Bioactive proteins and peptides isolated from Chinese medicines with pharmaceutical potential.

Some protein pharmaceuticals from Chinese medicine have been developed to treat cardiovascular diseases, genetic diseases, and cancer. Bioactive proteins with various pharmacological properties have been successfully isolated from animals such as Hirudo medicinalis (medicinal leech), Eisenia fetida (earthworm), and Mesobuthus martensii (Chinese scorpion), and from herbal medicines derived from species such as Cordyceps militaris, Ganoderma, Momordica cochinchinensis, Viscum album, Poria cocos, Senna obtusifolia, Panax notoginseng, Smilax glabra, Ginkgo biloba, Dioscorea batatas, and Trichosanthes kirilowii. This article reviews the isolation methods, molecular characteristics, bioactivities, pharmacological properties, and potential uses of bioactive proteins originating from these Chinese medicines.

Tyrosinase inhibitory activity of a glucosylated hydroxystilbene in mouse melan-a melanocytes.

2,3,5,4'-Tetrahydroxystilbene-2-O-β-D-glucopyranoside (1), isolated from Polygonum multiflorum, is a noncompetitive inhibitor of tyrosinase in cell-free kinetics; it reduced the Vmax values in a dose-dependent manner. Compound 1 inhibited PKA-induced melanogenesis, reduced the protein expression of tyrosinase and its transcription factor, the microphthalmia-associated transcription factor, and lowered the complex formation between tyrosinase and tyrosinase-related protein 1 (TRP-1). Immunofluorescence microscopy revealed no association of tyrosinase with the endoplasmic reticulum or lysosomes, implying the absence of a direct effect of 1 on the maturation process of the enzyme.

MicroRNA-218 inhibits melanogenesis by directly suppressing microphthalmia-associated transcription factor expression.

The microphthalmia-associated transcription factor (MITF) is a pivotal regulator of melanogenic enzymes for melanogenesis, and its expression is modulated by many transcriptional factors at the transcriptional level or post-transcriptional level through microRNAs (miRNAs). Although several miRNAs modulate melanogenic activities, there is no evidence of their direct action on MITF expression. Out of eight miRNAs targeting the 3'-UTR of Mitf predicted by bioinformatic programs, our results show miR-218 to be a novel candidate for direct action on MITF expression.

Inducing self-rotation of cells with natural and artificial melanin in a linearly polarized alternating current electric field.

The phenomenon of self-rotation observed in naturally and artificially pigmented cells under an applied linearly polarized alternating current (non-rotating) electrical field has been investigated. The repeatable and controllable rotation speeds of the cells were quantified and their dependence on dielectrophoretic parameters such as frequency, voltage, and waveform was studied. Moreover, the rotation behavior of the pigmented cells with different melanin content was compared to quantify the correlation between self-rotation and the presence of melanin.

Self-rotation of cells in an irrotational AC E-field in an opto-electrokinetics chip.

The use of optical dielectrophoresis (ODEP) to manipulate microparticles and biological cells has become increasingly popular due to its tremendous flexibility in providing reconfigurable electrode patterns and flow channels. ODEP enables the parallel and free manipulation of small particles on a photoconductive surface on which light is projected, thus eliminating the need for complex electrode design and fabrication processes. In this paper, we demonstrate that mouse cells comprising melan-a cells, RAW 267.

Automated rotation rate tracking of pigmented cells by a customized block-matching algorithm.

This article describes an automated rotation rate tracking algorithm for pigmented cells that undergo rotation in a dielectrophoretic (DEP) force field. In a completely automated process, we preprocess each frame of a video sequence, then analyze the sequence frame by frame using a rotating-circle template with a block-matching algorithm, and finally estimate the rotation rate of the pigmented cells using a pixel-patch correlation. The algorithm has been demonstrated to accurately calculate the DEP-induced rotation rate of the cell up to 250 rpm.

Protective roles of Cordyceps on lung fibrosis in cellular and rat models.

Ethnopharmacological Relevance: Cordyceps sinensis is a fungus used in traditional Chinese medicine as a tonic to soothe the lung for the treatment of fatigue and respiratory diseases. Idiopathic pulmonary fibrosis is a chronic, irreversible and debilitating lung disease showing fibroblast/myofibroblast expansion and excessive deposition of extracellular matrix in the interstitium leading to breathing difficulty. Our previous observation revealed a partial relief of lung fibrosis in patients suffering from severe acute respiratory syndrome (SARS).

Mercury levels in road dust and household TSP/PM₂.₅ related to concentrations in hair in Guangzhou, China.

Road dust, household total suspended particulate matters (TSP) and PM₂.₅ were collected in urban area of Guangzhou, south of China, to investigate the concentrations of total mercury (THg) and methyl mercury (MeHg). The household PM₂.

Stellettin A induces endoplasmic reticulum stress in murine B16 melanoma cells.

Isomalabaricanes are a small class of rearranged triterpenoids obtained from marine sponges. Most of these are cytotoxic to tumor cells, but the underlying mechanism is not clear. In this study, it was demonstrated that stellettin A (1), obtained from Geodia japonica, inhibited the growth of B16F10 murine melanoma cells by the induction of endoplasmic reticulum stress and accumulation of unfolded proteins.

Anti-melanogenic property of geoditin A in murine B16 melanoma cells.

Geoditin A, an isomalabaricane triterpene isolated from marine sponge Geodia japonica, has been demonstrated to induce apoptosis in leukemia HL60 cells and human colon HT29 cancer cells through an oxidative stress, a process also interfering with normal melanogenesis in pigment cells. Treatment of murine melanoma B16 cells with geoditin A decreased expression of melanogenic proteins and cell melanogenesis which was aggravated with adenylate cyclase inhibitor SQ22536, indicating melanogenic inhibition was mediated through a cAMP-dependent signaling pathway. Immunofluorescence microscopy and glycosylation studies revealed abnormal glycosylation patterns of melanogenic proteins (tyrosinase and tyrosinase-related protein 1), and a co-localization of tyrosinase with calnexin (CNX) and lysosome-associated membrane protein 1 (LAMP-1), implicating a post-translational modification in the ER and a degradation of tyrosinase in the lysosome.

Polybrominated diphenyl ethers and polychlorinated dibenzo-p-dioxins and dibenzofurans in surface dust at an E-waste processing site in Southeast China.

Surface dust collected from printed circuit board recycling workshop floors, roads, a schoolyard, and an outdoor food market in Guiyu, China, a village intensely involved in e-waste processing, were investigated for levels of polybrominated diphenyl ethers (PBDEs) and polychlorinated dibenzo-p-dioxins and dibenzofurans (PCDD/Fs). PBDE concentrations in dust from workshop-floors (14,800 ± 5130 ng/g) and on adjacent roads to the workshops (24,900 ± 31,600 ng/g) were highest among the study sites whereas PCDD/F concentrations were highest at the schoolyard (1316 pg/g) and in a workshop (1264 pg/g). Analyses of <2 mm and <53 μm dust particle sizes did not show any significant differences in PBDE concentrations.

Tian Xian Liquid (TXL) induces apoptosis in HT-29 colon cancer cell in vitro and inhibits tumor growth in vivo.

Background: Tian Xian Liquid (TXL) is a Chinese medicine decoction and has been used as an anticancer dietary supplement. The present study aims to investigate the effects of TXL on the apoptosis of HT-29 cells and tumor growth in vivo.

Method: HT-29 colon cancer cells were treated with gradient dilution of TXL.

Geoditin A induces oxidative stress and apoptosis on human colon HT29 cells.

Geoditin A, an isomalabaricane triterpene isolated from the marine sponge Geodia japonica, has been demonstrated to dissipate mitochondrial membrane potential, activate caspase 3, decrease cytoplasmic proliferating cell nuclear antigen (PCNA), and induce apoptosis of leukemia cells, but the underlying mechanism remains unclear [1]. In this study, we found fragmentation of Golgi structure, suppression of transferrin receptor expression, production of oxidants, and DNA fragmentation in human colon cancer HT29 cells after treatment with geoditin A for 24 h. This apoptosis was not abrogated by chelation of intracellular iron with salicylaldehyde isonicotinoyl hydrazone (SIH), but suppressed by N-acetylcysteine (NAC), a thiol antioxidant and GSH precursor, indicating that the cytotoxic effect of geoditin A is likely mediated by a NAC-inhibitable oxidative stress.

Involvement of p21 and FasL in induction of cell cycle arrest and apoptosis by neochamaejasmin A in human prostate LNCaP cancer cells.

Neochamaejasmin A ( 1), a biflavonoid isolated from the roots of a traditional Chinese medicine, Stellera chamaejasme L., was shown to inhibit cellular (3)H-thymidine incorporation (IC 50 12.5 microg/mL) and subsequent proliferation of human prostate cancer LNCaP cells.

Quantitative structure-cytotoxicity relationship analysis of betulinic acid and its derivatives by semi-empirical molecular-orbital method.

A semi-empirical molecular-orbital method (CAChe) demonstrates that the cytotoxicity of betulinic acid derivatives can be predicted by several physical parameters (such as heat of formation, hydrophobicity (log P), watersolubility, ionization potential, electron affinity, dipole moment), but not by molecular size (maximum length and width). The present study demonstrates how this method can be applied to estimate the cytotoxic activity of structurally-related compounds.

Apoptotic activity of betulinic acid derivatives on murine melanoma B16 cell line.

The mitochondrion plays a crucial role in the process of apoptosis and has thus become one of the targets for the search for potential chemotherapeutic agents. Betulinic acid [3beta-hydroxy-lup-20(19)lupaen-28-carbonic acid], a lupane-type triterpene which is abundant in many plant species, has been shown to exert a direct effect on the mitochondria and subsequent apoptosis in melanoma cells. Chemical synthesis and modification of betulinic acid are being explored to develop more potent derivatives.

Polyhydroxylated steroids and other constituents of the soft coral Nephthea chabroli.

Polyhydroxylated steroids and other metabolites were isolated from the soft coral Nephthea chabroli collected in South China Sea. The structures of two new compounds were determined to be 24-methylcholesta-9(11), 24(28)-diene-3beta,12alpha,19-triol and 4alpha-methyl-3beta,14beta-dihydroxy-5alpha-ergost-24(28)-en-23-one on the basis of spectroscopic analysis. Cytotoxic activities of the polyhydroxylated sterols were evaluated on prostate carcinoma LNCaP cell line.

Lignanamides and nonalkaloidal components of Hyoscyamus niger seeds.

Four lignanamides, a tyramine derivative, and 10 other nonalkaloidal components were isolated from the seeds of Hyoscyamus niger. Among them, hyoscyamide (1), 1,24-tetracosanediol diferulate (6), and 1-O-(9Z,12Z-octadecadienoyl)-3-O-nonadecanoyl glycerol (7) are new structures. The other compounds were identified as grossamide, cannabisin D, cannabisin G, N-trans-feruloyl tyramine, 1-O-octadecanoyl glycerol, 1-O-(9Z,12Z-octadecadienoyl) glycerol, 1-O-(9Z,12Z-octadecadienoyl)-2-O-(9Z,12Z-octadecadienoyl) glycerol, 1-O-(9Z,12Z-octadecadienoyl)-3-O-(9Z-octadecenoyl) glycerol, rutin, vanillic acid, beta-sitosterol, and daucosterol.