradical, antioxidant, antibacterial, antifungal, and antitumor properties. The main goals of the present research included: (i) characterization of the chemical composition of the inflorescences of A. montana harvested in different development stages; and (ii) presentation of the role of the development stage and different extraction methods in the antitumor activity of extracts through analyses of apoptosis, autophagy, and necrosis induction in human cervical carcinoma HeLa, human colon carcinoma HT29, and human colon metastatic carcinoma SW620 cell lines. The development stage was found to modify the composition of pharmacologically active substances, e.g., sesquiterpene lactones (SLs), flavonoids (Fs), and essential oil (EO), in arnica inflorescences. The content of Fs and EO increased during flowering to the full flowering phase; however, the highest content of SLs was noted in the full flowering phase and at the end of flowering. More promising results, i.e., a relatively high level of apoptosis and a low level of necrosis induced by the arnica extracts, were demonstrated in the HeLa cell line (full flowering; concentration: 0.5 µL/mL), the HT29 cell line (beginning of flowering; concentration: 0.5 µL/mL), and the SW620 cell line (stage of yellow buds; concentration: 1 µL/mL). This extremely valuable medicinal plant species provides a very broad range of RMs (e.g., inflorescences, rhizomes, roots, achenes, and all plant); therefore, attention should be paid to the more frequent use of water as a solvent in studies on the biological activity of mountain arnica extracts.

Evaluation of the in vitro antioxidant and antitumor activity of extracts from Camellia fascicularis leaves.

Camellia fascicularis is a unique plant rich in bioactive components. However, the isolation of the active substances in C. fascicularis leaves via sequential extraction with solvents of different polarity and the determination of their antioxidant and antitumor activities have not been reported. In this study, the total methanol extract of C. fascicularis leaves was sequentially extracted with different polar solvents, and the corresponding petroleum ether extract (PEE), ethyl acetate extract (EAE), and water extract (WE) were analyzed for their contents in active substances such as flavonoids, polyphenols, polysaccharides, and saponins. The antioxidant ability of the polar extracts was investigated by determining their reducing power and the radical scavenging rate on 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and hydroxyl radicals, and CCK-8 and Annexin-FITC/propidium iodide staining assays were conducted to investigate their inhibitory effects on HCCLM6 and HGC27 tumor cells. The results showed that PEE had a high saponin content of 197.35 ± 16.21mgOAE/g, while EAE and WE exhibited a relatively higher polysaccharide content of 254.37 ± 1.99 and 373.27 ± 8.67mgGE/g, respectively. The EAE demonstrated the greatest reducing power and the strongest clearing abilities on ABTS and DPPH radicals with respective EC50 values of 343.45 ± 20.12 and 14.07 ± 0.06μg/ml. Moreover, the antitumor ability of the different polar extracts was dose-dependent, with WE showing the most potent inhibitory ability against HCCLM6 and HGC27 cells.

Identification of Antitumor Constituents in Toad Venom by Spectrum-Effect Relationship Analysis and Investigation on Its Pharmacologic Mechanism.

(1) Background: Toad venom (Bufonis Venenum, known as ‘Chansu’ in Chinese), the secretion of the ear-side gland and skin gland of Bufo gargarizans cantor or Duttaphrynus melanostictus Schneider, has been utilized to treat several diseases in China for thousands of years. However, due to the chemical variability of the components, systematic chemical composition and the key pharmacophores in toad venom have not yet fully understood. Besides, it contains a variety of effective compounds with different physiological activity and chemotypes, mainly including alkaloids, bufogenins, bufotoxins, and so on. The recent pharmacological researches have demonstrated that several bufogenins have remarkable pharmacological effects, such as anti-inflammatory, analgesic effects, and anti-tumor effects. Aim of the study: To identify the bioactive compounds and pharmacophores originating from toad venom based on analyzing spectrum-effect relationship by chemometrics and to explore the anti-cancer mechanism primarily. (2) Materials and methods: Fingerprint of the 21 batches of samples was established using HPLC (High Performance Liquid Chromatography). The anti-tumor activity of extracts were determined by in-vitro assays. Chemometric analysis was used to establish the spectrum-effect model and screen for active ingredients. Pharmacodynamic tests for the screened active compound monomers were conducted with in-vitro assays. Further anti-tumor mechanisms were investigated using western blot and flow cytometry. (3) Results: The established spectrum-effect model has satisfactory fitting effect and predicting accuracy. The inhibitory effect of major screened compounds on lung carcinoma cells A549 were validated in vitro, demonstrating that arenobufagin, telocinobufogenin, and cinobufotalin had significant anti-tumor effects. Through further investigation of the mechanism by western blotting and flow cytometry, we elucidated that arenobufagin induces apoptosis in A549 cells with the enhanced expression of cleaved PARP (poly (ADP-ribose) polymerase). These results may provide valuable information for further structural modification of bufadienolides to treat lung cancer and a method for discovery of anti-tumor active compounds. Conclusions: Our research offers a more scientific method for screening the principal ingredients dominating the pharmacodynamic function. These screened compounds (arenobufagin, etc.) were proven to induce apoptosis by overactivation of the PARP-pathway, which may be utilized to make BRCA (breast cancer susceptibility gene) mutant cancer cells more vulnerable to DNA damaging agents and kill them.

Insights on the anti-inflammatory and antitumor activities of extracts from the marine green alga Codium decorticatum

IntroductionThe Codium genus has been shown to be an important source of marine bioactive compounds for pharmaceutical and nutraceutical applications. The present study was conducted to investigate the anti-inflammatory activity of the n-hexane (Extr 1), dichloromethane (Extr 2) and acetone/methanol (Extr 3) extracts of the green alga Codium decorticatum, as well as their antitumor effects on several cancer cell lines. MethodsIn order to evaluate the anti-inflammatory effect of the extracts of C. decorticatum on the production of the pro-inflammatory proteins, we have undertaken analyses of LPS- and TNF-α-stimulated endothelial cells treated with extracts using enzyme-linked immunosorbent assay (ELISA). Real-time PCR (qPCR) was used to modulate the mRNA expression of inflammatory genes. For the antitumor activity, in vitro cytotoxicity was determined by MTT assay and apoptosis was determined by flow cytometry. ResultsOur results revealed that the Extr 2 and Extr 3 dramatically inhibited the expression of the pro-inflammatory cytokine Interleukin-8 (IL-8) in LPS- and TNF-α-stimulated endothelial cells. We also demonstrated that Extr 2 suppressed the LPS-induced mRNA expression of E-selectin and IL-8. Furthermore, Extr 2 showed cytotoxic activity against the HeLa cell line (IC50 = 37.22 μg/mL), by inducing apoptosis at highest concentrations. ConclusionsThe present data suggest that the seaweed C. decorticatum has the anti-inflammatory properties in endothelial cells, together with the anticancer effect on cervix cancer cells, which may have a potential therapeutic use for inflammatory diseases and cancer. Although, its application as nutraceuticals and functional food could be also considered.

Ovarian cancer cells with CD133+ phenotype is more resistant against Ngai Bun Boesenbergia pandurata extract than original ovarian cancer cells

Introduction: Ovarian cancer is one of the most common cancers in women. Due to the difficulty in early detection and treatment of ovarian cancer, many research studies and clinical trials have been developed to discover more efficient therapies. Besides Western medicine, traditional medicine has gained increased interest as a research field with potential to lead to the production of marketable therapeutic products. With the diversity of tropical plants in Asia, traditional medicine has been very popular and has served as a traditional therapy for generations. The Ngai bun (Boesenbergia pandurata) root is used not only as a food spice but also in ethnomedicine. This study aimed to compare the anti-tumor activity of Boesenbergia pandurata root extract against ovarian cancer cells and CD133+ ovarian cancer cells that were enriched from the original ovarian cancer cells.
 Methods: Crude extract of Boesenbergia pandurata roots were prepared in two kinds of solvents (methanol and chloroform). The ovarian cancer cells OVP-10 were used in this study. The population of CD133+ ovarian cancer cells (CD133+OVP-10) were sorted from the OVP-10 cancer cells. Both OVP-10 cells and CD133+OVP-10 cells were treated with these crude extracts. Adiposederived stem cells (ADSCs) were used as control normal cells for all assays. The anti-tumor activity of extracts were evaluated based on the IC50 values.
 Results: Based on the IC50 index, the chloroform extract had an anti-tumor activity higher than that of methanol extract, on both OVP-10 and CD133+OPV-10 cells (IC50 of methanol and chloroform extracts were 330.1 +/- 16.9 ug/mL and 246.5 +/- 21.2 ug/mL, respectively, for OVP-10 cells; IC50 of methanol and chloroform extracts were 411.8 +/- 83.7 ug/mL and 307 +/- 9.2 ug/mL respectively, for CD133+OVP-10 cells). The results also showed that CD133+OVP-10 cells were more resistant to chloroform extract than were OVP-10 cells (307 +/- 9.2 mg/mL vs. 246.5 +/- 21.2 mg/mL, respectively, for CD133+OVP-10 vs. OVP-10 cells, p < 0.05).
 Conclusion: The chloroform extract of Boesenbergia pandurata roots displayed strong antitumor activity against ovarian cancer cells OVP-10 and CD133+OVP-10; the latter cells were found to be more resistant than the original ovarian cancer cells.

Hopea odorata Extract Can Efficiently Kill Breast Cancer Cells and Cancer Stem-Like Cells in Three-Dimensional Culture More Than in Monolayer Cell Culture.

The breast cancer cells with CD44+CD24- phenotype are known to play an important role in tumorigenesis, drug resistance, and cancer recurrence. Breast cancer cells with CD44+CD24- phenotype are cultured in three-dimensional (3D) stereotype showing the recapitulation of tumors in vivo such as cell differentiation, heterogeneity, and microenvironment. Using this 3D model in anti-cancer compound research results in a more accurate reflection than conventional monolayer cell culture. This study aimed to identify the antitumor activity of Hopea odorata methanol extract (HO-MeOH-E) on breast cancer cells and cancer stem-like cells in both models of three-dimensional culture (3D) and monolayer cell culture (2D). HO-MeOH-E was produced from Hopea odorata plant. The VN9 breast cancer cells (VN9) were collected and expanded from the previous study. The breast cancer stem-like cells (VN9CSC) were sorted from the VN9 based on phenotype CD44+CD24-. Both VN9 and VN9CSC were used to culture in monolayer culture (2D) and organoids (3D) before they were used to treat with HO-MeOH-E. Two other anticancer drugs, doxorubicin and tirapazamine, were used as references. The antitumor activities of extracts and drugs were determined via two assays: antiproliferation using the Alamar blue assay and cell cycle assay. The results showed that HO-MeOH-E was sensitive to both VN9 and VN9CSC in 3D more than 2D culture (IC50 on 3D organoids 144.8±2.172μg/mL and on 2D 340.2±17.01μg/mL for VN9CSC (p<0.001); IC50 on 3D organoids 2055±82.2μg/mL and on 2D 430.6±8.612μg/mL for VN9 (p<0.0001), respectively). HO-MeOH-E inhibits VN9CSC proliferation by blocking S phase and increasing the populations of apoptotic cells; this is consensus to the effect of tirapazamine (TPZ) which is used in hypoxia-activated chemotherapy. Taken these results, HO-MeOH-E has the potential effect in hypoxia-activated chemotherapy specifically on breast cancer stem-like cells with CD44+CD24- phenotype.

ANTIOXIDANT, ANTIBACTERIAL AND ANTITUMOR PROPERTIES OF DIFFERENT EXTRACTS OF MELISSA LEAVES AND BARBERRY ROOTS

Ethyl acetate and ethanol 80% extracts from Melissa officinalis (L.) (leaves) and Berberis vulgaris (roots) plants were studied in terms of phenolic compounds, for their antioxidant, antibacterial and antitumor properties. Total phenolics and total flavonoids were measured using Folin-Ciocalteu reagent and aluminium chloride (AlCl3), respectively. The active ingredients of phenolics and flavonoids were identified using high performance liquid chromatography (HPLC). The major phenolic compound was identified by HPLC for melissa ethanolic extract was Rosmarinic acid (40.24 µg g-1 extract) and for ethanolic barberry extract was Catechol (40.2 µg g-1 extract). Total antioxidant capacity of the extracts was estimated by different methods including DPPH (1,1-diphenyl-2-picrylhydrazyl radical), β-carotene/linoleic bleaching, and ferric reducing antioxidant power (FRAP). Extracts exhibited antioxidant activity that was comparable to the standard antioxidants TBHQ and gallic acid. Antibacterial activity of extracts was determined using pathogen gram-positive and gram-negative bacteria by disc assay method. Antitumor activity of extracts was determined using 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method. The highest activity of extracts for antioxidants, antibacterial and antitumor was Melissa leaves ethanolic extract. Therefore, these extracts could be used as preservative ingredients in the food and/or pharmaceutical industries. Results from this study could be used for improving natural antioxidants and bioactive factors to promote human health.

Antitumor activity of extract and isolated compounds from Drechslera rostrata and Eurotium tonophilum

Total extracts of Drechslera rostrata and Eurotium tonophilum in addition of two isolated compounds from their cultures [di-2-ethylhexyl phthalate (H1) and 1,8-Dihydroxy-3-methoxy-6-methyl-anthraquinone (H2)] were tested for their antitumor activity using four human carcinoma cell lines. Antitumor activity was assessed by performing MTT assay to check the % cell viability. The % viability of HCT-116 (colon carcinoma), HeLa (cervical carcinoma), HEp-2 (larynx carcinoma) and HepG-2 (hepatocellular carcinoma) cells decreased after treatment with Drechslera rostrata and Eurotium tonophilum extracts, these effects were ranged from 059.0± 0.1 to 217.0 ± 0.3 µg/ml on all types of cancer cells. The best activity was recorded for Eurotium tonpholium extract (054.5 ± 0.3, 059.0 ± 0.5 and 059.0 ± 0.1 for HEp-2, Hela, and HepG-2 respectively). The isolated compounds (H1&H2) were found to be responsible about the activities because they recorded the lowest IC50 on tested cell lines with range of 9.5–20.3 μg/ml. Vinblastine sulphate was used as a reference standard and showed in vitro anticancer activity. This study demonstrated that all extracts and isolated compounds have antitumor activity against HCT-116, HeLa, HEp-2 and HepG-2 cells.

Antitumor Activity of Extracts from Medicinal Basidiomycetes Mushrooms.

Aqueous extracts from the vegetative submerged mycelia of cultivated Basidiomycetes Ganoderma lucidum, Lentinus edodes, and Grifola frondosa, as well as from the fruiting bodies of G. lucidum, were found to have antitumor activity. The antitumor effect of the mycelial extracts from all 3 fungal species was ascertained in vivo in rats with implanted kidney cancer. Dystrophic changes in tumor cells and tumor necrosis (up to 90%) were noted. In vitro cytotoxicity studies of the A549 human lung adenocarcinoma cell line and HEp-2 human laryngeal epidermoid carcinoma cells showed that the extracts from the G. lucidum fruiting bodies and from the L. edodes vegetative mycelium were the most effective. The animals' immune systems were activated, and the fungal extracts displayed no toxicity when administered orally.

Evaluation of phytochemical content, antimicrobial, cytotoxic and antitumor activities of extract from Rumex hastatus D. Don roots.

BackgroundBeing a part of Chinese as well as ayurdic herbal system, roots of Rumex hastatus D. Don (RH) is highly medicinal, used to regulated blood pressure. It is also reported that the plant is diuretic, laxative, tonic, used against microbial skin diseases, bilious complaints and jaundice. The present study is conducted to evaluate phytochemical, antimicrobial, antitumor and cytotoxic activities of extract obtained from R. hastatus roots.MethodsRH roots were powdered and extracted with methanol to get crude extract. Crude extract was further fractioned on the basis of increasing polarity, with n-hexane (HRR), chloroform (CRR), ethyl acetate (ERR), n-butanol (BRR) and residual aqueous fraction (ARR). Methanol extract and its derived fractions were subjected to phytochemical screening and assayed for antibacterial activities via agar well diffusion method. Antifungal activities were checked through agar tube dilution method whereas potato disc assay was employed for the determination of antitumor activity. On the other hand cytotoxic activities were conducted using brine shrimps procedures.ResultsThe results obtained from phytochemical analysis indicate the presence of alkaloids, anthraquinones, flavonoids and saponins in all the fractions. Most of the plant fractions showed substantial antimicrobial activities, which is in accordance with the spacious use of tested plant samples in primary healthcare center. Fractions of R. hastatus roots for cytotoxicity were tested as an effective cytotoxic was found as BRR > MRR > CRR > ARR > ERR > HRR. Ranking order of fractions of R. hastatus roots for effective antitumor screening was found as MRR > BRR > ARR > CRR > ERR > HRR.ConclusionsThese results showed that R. hastatus appeared as an important source for the discovery of new antimicrobial drugs and antitumor agents; verify its traditional uses and its exploitation as therapeutic agent.

Evaluation of antitumor property of extracts and steroidal alkaloids from the cultivated Bulbus Fritillariae ussuriensis and preliminary investigation of its mechanism of action.

BackgroundCancer is well known as a leading cause of death in the world. At present, it is the very active area to search for anticancer drugs from natural products. In this study, we evaluated the antitumor property of chloroform extract (CE), n-hexane extract (HE), water extract (WE) and steroidal alkaloids from the cultivated Bulbus Fritillariae ussuriensis (BFU) and its preliminary mechanism for its action was investigated.MethodsFirstly, cytotoxicity of the different extracts from BFU against Lewis lung carcinoma cell line (LLC), Human ovarian cancer cell line (A2780), human hepatocellular carcinoma cell line (HepG2), human lung carcinoma cell line (A549) was measured by MTT assay. Then, we identified the compounds from the active extract of BFU by bioassay guided isolation, determined their antitumor activity in vitro, and detected cell cycle distribution using flow cytometry. Moreover, the extract of BFU which showed remarked anti-proliferative activity in vitro was further evaluated using S180 and LLC tumor models. Additionally, a preliminary investigation of the mechanism of the action was carried out by using histological and immunohistochemical staining technique.ResultsThe results showed that CE and the purified total alkaloids of BFU (TAFU) exhibited stronger cytotoxic activity than the others (WE and HE). We further isolated the four main steroidal alkaloids from TAFU, and found all alkaloids showed significant cytotoxicity, and peimisine induced G0/G1 phase arrest and increased apoptosis. The results showed that TAFU had significant antitumor activity and low toxicity in vivo. Additionally, the immunohistochemical examinations signified that TAFU remarkably increased caspase-3 expression and reduced microvessel density (MVD) in tumor tissues of transplantable S180 and LLC tumor models.ConclusionsThese results achieved suggested that the steroidal alkaloids could hold a good potential for use as an antitumor drug. Notably, our finding is the first report on the antitumor activity of extracts and steroidal alkaloids from the cultivated BFU in vitro and in vivo and its mechanisms.

Antitumor activities of extracts from selected desert plants against HepG2 human hepatocellular carcinoma cells

Context: Phytochemicals are produced by desert plants to protect themselves against stressful environments. They have been shown to be useful in preventing and fighting adverse pathophysiological conditions and complex diseases, including cancer. Although many desert plants have been investigated for their antitumor properties, a large number of them still remain to be explored for possible therapeutic applications in oncologic diseases.Objective: To screen the antitumor effects of selected desert plants, namely Achillea fragrantissima (Forssk.) Sch. Bip. (Compositae), Ochradenus baccatus Delile (Resedaceae), Origanum dayi Post (Lamiaceae), Phlomis platystegia Post (Lamiaceae) and Varthemia iphionoides Boiss (Compositae), against an in vitro tumor model utilizing HepG2 human hepatocellular carcinoma cells.Materials and methods: The aqueous extracts of aerial parts of the aforementioned plants were prepared and used for the in vitro experiments. The HepG2 cells were exposed to varying concentrations (0–4 mg/mL) of each plant extract for 24 or 48 h and the cytotoxicity was measured by the MTT assay.Results: Following 24 h exposure, O. dayi extract exhibited a substantial antiproliferative effect in HepG2 cells (IC50 = 1.0 mg/mL) followed by O. baccatus (IC50 = 1.5 mg/mL). All plant extracts displayed cytotoxicity following 48 h exposure. Nevertheless, a substantial effect was observed with O. dayi (IC50 = 0.35 mg/mL) or O. baccatus (IC50 = 0.83 mg/mL).Conclusion: The aqueous extracts from aerial parts of O. dayi and O. baccatus possess antitumor effects against human liver cancer cells. These desert plants represent valuable resources for the development of potential anticancer agents.

Eclipta prostrata L. phytochemicals: Isolation, structure elucidation, and their antitumor activity

Eclipta prostrata L., (Asteraceae), is used in China for both food and medicine purposes. This research is concerned with the isolation and purification of phytochemical constituents from the aerial parts of E. prostrata, using gradient solvent fractionation, macroporous resin, silica gel, Sephadex LH-20 and ODS columns, and TLC analyses. Four fractions (water, 30% ethanol, 60% ethanol and 90% ethanol) were obtained. Four compounds, wedelolactone (I), eclalbasaponin I (II), luteolin (III) and luteolin-7-O-glucoside (IV) were purified and their structures were identified by the interpretation of spectroscopic analyses including MS, 1H and 13C NMR. Antitumor activities of extracts (total fraction), four fractions and the isolated compounds were assessed using hepatoma cell smmc-7721 as an in vitro assay system. The 30% ethanol fraction and eclalbasaponin I dose-dependently inhibited the proliferation of hepatoma cell smmc-7721 with IC50 values of 74.2399 and 111.1703μg/ml, respectively, more strongly compared with 5-fluorouracil positive control group with the IC50 value of 195.3131μg/ml. Antitumor activities of other fractions and compounds were lower than positive control. These results suggested that some specific compounds or extracts from E. prostrata are potential sources of natural anti-tumor materials and worthy of further study.

Antitumor Activity of Leaves from Hyptis mutabilis (A. Rich.) Briq. (Lamiaceae) in Mice Bearing Tumor

The Hyptis genus has more than 400 species, many of them being used in folk medicine to treat several conditions. Some anticancer compounds have been isolated from plants of this genus, and for that reason we decided to investigate the potential in vivo antitumor activity of extracts of leaves of Hyptis mutabilis with different polarities (hexane, methanol, water, and hot water) against two mice tumors: sarcoma 180 and Ehrlich solid tumor. Phytochemical analysis revealed strong presence of steroids, saponins, flavonoids (mainly dihydroflavanols), and catechins. Acute toxicity was perfomed according to the up-and-down method showing LD50 values ranging from 100 up to 2500 mg/kg. Antitumor activity was investigated using 10% of the LD50 for each extract. Methotrexate was used as positive control. Both aqueous extracts showed strong inhibition of tumor growth with values up to 70% of inhibition growth for sarcoma 180. Ehrlich solid tumor was only slight inhibited by hexane extract (38.6%). In conclusion, the aqueous extracts of H. mutabilis showed promising results against sarcoma 180 mice tumor.

Antitumor Activity of Extracts from Oxytropis falcata Bunge on human Hepatocellular Carcinoma SMMC-7721 Cells In Vitro and in H22 Bearing Mice In Vivo

Oxytropis falcata Bunge is widely used as one of the “three anti-inflamatory drugs” and is considered to be the “king of herbs” in Chinese Tibetan medicine. For thousands of years it has been used to treat inflammation, pyreticosis and bleeding [1]. In the present study, we investigated the antitumor effects of O. falcata extracts on human hepatocellular carcinoma SMMC-7721 cells in vitro and in transplanted murine H22 tumors in vivo. Cell proliferation, morphological changes, cell cycle distribution and apoptosis in SMMC-7721 cells were determined and tumor growth inhibition in H22 tumors was investigated. MTT assay revealed that essential oil fraction (EOOF) and total flavonoids fraction (TFOF) of O. falcata inhibited proliferation of SMMC-7721 cells in a dose-dependent manner. Growth inhibition in H22 solid tumors was significantly pronounced after being treated with TFOF. Hoechst 33258 staining of SMMC-7721 cells indicated that TFOF caused typical characteristics of apoptotic programmed cell death, such as cell shrinkage, apoptotic body formation and nuclear fragmentation. Cell cycle distribution was analyzed by flow cytometry with propidium iodide (PI) and annexin V-FITC/PI double staining that significant solid tumor inhibition occurred in H22 transplanted mice, cell cycle was arrested at G1 phase, and induction of apoptosis occurred in SMMC-7721 cells when subjected to TFOF. These results suggest that TFOF promotes apoptosis in SMMC-7721 cells and inhibits H22 tumor growth, resulting in a potential antitumor effect on hepatic cancer. Acknowledgements: Support for this research from the National Natural Science Foundation of China for Youth (Grant No.30902012) is gratefully acknowledged.

The antitumor activity of extracts from Cordia verbenacea D.C. obtained by supercritical fluid extraction

The present study aims to provide a comparative evaluation of the antitumor activity from Cordia verbenacea extracts obtained by supercritical fluid extraction (SFE) with CO 2 at 300 bar and 50 °C and by classical organic solvent extraction (CE) with ethanol. Antitumor in vitro assays were performed for both extracts and the results demonstrate that the supercritical extract causes superior reduction in tumor cells viability and proliferation, whereas the most probable type of cell death is apoptosis. Only the extract obtained by SFE was able to reduce the expression of COX-2 in MCF-7 cells. The in vivo treatment using supercritical extract decreased the tumor volume, the body weight and packed cell volume, as well as increased in 25% the mean survival time, compared to negative control. As a conclusion, the high pressure extraction method enhanced the cytotoxicity and the antitumor activity of extract from C. verbenacea. Additionally, the antitumor mechanism was probably caused by the inhibition of COX-2, leading to the blockage of the survival cells by apoptosis induction.

가시오갈피 열매 추출물의 생리활성 검정

In this study, we investigated the antioxidant activities, inhibition activity against ACE (angiotensin converting enzyme) and antitumor activity of extract from Acanthopanax senticosus HARMS fruits for development novel functional resources. In order to understand the factors responsible for the potent antioxidant and antihypertensive ability of fruits in A. senticosus, it has been evaluated for anti-oxidative activity using Fenton`s reagent/ethyl linoleate system and for free radical scavenging activity using the l,l-diphenyl-2-picryl hydrazyl free radical generating system. The fruits extract of A. senticosus showed higher antioxidant activities than positive control, -tocopherol at all concentrations, while fruits extract of A. senticosus showed same degree of radical scavenging activity with positive control, -tocopherol. The ability of fruit extracts from A. senticosus to influence the inhibitory activity of angiotensin converting enzyme (ACE) and xanthine oxidase (XOase) has also been discussed. The activity of growth-inhibitory of fruit extracts of A. senticosus was screened by SRB (sulphorhodamine B) method on diverse cancer cells representing different types of cancers. The fruit extracts of A. senticosus showed moderate inhibition on proliferation of LNCaP and MOLT-4F cells and did not inhibit the proliferation of other cancer cells. The fruit extracts of A. senticosus inhibited the proliferation of cancer cells with values ranging from 5 to . This result revealed that the fruit extracts of A. senticosus was expected to be good candidate for development into source of free radical scavengers, antihypertentive, and anti-tumor agent.

Antitumor activity of extracts and compounds from the skin of the toad Bufo bufo gargarizans Cantor

The skin of the toad Bufo bufo gargarizans Cantor is known to be rich in bufadienolides, peptides and alkaloids. It has been found to be a source of some extracts and biologically active compounds with antitumor activity. Cinobufacini (Huachansu), a Chinese medicine prepared from the dried toad skin, has been widely used in clinical therapy for various cancers in China. Bufadienolides, such as bufalin, cinobufagin, resibufogenin, and telocinobufagin, are the major active compounds derived from the toad skin. They are the maker biologically active compounds of cinobufagin while the antitumor activity of cinobufagin may be due to this kind of components. Experimental research has suggested that cinobufacini and its active compounds ( e.g. bufalin and cinobufagin) exhibit significant antitumor activity, including inhibition of cell proliferation, induction of cell differentiation, induction of apoptosis, disruption of the cell cycle, inhibition of cancer angiogenesis, reversal of multi-drug resistance, and regulation of the immune response. Clinical data have indicated that cinobufacini may have effective anticancer activity with low toxicity and few side effects. Data to date suggest it may also enhance quality of life for patients with cancer. Thus, this review briefly summarizes recent studies on the anticancer activity of cinobufacini and some of its active compounds from the skin of the toad Bufo bufo gargarizans Cantor. This might provide additional evidence for further study of the extracts and active compounds from the toad skin in cancer treatment.

Antioxidant, antitumor and antimicrobial activities of the crude extract and compounds of the root bark of Allanblackia floribunda

Context: Allanblackia floribunda Oliver (Guttiferae) is an African medicinal plant used traditionally to treat a variety of ailments.Objective: We investigated the antitumor, radical scavenging, antimycobacterial, antibacterial and antifungal activities of the root bark extract of A. floribunda and three isolated phenolics, namely 1,7-dihydroxyxanthone (1), morelloflavone (2) and 7′-O-glucoside of morelloflavone (3).Materials and methods: The 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) radical scavenging assay was used for antioxidant tests, while crown gall tumor assay was used for assay of antitumor activity. The p-iodonitrotetrazolium chloride (INT) colorimetry and Microplate Alamar Blue Assay (MABA) were used for antimicrobial investigations.Results: Moderate tumor reducing activity was observed with the extract, while better activities were recorded with compounds 2 and 3. The antimycobacterial and antitumor activities of the extract are being reported for the first time. The DPPH radical scavenging test showed that all the studied samples were able to scavenge more than 50% of the free radical, with compound 3 showing the best inhibitory activity (IC50 of 49.08 µg/mL). Compounds 1 to 3 prevented the growth of Mycobacterium smegmatis and both extract and compound 2 were active on M. tuberculosis. The lowest MIC value for the extract (9.76 μg/mL) was recorded against Enterobacter aerogenes while the corresponding value for the compounds (4.88 µg/mL) was obtained with compound 2 on Trichophyton rubrum.Discussion and conclusion: The overall results of the present work provide baseline information for the potential use of the root bark extract of A. floribunda as an antimicrobial, antitumor and antioxidant phytomedicine.

Antitumor Activities of Extracts and Compounds from Water Decoctions of Taxus cuspidata

Water decoctions from the leaves of Taxus cuspidata are used in traditional Chinese medicine to treat cancer, suggesting that water soluble constituents from these leaves may possess anticancer properties. Interestingly, hydrophilic paclitaxel derivatives, as opposed to paclitaxel itself, can be detected by high pressure liquid chromatography in water decoctions from these leaves. The remainder extracts, which are free of paclitaxel and hydrophilic paclitaxel derivatives, from the T. cuspidata leaves were investigated for antitumor activity in vivo and in vitro for the first time in this study. EE80B, 7-xylosyl-10-deacetylpaclitaxel and 7-xylosyl-10-deacetylpaclitaxel C displayed the most antitumor activity in vivo. However, in vitro studies with tumor cell lines showed that EE80B had a significantly smaller antitumor effect than paclitaxel. We hypothesize that water decoctions from T. cuspidata leaves exhibit antitumor effects in vivo, which may be aided by the activation of specific host mechanisms (e.g. stimulation of antitumor immunity) which are not present in vitro.