Study on the improvement effects and mechanism of Phyllanthus emblica water extracts on insulin resistance and lipid metabolism disorder in diabetic model rats / 中国药房

OBJECTIVE To investigate the improvement effects and possible mechanism of Phyllanthus emblica water extracts on lipid metabolism disorder and insulin resistance （IR） in diabetic model rats. METHODS IR model of male SD rats was established and randomly divided into model group， positive control group， P. emblica water extracts high-dose， medium-dose and low-dose groups， and another blank group was set up， with 10 rats in each group. P. emblica water extracts high-dose， medium- dose and low-dose groups were given P. emblica water extract diluent at the doses of 800， 400 and 200 mg/kg respectively； positive control group was given pioglitazone solution 2.7 mg/kg； blank group and model group were given the same volume of normal saline， by intragastrical administration， once a day， for consecutive 4 weeks. The general state of rats was observed， and the body mass and the levels of serum lipid metabolism indexes [triacylglycerol （TG）， total cholesterol （TC）， low-density lipoprotein cholesterol （LDL-C）， high-density lipoprotein cholesterol （HDL-C）] were measured； fasting insulin of serum （FINS）， insulin resistance index （IRI） and insulin sensitivity index （ISI） were measured and calculated by enzyme-linked immunosorbent assay （ELISA）. The pathological morphology of liver tissue was observed by hematoxylin-eosin staining； the expression of glycogen in the liver was observed by periodic acid-Schiff staining， and the staining area was calculated； the protein expressions of peroxisome proliferator-activated receptor γ （PPARγ）， nuclear factor κB（NF-κB） and AMP-activated protein kinase （AMPK） were detected by Western blot. RESULTS Compared with blank group， the rats in the model group had obvious symptoms of polydipsia， polyphagia and polyuria， and the serum levels of TC， TG， LDL-C， FINS and IRI were significantly increased （P＜0.05）， while ISI was significantly reduced （P＜ 0.05）； the structure of hepatic lobule was obviously disordered， the liver cells were deformed and enlarged， and there were many lipid deposits and fat vacuoles； PAS staining area of glycogen was significantly reduced（P＜0.05）； the protein expression levels of PPARγ and p-AMPK were significantly decreased （P＜0.05）， while the protein expression level of NF-κB was significantly increased （P＜0.05）. Compared with model group， the mental state of rats， liver histopathological morphology and glycogen expression were improved significantly in P. emblica water extracts high-dose and medium-dose groups； the levels of the above indicators were significantly reversed（P＜0.05）. CONCLUSIONS P. emblica water extracts may improve glucose and lipid metabolism disorders， liver function and IR in IR model rats， and regulate IR by activating the PPARγ/AMPK/NF-κB signaling pathway.

Effect of Compound Phyllanthus urinaria Ⅱ on Growth and Expression of miR-122 and IGF-1R of Hepatocellular Carcinoma Hep3B Cells in Nude Mice / 中国实验方剂学杂志

ObjectiveTo investigate the inhibitory effects and mechanism of the compound Phyllanthus urinaria Ⅱ （CPU Ⅱ）on the growth of transplanted hepatocellular carcinoma Hep3B2.1-7 （Short for Hep3R） cells in nude mice. MethodAfter the establishment of a xenograft model of hepatocellular carcinoma Hep3B cells in mice， the model mice were randomly divided into a model group， a high-dose CPU Ⅱ group （57.5 g·kg-1）， a low-dose CPU Ⅱ group （28.75 g·kg-1）， and a 5-fluorouracil （5-FU） group （0.025 g·kg-1）， with eight mice in each group. The mice in the high- and low-dose CPU Ⅱ groups were treated with drugs by gavage， once per day， and those in the model group were treated with the same volume of normal saline. The mice in the 5-FU group were treated by 5-FU by intraperitoneal injection， once every other day. After 28 days of administration， mice were sacrificed， and transplanted tumors were collected. Immunohistochemistry （IHC） was used to detect the expression of proliferating cell nuclear antigen （PCNA） of tumor tissues. Terminal-deoxynucleotidyl transferase-mediated nick end labeling （TUNEL） was used to detect cell apoptosis of tumor tissues. The mRNA expression of miR-122 and insulin-like growth factor 1 receptor （IGF-1R） in tumor tissues was detected by Real-time quantitative PCR （Real-time PCR）. The protein expression of CCAAT/enhancer-binding protein α （C/EBPα）， hepatocyte nuclear factor-4α （HNF-4α）， and IGF-1R in tumor tissues was detected by Western blot. ResultThe tumor suppression rates of the high- and low-dose CPU Ⅱ groups and the 5-FU group were 74.90%， 63.62%， and 64.15%， respectively. Compared with the model group， the CPU Ⅱ groups and the 5-FU group showed reduced weight （P<0.01） and volume of tumors （P<0.01）， decreased PCNA positive cells， shallow staining， increased apoptosis cells of transplanted tumor tissues （P<0.05， P<0.01）， increased expression of mRNA expression of miR-122 （P<0.01）， down-regulated mRNA expression of IGF-1R （P<0.01）， and up-regulated protein expression of C/EBPα and HNF-4α in nude mouse transplanted tumor tissues （P<0.01）. The expression of IGF-1R protein in the high-dose CPU Ⅱ group was down-regulated （P<0.05）. Compared with the low-dose CPU Ⅱ group， the high-dose CPU Ⅱ group showed increased apoptotic cells （P<0.01）， up-regulated mRNA expression of miR-122 （P<0.01）， and increased expression of C/EBPα and HNF-4α proteins （P<0.01）. ConclusionCPU Ⅱ has an obvious inhibitory effect on the growth of transplanted hepatocellular carcinoma Hep3B cells in nude mice. The mechanism of action is related to enhancing the expression of transcription factors HNF-4α and C/EBPα， thereby promoting the expression of miR-122 and inhibiting the expression of its target gene IGF-1R.

Quality by Design approach for the investigation of critical characteristics of Phyllanthus emblica from different vicinities / 数字中医药（英文）

@#[Objective] To explore the application of Quality by Design (QbD) tools in assessing geographical variations of Phyllanthus emblica (P. emblica) from five distinct Indian states. [Methods] In the current experiment, the Box-Behnken design with a reduced quartic model and 105 runs was employed with the use of the Design Expert software for randomized response surface mapping. Three different extraction methods (Soxhlet, maceration, and sonication) along with three solventst [distilled water, methanol, and water-methanol mixture (50 : 50 v/v)] were considered in the present study. The anti-oxidant activities, total flavonoid content (TFC), and total phenolic content (TPC) in the P. emblica were determined and analysed by gas chromatography-mass spectrometry (GC-MS) to identify the major components. [Results] The QbD overlay plot showed that the extractive value of the P. emblica was no less than 30% w/w, 2,2-diphenyl-1-picrylhydrazyl (DPPH) no less than 60% mcg/mL (micrograms per millilitre), TFC no less than 75 mg QE/g (milligrams of quercetin equivalents per gram), and TPC no less than 80 mg GAE/g (milligrams of gallic acid equivalents per gram). Moreover, the GC-MS data confirmed the presence of variation in the bioactives of P. emblica extracts. [Conclusion] The model was significant in describing the variation in extractive value, DPPH, TFC, and TPC. The QbD approach may tend to prioritize thoroughness in the extraction process, ultimately resulting in improved quality in the extracted products.

A new class of potent liver injury protective compounds: Structural elucidation, total synthesis and bioactivity study

A new class of potent liver injury protective compounds, phychetins A-D ( 1- 4) featuring an unique 6/6/5/6/5 pentacyclic framework, were isolated and structurally characterized from a Chinese medicinal plant Phyllanthus franchetianus. Compounds 2- 4 are three pairs of enantiomers that were initially obtained in a racemic manner, and were further separated by chiral HPLC preparation. Compounds 1- 4 were proposed to be originated biosynthetically from a coexisting lignan via an intramolecular Friedel-Crafts reaction as the key step. A bioinspired total synthesis strategy was thus designated, and allowed the effective syntheses of compounds 2- 4 in high yields. Some of compounds exhibited significant anti-inflammatory activities in vitro via suppressing the production of pro-inflammatory cytokine IL-1β. Notably, compound 4, the most active enantiomeric pair in vitro, displayed prominent potent protecting activity against liver injury at a low dose of 3 mg/kg in mice, which could serve as a promising lead for the development of acute liver injury therapeutic agent.

Phyllanthi Fructus: A modal medicinal and food homologous item in quality evaluation / 中草药·英文版

Phyllanthi Fructus is a highly unique medicine and food homologous item, which exhibits distinctive flavor, notable nutritional value, and abundant pharmacological activity. It has enormous potential in the creation of health products and pharmaceuticals. However, due to the unique laws of quality formation and transfer of Phyllanthi Fructus, its appearance, shape, chemical compositions, nutrients, and sensory flavors are frequently greatly influenced by botanical resources, the processing and storage conditions. As a result, the current quality evaluation model is difficult to meet the needs of Phyllanthi Fructus as a medicine and food homologous item in the development of diversified products. This paper constructs the hierarchical utilization mode of Phyllanthi Fructus based on its unique quality formation and transmission laws, explores the quality evaluation model for food-oriented use and medicinal-oriented use, respectively, and systematically describes the quality evaluation idea under diversified application scenarios. This paper aims to serve as a reference for the construction of a quality evaluation model suitable for the medicine and food homologous item of Phyllanthi Fructus.

Comparative Repellency of Selected Plants to Adult Anopheles gambiea complex (Gilles) in the Laboratory

Aims: The study evaluated the repellency effects of some tropical plants and shrubs found in semi- rural communities of Badagry Area of Lagos state; which are acclaimed to have the potentials of repelling mosquitoes from human dwellings. The repellency effects of Moringa oleifera, Morinda lucida, Magnifera indica and Phyllanthus muellerianus to adult Anopheles gambiea was evaluated in the Laboratory. Study Design: The study was carried out at Central Research Laboratory of Lagos State University, Ojo, Lagos, Nigeria and Central Research Laboratory of University of Lagos, Akoka, Lagos, Nigeria. Powdered of dried test plants were prepared and admix with coconut husk as inert, different concentrations were rubbed on the forearm of volunteers and repellency to blood starved female Anopheles mosquitoes was observed. Methodology: Test plants were collected from Badagry area of Lagos State, they were identified at University of Lagos Herbarium and given numbers. They were dried between 10 and 14 days at temperature of 25-27oC and powdered. Different concentrations of the powder mixed with powdered coconut husk was used to treat volunteers forearms and they were exposed to 0-2 two day old adult unfed mosquitoes in an aluminum glass cage fitted with net as arm entrance and repellency was observed for a period of 180 minutes, with landing counts taken every 30 minutes. The test plants were also subjected to qualitative and quantitative phytochemical analysis at University of Lagos Central Research Laboratory. Results: Results showed that all test plants were able to repel Anopheles mosquitoes in the study, repellency was shown in descending order Moringa oleifera with 88%, Magnifera indica 83%, Phyllantus muellerianuss 80% and Morinda lucida 72%. There was no statistical significance in percentage repellency at 95% CL. The result of phytochemical screening of the test plants showed that only M .indica indicated presence of saponing (36.99%). While M.oleifera has highest phenol content (45.6%3), Alkaloid (38.68%), steroid (24.89%) and Tannin (33.19%). Flavonoid and reducing sugar quantity was highest in M. indica (39.39%) and (55.18%) respectively. Conclusion: The plants were able to show repellency to Anopheles gambiae a nuisance malaria vector of serious medical importance. These plants are available in all tropical areas of Africa, they can therefore be used to prevent nuisance and painful mosquito bites which could be a sustainable way to prevent mosquito vectored diseases

Phyllanthus amarus Aqueous Extract as Antidote to Alcoholic Liver Injury

Objective: In most human communities, the consumption of alcoholic beverages is unregulated with negative impact on health. The liver is one of the major organs that bear the brunt of regular and or heavy consumption of alcohol. This study set out to elucidate the modulation of alcohol induced liver injury in wistar rat by aqueous extract of Phyllanthus amarus plant. Methodology: Five groups of six animals each were used for the study. Group CN was the control. The alcohol only group (ALC) had 1ml / 100g body weight (b.w) of 43% ethanol. The Extract only group (EXT) had 200mg/ Kg b.w of P.amarus aqueous extract. The Low Extract plus Alcohol group (LEA) had concomitant administration of 1ml/100g b. w of 43% ethanol with 200 mg/ Kg of the extract. The High Extract plus Alcohol group (HEA) had concomitant administration of 1ml/100g b. w of 43% ethanol and the extract at 400 mg/ Kg. The alcohol and extract were administered once daily for fourteen days. Thereafter, blood samples were collected for biochemical analyses, the animals sacrificed and livers harvested for histopathological analyses. Results: Group HEA had the highest mean body weight. The mean liver weight of group EXT was significantly higher than those of other groups. Both the total protein and its globulin fraction of the ALC group were significantly lower than those of others. The liver enzymes (Alanine and Aspartate transaminases) levels were significantly low in the ALC group. However, those of the LEA and HEA groups were comparable with the EXT group. The glutathione peroxidase and superoxide dismutase activities of the LEA and HEA groups were significantly higher than that of ALC. Lipid peroxidation was most severe in the ALC group as evidenced by the significantly high malondialdehyde level. Histopathological sections of the liver revealed preserved hepatic architecture with pronounced steatosis in the ALC group. Conclusion: Aqueous extract of Phyllanthus amarus considerably reduced the severity of alcohol induced liver injury.

Phytochemical Screening and in vitro Antibacterial Activity of the Aqueous Extract of Phyllanthus niruri L. from Kasa� Oriental in DR Congo

Objectives: The aim of this work is to carry out a phytochemical study and to evaluate in vitro antibacterial potential of the aqueous extract of Phyllanthus niruri, a plant traditionally used in Kasai Oriental (DR Congo) against various bacteriosis and non-bacterial diseases. Study Design: P. niruri, was selected from a list resulting from an ethnobotanical survey carried out in Kasai Oriental because of the number of citations and recipes involving it, the level of preference of the species as well as the diversity of diseases treated and the plebiscite of its effectiveness by local traditional healers. To contribute to the enhancement of this plant traditionally used against various bacteriosis and to confirm its potential antibacterial power, it was subjected to phytochemical screening and its aqueous extract was tested in vitro on bacterial strains. Place and Duration of the Study: The period of this research went from December 2017 to February 2018. The analyzes were carried out at the physico-chemical and microbiological analysis laboratories of the Congolese Control Office of Mbujimayi (DR Congo) and at the Biology and Chemistry laboratories of the ISP Mbujimayi. Methodology: The chemical groups of the bioactive substances were sought using the classic methods of characterization in solution by precipitation, coloring and foam reactions. The diameters of the zones of inhibition, MICs and CMBs of the aqueous extract of this plant were determined in vitro against 20 bacterial strains subjected to the test. Results: P. niruri contains various bioactive chemical groups. Its aqueous extract showed antibacterial activity in vitro against several of 20 tested bacterial strains. According to the MICs and CMBs, the inhibitory action spectrum covers 12 bacterial strains out of the 20 tested. Conclusion: The results found confirm that P. niruri has antibacterial principles and a therapeutic potential by the presence of several bioactive substances and the inhibitory power of its aqueous extract on some bacterial strains tested.

Phyllanthaceae in the Atlantic Forest of northeastern Brazil / Phyllanthaceae na Mata Atlântica do Nordeste brasileiro

Abstract: The taxonomy of Phyllanthaceae Martinov in the Atlantic Forest of northeastern Brazil was updated through the analysis of approximately 200 specimens deposited in regional herbaria as well as field observations. Thirty-five species were recorded, belonging to seven genera: Amanoa Aubl. (1 species), Astrocasia B.L. Rob. & Millsp. (1), Discocarpus Klotzsch (1), Hieronyma Allemão (2), Margaritaria L.f. (1), Phyllanthus L. (28), and Richeria Vahl (1). Of the 35, six are new records for Alagoas State, two for Rio Grande do Norte, four for Paraíba, and six for Sergipe. Among the recorded species, 18 are endemic to Brazil, and of those, 11 are endemic to the Brazilian northeast and nine are exclusive to the Atlantic Forest. An identification key, comments on their taxonomy, phenology and geographic distributions, species conservation status, distribution maps, and illustrations of the species are provided.

Resumo: Este estudo teve como objetivo atualizar a taxonomia de Phyllanthaceae Martinov na Mata Atlântica do Nordeste brasileiro, através da análise de aproximadamente 200 espécimes depositados nos herbários da região e observação das espécies em campo. Foram registradas 35 espécies, pertencentes a sete gêneros: Amanoa Aubl. (1 espécie), Astrocasia B.L. Rob. & Millsp. (1), Discocarpus Klotzsch (1), Hieronyma Allemão (2), Margaritaria L.f. (1), Phyllanthus L. (29), e Richeria Vahl (1). Das 35 espécies, seis são novos registros para Alagoas, dois para o Rio Grande do Norte, quatro para Paraíba e seis para Sergipe. Dentre as espécies registradas, 18 são endêmicas do Brasil, destas, onze são endêmicas do Nordeste e nove são exclusivas da Mata Atlântica. São fornecidos chave de identificação, comentários taxonômicos, fenológicos e de distribuição geográfica, bem como o status de conservação das espécies. Além disso, são apresentados mapas de distribuição e ilustrações das espécies.

HPLC fingerprint studies and determination of six components in Phyllanthus urinaria L. collected from different habitats / 国际中医中药杂志

Objective:To establish a method of measuring the contents of gallic acid, brevifolin, corilagin, geraniin, ellagic acid and rutin in Phyllanthus urinaria L. simultaneously with fingerprint study for analysis. Methods:Phyllanthus urinaria L. was extracted by ultrasound with 50% methanol. Chromatographic separation was performed on a Phenonmenex Luna C18 (4.6 mm×250 mm, 5 μm). The mobile phase consisted of acetonitrile (A) and 0.1% phosphoric acid aqueous solution (B) with gradient elution. The flow rate was 1.0 ml/min. The column temperature was 25 ℃, and the injection volume was 10 μl. The detection wavelength was 270 nm. HPLC fingerprints of Phyllanthus urinaria L. from different habitats was established. PCA and OPLS-DA were used to analyze the differences in chemical components of different habitats. Results:Gallic acid, brevifolin, corilagin, geraniin, ellagic acid and rutin showed good linearity at 0.042 8-0.641 6, 0.033 4-0.501 4, 0.142 2-2.133 1, 0.383 1-5.746 5, 0.063 1-0.946 2 and 0.019 2-0.287 8 μg, respectively. The average recovery rate of them was 103.65%, 96.39%, 101.85%, 95.04%, 98.79% and 98.33%, respectively. The HPLC fingerprints of different habitats contained 14 characteristic common peaks, and six compounds characteristic peaks were identified. PCA analysis showed that the chemical components of Phyllanthus urinaria L. from different habitats were different. Geraniin, ellagic acid and corilagin were screened by OPLS-DA. Conclusions:The method is efficient, accurate and sensitive, which can be used to measure the six components in Phyllanthus urinaria L.. The established HPLC fingerprint of different habitats combined with the measrurement method of six components can be used for the quality control and evaluation of Phyllanthus urinaria L..

Actividad citotóxica y antiproliferativa in vitro del extracto acuoso de Phyllanthus comosus

RESUMEN Introducción: Desde los inicios de la medicina antigua, las plantas han sido utilizadas como tratamiento en diversas enfermedades incluyendo las de naturaleza infecto-contagiosa y el cáncer. Son numerosos los informes sobre las propiedades biológicas del género Phyllanthus. Objetivo: Evaluar la actividad citotóxica y antiproliferativa de un extracto acuoso de Phyllanthus comosus en tres líneas celulares, dos de origen tumoral (SiHa y HeLa) y una no tumoral (Vero). Métodos: La actividad citotóxica se evaluó mediante el método del MTT y la capacidad antiproliferativa mediante el ensayo de detección de inhibición de colonias o clonogénico. Se tuvieron en cuenta valores como la concentración citotóxica media (CC50), índice selectivo y porcentaje de disminución de la proliferación celular. Resultados: En el ensayo de citotoxicidad se obtuvieron CC50 similares para ambas líneas tumorales; mientras que el valor para la línea Vero resultó tres veces menos tóxico, con valores de índice de selectividad mayor que tres. El ensayo clonogénico demostró inhibición de la proliferación en las líneas tumorales, mientras que en células Vero no se observó inhibición de la capacidad de formación de colonias. Conclusiones: El extracto de P. comosus es más citotóxico para las líneas tumorales SiHa y HeLa que para las células Vero, no tumorales. Además, la inhibición de la formación de clonos celulares en ambas líneas tumorales evidencia su acción antiproliferativa y selectiva, lo que argumenta su potencialidad antitumoral in vitro

ABSTRACT Introduction: Ever since the onset of ancient medical practice, plants have been used to treat a variety of conditions, including infectious communicable diseases and cancer. A large number of reports are available about the biological properties of the genus Phyllantus. Objective: Evaluate the cytotoxic and antiproliferative activity of an aqueous extract of Phyllanthus comosus on three cell lines: two of tumoral origin (SiHa and HeLa) and one of non-tumoral origin (Vero). Methods: Cytotoxic activity was evaluated by the MTT method, and antiproliferative capacity by colony inhibition detection or clonogenic assay. Mean cytotoxic concentration (CC50), selective index and cell proliferation reduction percentage were some of the values taken into account. Results: The cytotoxicity assay obtained similar CC50 values for both tumor cell lines, whereas the value for the Vero line was three times less toxic, with a selectivity index above three. The clonogenic assay revealed proliferation inhibition in the tumor cell lines, whereas no inhibition of colony forming capacity was observed in Vero cells. Conclusions: The P. comosus extract is more cytotoxic for tumoral cell lines SiHa and HeLa than for non-tumor Vero cells. Additionally, inhibition of the formation of cell clones in both tumor cell lines is evidence of its antiproliferative and selective action, substantiating its in vitro antitumor potential.

Effect of Compound Phylanthus urinaria Ⅱ in Regulating Expression of lncRNA CCAT1 in Hepatocellular Carcinoma HepG2 Cells / 中国实验方剂学杂志

Objective:To explore the anti-hepatoma effect of compound <italic>Phylanthus urinaria</italic> Ⅱ （ CPU Ⅱ） by inhibiting the expression of the long non-coding RNA （lncRNA） colon cancer associated transcript-1 （CCAT1） and restoring the expression of microRNA let-7a. Method:Real-time fluorescence quantitative polymerase chain reaction （PCR） was used to detect the expression of lncRNA CCAT1 in normal liver cells （LO2 cells） and hepatocellular carcinoma HepG2 cells， and the differences in expression between these two types of cells were compared. The methylthiazolyl tetrazolium（MTT） assay was used to detect the proliferation of HepG2 cells after treatment with different concentrations of CPU Ⅱ and 5-fluorouracil（5-FU） for 24， 48 and 72 h. Hepatocellular carcinoma HepG2 cells were cultured <italic>in vitro </italic>and set into three gropes： cell control group， CPU Ⅱ low-dose group （0.8 g·L^-1） and high-dose group （1.6 g·L^-1）. Real-time PCR was used to detect the mRNA expression of lncRNA CCAT1， microRNA let-7a and its target genes high mobility group protein A2（HMGA2）， and N-RAS in each grope. Western blot was used to detect the protein expression of HMGA2， and Cyclin D₁ in each grope. Result:As compared with LO2 cells， expression of lncRNA CCAT1 in HepG2 cells was significantly up-regulated （<italic>P</italic><0.05）. Results of MTT assay showed that the 50% inhibiting concentration（IC₅₀）of CPU Ⅱ and 5-FU on hepatocellular carcinoma HepG2 cells was 1.649， 0.044 648 g·L^-1respectively. As compared with the control group， CPU Ⅱ high-and low-dose groups （1.6， 0.8 g·L^-1） significantly inhibited the proliferation of HepG2 cells （<italic>P</italic><0.05）， and the effect was most remarkable in CPU Ⅱ high-dose group （<italic>P</italic><0.05）. The results of Real-time PCR showed that as compared with control group， the expression of lncRNA CCAT1 mRNA was significantly inhibited in CPU Ⅱ high-and low-dose groups （<italic>P</italic><0.05）， and the expression of microRNA let-7a mRNA was obviously up-regulated in high-dose group （<italic>P</italic><0.05）， but the expression of HMGA2 mRNA in CPU Ⅱ high-and low-dose groups as well as the expression of N-RAS mRNA in CPU Ⅱ low-dose group were down-regulated （<italic>P</italic><0.05）. Western blot results showed that as compared with the cell control group， the protein expression of HMGA2 and Cyclin D₁ in CPU Ⅱ high-and low-dose groups （1.6， 0.8 g·L^-1） was significantly down-regulated （<italic>P</italic><0.05）. Conclusion:CPU Ⅱ can inhibit the expression of lncRNA CCAT1， recover the expression of microRNA let-7a， and suppress the mRNA and protein expression of related downstream target genes in hepatoma cells line HepG2， thereby inhibiting the proliferation of hepatocellular carcinoma cells and exerting anti-hepatocellular carcinoma effect.

Strategies and ideas of comprehensive development and utilization of medicine and food homologous variety Phyllanthus emblica / 中国中药杂志

Phyllanthus emblica is a kind of traditional medicine and medicinal and edible plant, with rich variety resources and high development value. It is a key poverty alleviation variety in China at present. As P. emblica processing industry is rising gradually in recent years, in order to fully develop and utilize its industrial resources, this paper systematically introduces current comprehensive development and utilization of P. emblica, discusses the problems in P. emblica processing industry, and puts forward comprehensive development and utilization strategies and industrial models in terms of cultivation, breeding, grading, quality evaluation and waste recycling, so as to provide a certain reference for promoting the high-quality development of P. emblica industry in China.

Phyllanthus fraternus manifests potent anti-proliferative activity on cultured Daudi cells

Objective: The aim of this study is to observe the apoptosis of Phyllanthus fraternus Webster against Daudi cells and to study its primary mechanism. Materials and Methods: Antiproliferative activity of cultured Daudi cells was evaluated using 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide assay in a dose- and time-dependent manner after treatment with the hydroalcoholic extract of P. fraternus . Trypan blue viability assay was also performed. Apoptosis induction in the cells posttreatment was determined by DNA fragmentation assay, Agarose gel electrophoresis, and Acridine orange/Ethidium bromide dual staining. Protein isolation and analysis was carried out using the standard polyacrylamide gel electrophoresis protocols. Results: The extracts inhibited the growth and proliferation of Daudi cells through induced cell death, which was dose-dependent and time-dependent. The IC50 value was found to be 220 μg/ml after 72 h of treatment. The induction of DNA fragmentation and increase in a number of apoptotic cells posttreatment suggest the possibility of apoptosis induction. A significant decrease in protein level was also observed. Conclusion: The results raise the possibility that the hydroalcoholic extract of P. fraternus could be a potent chemotherapeutic agent for the treatment of various cancers. Further evaluation of its potency as a chemotherapeutic agent is imperative

A new triterpenes isolated from leaves of Phyllanthus acidus / 中草药

Objective: To investigate the chemical constituents of the leaves of Phyllanthus acidus. Methods: All compounds were isolated by silica gel and Sephadex LH-20 gel column chromatographies as well as semi-preparative HPLC, and their structures were elucidated on the basis of physicochemical properties and spectral data. Results: Ten compounds were isolated and identified as 3α-cinnamoyloxyurs-20(29)-en-18β-ol (1), phyllanthol (2), maslinic acid (3), ovoideal E (4), quercetin-3-rhamnoside (5), 4-hydroxybenzoic acid (6), methyl 4-hydroxyphenylacetate (7), 4-O-(β-glucopyranosyloxy)-benzoic acid (8), thioacetic anhydride (9), L-pyroglutamic acid (10). Conclusion: Compound 1 is a new compound named as phyllanacidol B, and compounds 3-10 are obtained from P. acidus for the first time.

Analysis and comments on current development situation of whole industry chain of Phyllanthus emblica from perspective of patents / 中草药

Phyllanthi Fructus is a dried and ripe fruit that comes from Phyllanthus emblica of Euphorbiaceae. It is a characteristic Chinese and Tibetan medicine and one of homologous varieties of medicine and food with the breeding potential and development value. Abundant patents of P. emblica have been applied in recent years, which have advantages in food and beverages with rich downstream product development. However, the upstream industry chain has weak patent protection with low patents conversion rate, and the basic research of patent application is weak. Therefore, technological breakthroughs and technical protection in the upstream and middle reaches of the industrial chain should be strengthened. At the same time, the quality of patents should be improved, the status of varieties of P. emblica should be enhanced, the collaboration between industry, university and research institute should be strengthened and the basic and applied research should be improved. Based on the Incopat global patent database, the combination of patent analysis method and SWOT analysis method was used to analyze the status and development trends of domestic and foreign patents applications in P. emblica industrial chain, with a view to providing a reference for the development and utilization of P. emblica in the new era, industry chain patent layout and related industries, and the improvement of international competitiveness.

Cytotoxic activity of extracts and fractions from Paramignya trimera root and Phyllanthus amarus against pancreatic cancer cell lines

Objective: The aim of this study was to assess cytotoxic activity of extracts and fractions from the Paramignya trimera root (PTR) and Phyllanthus amarus (PA) against two pancreatic cancer cell lines (primary: BxPc3 and secondary: CFPAC1). Materials and Methods: The root of PT and whole plant of PA were used in this study. The extracts and fractions from the PTR and PA were prepared using microwave-assisted extraction and high-performance liquid chromatography, respectively. The cytotoxic activity was assessed using the Dojindo Cell Counting Kit-8 assay. Results: The findings showed impressive cytotoxic capacity of the PTR extract against both pancreatic cancer cells of BxPc3 and CFPAC1 in a range of concentrations from 50 to 200 μg/mL, which was higher than those of ostruthin (67 μM), gemcitabine (50 nM), and four its fractions (50 μg/mL), and to be comparable to a saponin-enriched extract from Quillaja bark at 200 μg/mL. In contrast, the cytotoxic capacity of the PA extract and nine its fractions against these pancreatic cancer cell lines was significantly lower (P < 0.05) than those of gemcitabine (50 nM) and Quillaja bark extract (200 μg/mL) and being comparable to phyllanthin (4.8 μM). The IC50 values of the PTR extract against BxPc3 and CFPAC1 cancer cells were 32.12 and 36.65 μg/mL, respectively, which was much lower than that of the PA extract against CFPAC1 cancer cells (128.81 μg/mL). Conclusion: The outcomes obtained from this study reveal that the PTR extract is a lead source for the potential development of novel antipancreatic cancer drugs and/or functional foods

Phyllanthus acidus (L.) Skeels and Rhinacanthus nasutus (L.) Kurz leaf extracts suppress melanogenesis in normal human epidermal melanocytes and reconstitutive skin culture

Objective: To determine the effect of extracts from Phyllanthus acidus (P. acidus) (L.) Skeels and Rhinacanthus nasutus (R. nasutus) (L.) Kurz leaves on melanogenesis and the underlying mechanism in normal human epidermal melanocytes (NHEM) and a reconstitutive skin model. Methods: NHEM and a reconstitutive skin model were stimulated with ethanol extracts of P. acidus (L.) Skeels and R. nasutus (L.) Kurz leaves. mRNA expression of microphthalmia-associated transcription factor (MITF), tyrosinase (TYR), tyrosinase-related protein 1 (TYRP1) and dopachrome tautomerase (DCT) were examined by real-time PCR. The melanin content in NHEM was also measured. Moreover, protein levels of tyrosinase were determined using western blot analysis. Results: In NHEM and the reconstitutive skin model, ethanol extracts from P. acidus (at 12.5 and 25.0 μg/mL) and R. nasutus (at 6.25 and 12.50 μg/mL) significantly diminished mRNA expression of MITF, TYR, TYRP1 and DCT in a concentration-dependent manner. P. acidus and R. nasutus extracts also reduced the amount of melanin in α-MSH-stimulated NHEM. Moreover, P. acidus and R. nasutus extracts markedly suppressed tyrosinase at the translational level in the reconstitutive skin model. Conclusions: P. acidus and R. nasutus extracts significantly reduced melanogenesis in NHEM and the reconstitutive skin model, suggesting that P. acidus and R. nasutus extracts can inhibit melanin synthesis through downregulation of MITF, TYR, TYRP1 and DCT. Therefore, the ethanol extracts of P. acidus and R. nasutus contain compounds that have the potential for development as a skin lightening agent for the treatment of hyperpigmentation disorder or melasma.

Acetylcholinesterase inhibition, antioxidant and identification of some chemical constituents of Phyllanthus atropurpureus cultivated in Egypt

Investigation of the lipid constituents of the aerial parts of Phyllanthus atropurpureus resulted in isolation and identification of the fatty acid mixture which consists of eight acids with linolenic acid as major and the unsaponifiable fraction that contain a series of hydrocabons, sterols, in addition to one triterpene (α-amyrin). The acetone insoluble fraction was found to contain two fatty alcohols and three n-hydrocabons in which the n-eicosane is the most abundant (44.16%). The flavonoidal constituents were isolated from ethyl acetate and butanol fractions which were identified as: luteolin-7-O-glucoside, kaempferol 3-O-(p-coumaroylglucoside), kaempferitrin, luteolin and kaempferol. Evaluation of different extracts as acetylcholinesterase inhibitors (AChI), established the chloroform fraction as a promising inhibitor of the enzyme. The antioxidant testing with DPPH radical revealed the potential of precipitate from MeOH extract as a radical scavenger.

Chemical constituents of Phyllanthus emblica and its anti-inflammation activities / 中草药

Objective: To study the chemical constituents and its anti-inflammtory activity effect of Phyllanthus emblica. Methods: The chemical constituents of P. emblica were isolated and purified by silica gel column chromatography, ODS column chromatography, Sephadex LH-20 column chromatography, semi-preparative high-performance liquid chromatography and recrystallization method. Through their spectra data, physical and chemical properties analysis, the structures of those compounds with high content were identified. LPS-induced RAW264.7 inflammatory cell model was established to evaluate the effect of compounds in P. emblica on proinflammatory factors (NO, IL-6, TNF-α, and MCP-1) of RAW264.7 inflammatory cells. Results: Totally, 14 compounds were isolated from P. emblica. and idetified as isovanillic acid (1), trans-cinnamic acid (2), p-hydroxybenzaldehyde (3), coniferyl aldehyde (4), quercetin (5), kaempferol-3-O-α-L-rhamnose (6), naringenin (7), 2-hydroxy-3-methyl phenylpropiolate (8), hydroquinone (9), myricetin (10), 2-furoic acid (11), methyl gallate (12), protocatechuic acid (13), gallic acid (14). The experiment of anti-inflammatroy effects showed that those compounds had different inhibitory effects on the production of inflammatory factors NO, IL-6, TNF-α and MCP-1. Conclusion: Compounds 1, 3, 4, 8-11 and 13 are isolated from P emblica for the first time. The anti-inflammatory effect of P. emblica is related to its phenolic acids.