Acronyculatin P, A New Isoprenylated Acetophenone from the Stem Bark of Acronychia pedunculata

A new isoprenylated acetophenone, acronyculatin P (1) as well as two known compounds, 3′,5′-diisoprenyl-2′,4′-dihydroxy-6′-methoxyphenylethanone (2) and 3′-isoprenyl-2′,4′,6′-trihydroxyphenylethanone (3) were isolated from the stem bark of Acronychia pedunculata (L.) Miq. The structures were determined by HRESIMS, 1D and 2D NMR. The inhibitory activity of the isoprenylated acetophenone derivatives against murine leukemia P-388 cells showed compound 1 moderate activity with IC₅₀ 15.42 µM.

Meliglabrin, A New Flavonol Derivative from the leaves of Melicope glabra (Blume) T.G. Hartley

A new flavonol derivative, meliglabrin (1) along with three known flavonols, ternatin (2), meliternatin (3), and 5,4′-dihydroxy-3,7,3′-trimethoxyflavon (4) were isolated from the leaves of Melicope glabra (Blume) T.G. Hartley. Their structures were determined using extensive spectroscopic methods, including UV, IR, HRESIMS, 1D and 2D NMR. Compounds 1 – 4 were evaluated for their cytotoxicity against murine leukemia P-388 cells, compound 4 showed moderate activity.

Cytotoxicity and Structure Activity Relationship of Dammarane-Type Triterpenoids from the Bark of Aglaia elliptica against P-388 Murine Leukemia Cells

Six dammarane-type triterpenoids, dammar-24-en-3β-ol (1), 3β-epicabraleahydroxy lactone (2), (E)-25-hydroperoxydammar-23-en-3β,20-diol (3), dammar-24-en-3β,20-diol (4), 3β-acetyl-20S,24S-epoxy-25-hydroxydammarane (5), and 3β-epiocotillol (6) were isolated from the methanolic extract of the bark of Aglaia elliptica. The chemical structure were identified on the basis of spectroscopic evidence and by comparison with those spectra previously reported. Compounds 1 – 6 were isolated first time from this plant. Compounds 1 – 6, along with a known synthetic analog, cabraleone (7) were evaluated their cytotoxic activity against P-388 murine leukimia cells in vitro. Among those compounds 3β-acetyl-20S,24S-epoxy-25-hydroxydammarane (5) showed strongest cytotoxic activity with IC₅₀ value of 8.02 ± 0.06 µM.

Flavonoid Compounds from the Leaves of Kalanchoe prolifera and Their Cytotoxic Activity against P-388 Murine Leukimia Cells

Seven flavonoid compounds, kaempferol (1), quercetin (2), quercetin-3-O-β-D-glucopyranoside (3), kaempferol-3-O-β-D-glucopyranoside (4), kaempferol-3-O-α-L-rhamnoside (5), quercetin-3-O-sophoroside (6) and quercetin-3-O-rutinoside (7), were isolated from the methanolic extract of leaves of Kalanchoe prolifera. Compounds 1-7 were isolated for first time from this plant. These compounds were evaluated their cytotoxic activity against P-388 murine leukimia cells in vitro. Among those compounds kaempferol (1) and quercetin (2) showed strongest cytotoxic activity with IC₅₀ values of 4.45 ± 0.05 and 6.28 ± 0.02 µg/mL, respectively.

Piceatanol: Anti-Cancer Compound From Gewang Seed Extract.

Piceatannol (Compound 1), brownish white solids compound, is a stilbene compound has been isolated from methanol seeds extract of Corypha utan Lamk. Isolation and purification conducted by chromatographic methods. Structure elucidation deduced on the basis of spectroscopic data (UV spectrometer, FTIR, NMR and HRMS). MTT assay method of cytotoxicity activity showed that Compound 1 has a very strong cytotoxic activity against Murine leukemia P-388 cell lines with IC50 value 1.56 ppm.

Synthesis of Methyl 2-Cinnamamido-3-Hydroxy Propanoate Having Activity against P388 Leukemia Cells.

Cinnamic acid derivative compound was investigated for the anti-cancer inhibitory activity. To be able to obtain compounds that have bioactivity as above, it is needed to study quantitative structure-activity relationship (QSAR) which is the process by which the chemical structure is quantitatively correlated with biological activity/chemical reactivity. Chemical methods used in synthesizing the chemical of methyl trans-cinnamate derivatives are tailored to match their targeted bioactivities. Here, we investigated the anti-cancer inhibitor compound with the method amidation of cinnamic acid derivative compounds. In this reaction we use two steps to get the target product. Firstly, we hydrolize of methyl trans-cinnamate to cinnamic acid. That reaction has a yield 85.5 % and secondly, we amidate of cinnamic acid to metil 2-cinnamamido-3-hydroxy propanoate has a yield of 51.5%. The compound of metil 2-cinnamamido-3-hydroxy propanoate showed against P388 leukemia cells inhibitory activity with IC50 = 10.78 μg/mL.

Biological activity of sea anemone proteins: II. Cytolysis and cell line toxicity.

Potent cytolytic activity was exhibited by proteins extracted from three sea anemones viz. Heteractis magnifica, Stichodactyla haddoni and Paracodylactis sinensis by affecting the red blood corpuscles (RBC) and the mouse fibroblast cell line (L929) and leukemia cell line (P388). Crude toxin of all the three anemone species induced spontaneous hemolysis of chicken, goat and human erythrocytes. The crude toxin of H. magnifica (0.98 mg/ml) elicited hemolysis at levels of 4096, 512 and 4096 HU (hemolytic unit) in chicken, goat and human erythrocytes respectively. Subsequently, the crude toxin of S.haddoni (0.82 mg/ml) exhibited a hemolytic activity of 256, 128 and 512 HU and that of P. sinensis (0.60 mg/ml) had a hemolytic activity of 128, 4096 and 512 HU. Most of the partially purified proteins of these anemones also exhibited the activity against the three different erythrocytes. The viability of L929 and P388 was adversely affected on adding the crude toxins. The symptoms of toxicity shown by the cells were rounding, lysis and detachment from the substratum. These effects were the least in S. haddoni, as compared to those the crude toxins of the other two species. Inhibition of growth of L929 exhibited by the toxin of the three species ranged between 61.08 and 93.38%. Similarly, inhibition of the growth of P388 ranged between 51.32 and 86.16%. The present investigation reveal the cytotoxic nature of anemone toxins.

Effect of Hemidesmus indicus R.Br. root extract against Salmonella enterica serovar Typhimurium-induced apoptosis in murine macrophage cell line (P388D1).

Background & objectives: Previous studies on natural products had mainly dealt with their antimicrobial activity and studies on the interference of these bioactive compounds with host-bacterial interaction is limited. The present study was undertaken to investigate the effect of the sterols and fatty acids present in the chloroform fraction of crude methanol extract of Hemidesmus indicus root (CHI) on Salmonella enterica serovar Typhimurium (S. Typhimurium) mediated apoptosis in a murine macrophage cell line (P388D1). Methods: Bacterial sensitivity test was carried out with different concentrations of CHI and the optimum dose was fixed as 100 μg/ml for CHI, which was safe on host cells as the CD50 (50% of cell death) dose of CHI was determined to be 500 μg/ml in the P388D1 cell line. Results: The CHI-treated bacteria had negligible cytotoxicity and were less potent to invade and proliferate intracellularly. Murine macrophages infected with wild bacteria, stained with Hoechst 33258, had swollen and damaged morphology with characteristic apoptotic bodies whereas macrophages infected with treated bacteria had comparative normal architecture. Immunofluorescence and transmission electron micrographs both confirmed that CHI-treated bacteria were defective and smaller than the wild bacteria. Ultrastructures of P388D1 cells infected with wild bacteria showed many ingested bacteria and characteristic Salmonella-containing vacuoles (SCV). Some cells had condensed or fragmented nuclei with swollen mitochondria, whereas most of the cells infected with treated bacteria were normal in morphology and a few had internalized bacteria, but the typical bacteria laden SCV was not observed in cells infected with CHI-treated S. Typhimurium. Interpretation & conclusions: Our results showed that the choloroform fraction of H. indicus root blocked the cytotoxic activity of S. Typhimurium in a macrophage cell line. More studies need to be done to elaborate and confirm our findings.

The Impact of Compound Zhe-bei Granule and Adriamycin on p53 Gene Expression in the P388 Xenograft Tumor / 医学研究杂志

Objective To study the impact of compound zhe-bei granule and adriamycin on p53 gene expression in the P388 xenograft tumor.Methods The tumor xenografts model was established by injecting the mouse lymphocytic leukemia cells(P388) in the subcutis of anterior axillary of Kunming mice,and then was treated with CZBG by intragastric administration and different doses of adriamycin by intraperitoneal injection(i.p.).After the end of the experiment,tumor was striped completely,and the expression of p53 gene in xenograft tumor of each group was detected by fluorescence quantitative polymerase chain reaction,and the relative quantification of p53 gene of each group was computed using 2-??Ct method.Results Comparing the 2-??Ct values of p53 gene relative expression of each group,no statistical significance was found(F=0.56,P=0.7557).And the relative expression value of p53 gene of CZBG joint high-dose ADM group was higher,while the relative expression value of CZBG joint low-dose ADM group was lower.Conclusion Combined use of CZBG and ADM is able to raise the expression of p53 tumor suppressor gene in the P388 xenograft tumor.

HISTOLOGICAL AND HISTOCHEMICAL CHANGES OF THYMIC NURSE CELLS AND IMMUNE ORGANS OF MOUSE AFTER THE INOCULATION OF LEUKEMIC CELLS / 解剖学报

It was discovered in this experiment that 3 days after inoculation of the ascitic fluid from P_(388) leukemic mice, the positive percentages of AcP and ?-Gase of the lymphocytes within the TNC of the recipients were increased significantly, while the positive percentage of ANAE was decreased. All the positive percentages of the three enzymes of the thymocytes within the thymus were increased significantly, but no abnormal structural changes were seen in the thymus. No histological and cytochemical changes were found in the lymph nodes and the spleen. Nine days after inoculation, the leukemia cell infiltration, hemorrhage and cell degeneration occurred in all the thymus, lymph nodes and spleen of the mouse. The normal structures of the organs were destroyed. The positive percentages of the cytochemical reactions of the three enzymes in the lymphocytes were all increased significantly. At this stage, TNC was very difficult to be isolated from the thymus. The results indicate that thymus and TNC may have a close relationship with the development of this type of leukemia.