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1. Protocols for in vitro culture and phytochemical analysis of phyllanthus species (euphorbiaceae).

Catapan E, Moreno FN, Luís Busi da Silva M, Otuki MF, Niero R, Filho VC, Augusto Yunes R, Viana AM.

Departamento de Botânica, Centro de Ciências Biológicas, Universidade Federal de Santa Catarina, Campus Universitário, 88040-900, Florianópolis, SC, Brasil.

We developed reproducible protocols for micropropagation, callus culture, and root culture of the medicinal plant Phyllanthus urinaria, P. niruri, P. tenellus, P. corcovadensis, P. caroliniensis, P. stipulatus, and P. fraternus by using single node explants. Genotype-linked differences are visible among the Phyllanthus species concerning shoot culture, callus culture, and root culture growth. The protocols developed for phytochemical screening of callus and root extracts of P. urinaria, P. caroliniensis, P. stipulatus, and P. fraternus have shown the production of sterols and triterpenes. Both compounds are known to account for the antinociceptive activity of the methanolic extracts as glochidone and stigmasterol have strong activity against neurogenic and inflammatory pain. Similarly, methanolic callus extracts of P. tenellus, P. niruri and P. corcovadensis have potent analgesic properties, however phenolics are major compounds isolated from these species. The optimized micropropagation, callus culture, and root culture protocols offer the possibility to use cell/root culture techniques for vegetative propagation and secondary metabolite studies.

PMID: 19521844 [PubMed - in process]


2. Mechanisms of antihyperuricemic effect of Phyllanthus niruri and its lignan constituents.

Murugaiyah V, Chan KL.

School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia.

ETHNOPHARMACOLOGICAL RELEVANCE: Phyllanthus niruri Linn. (Euphorbiaceae) is used as folk medicine in South America to treat excess uric acid. Our initial study showed that the methanol extract of Phyllanthus niruri and its lignans were able to reverse the plasma uric acid of hyperuricemic animals. AIM OF THE STUDY: The study was undertaken to investigate the mechanisms of antihyperuricemic effect of Phyllanthus niruri and its lignan constituents. MATERIAL AND METHODS: The mechanisms were investigated using xanthine oxidase assay and uricosuric studies in potassium oxonate- and uric acid-induced hyperuricemic rats. RESULTS: Phyllanthus niruri methanol extract exhibited in vitro xanthine oxidase inhibition with an IC(50) of 39.39mug/mL and a moderate in vivo xanthine oxidase inhibitory activity. However, the lignans display poor xanthine oxidase inhibition in vitro and a relatively weak in vivo inhibitory activity at 10mg/kg. On the other hand, intraperitoneal treatment with Phyllanthus niruri methanol extract showed 1.69 folds increase in urinary uric acid excretion when compared to the hyperuricemic control animals. Likewise, the lignans, phyllanthin, hypophyllanthin and phyltetralin exhibited up to 2.51 and 11.0 folds higher in urinary uric acid excretion and clearance, respectively. The co-administration of pyrazinamide with phyllanthin exhibited a significant suppression of phyllanthin's uricosuric activity resembling that of pyrazinamide with benzbromarone. CONCLUSIONS: The present study showed that the antihyperuricemic effect of Phyllanthus niruri methanol extract may be mainly due to its uricosuric action and partly through xanthine oxidase inhibition, whereas the antihyperuricemic effect of the lignans was attributed to their uricosuric action.

PMID: 19397979 [PubMed - as supplied by publisher]



3. Validated HPLC method for the standardization of Phyllanthus niruri (herb and commercial extracts) using corilagin as a phytochemical marker.

Colombo R, de L Batista AN, Teles HL, Silva GH, Bomfim GC, Burgos RC, Cavalheiro AJ, da Silva Bolzani V, Silva DH, Pelícia CR, Guimarães FM, Heimberg MC.

Instituto de Química, Universidade Estadual Paulista, Araraquara, SP, Brazil. renatacolomb@gmail.com

Phyllanthus niruri L., commonly known in Brazil as 'quebra-pedra', has long been used in the treatment of diverse diseases and especially urolithiasis. The therapeutic effects of P. niruri are attributed to various compounds present in the plant, including the hydrolysable tannin corilagin. In the present study, high-performance liquid chromatography (HPLC-/PAD) profiles of leaves and commercial extracts of P. niruri were examined and three compounds, found to be present in all of the samples studied, were isolated by open column chromatography over C18)silica gel followed by preparative HPLC. These compounds were identified by nuclear magnetic resonance as corilagin, rutin and ethyl 3,4,5-trihydroxybenzoate. Corilagin, which has been proposed as a phytochemical marker for P. niruri, was employed as an external standard in the development and validation of a rapid and efficient qualitative and quantitative HPLC assay for the analyte. The method may be applied in the standardization of herbs and phytomedicines commercialized in Brazil as quebra-pedra.

PMID: 19277954 [PubMed - in process]



4. Medical expulsive therapy as an adjunct to improve shockwave lithotripsy outcomes: a systematic review and meta-analysis.

Schuler TD, Shahani R, Honey RJ, Pace KT.

St. Michael's Hospital, Toronto, Ontario, Canada. ts9@ualberta.ca

BACKGROUND AND PURPOSE: Modern shockwave lithotripsy (SWL) is associated with inferior results compared with the original Dornier HM3. To enhance SWL outcomes, improved patient selection based on radiographic features and modulation of shockwave delivery rate have been used. A growing body of evidence demonstrates the positive effect of medical expulsive therapy (MET) to improve spontaneous passage of urinary calculi. The purpose of this review is to tabulate the current available data that examine the addition of MET to SWL to enhance outcomes. MATERIALS AND METHODS: MEDLINE was searched with a strategy developed in conjunction with a medical librarian. Trials were included if patients were randomized to receive either a medical expulsive agent or placebo or standard therapy after SWL. Study quality was assessed according to the Cochrane Renal Group criteria. The data were analyzed using RevMan meta-analysis software. Subgroup analysis was performed with respect to MET agent used, stone size, and duration of follow-up. RESULTS: Four randomized trials were identified. MET agents varied, with two trials using tamsulosin, one using nifedipine, and a single trial using Phyllanthus niruri extract. Two trials included patients with renal calculi, one had patients with ureteral calculi, and the fourth included patients with both ureteral and renal calculi. The pool results of the four trials included 212 patients who received MET and 206 who received placebo. The absolute risk difference of a successful outcome after SWL with the addition of MET was significantly superior to control at 17% (95% confidence interval [CI] 9%-24%); means six patients need to be treated with MET to prevent a single unsuccessful SWL of six (95% CI 4-11). The effect of MET post-SWL was even more pronounced for stones larger than 10 mm with an absolute risk difference of 26% (95% CI, 9%-43%). CONCLUSIONS: MET post-SWL results in a significant increase in successful treatment outcomes. Further powered, randomized studies are encouraged.

PMID: 19245302 [PubMed - indexed for MEDLINE]


5. Effect of Phyllanthus niruri Linn. treatment on liver, kidney and testes in CCl4 induced hepatotoxic rats.

Manjrekar AP, Jisha V, Bag PP, Adhikary B, Pai MM, Hegde A, Nandini M.

Department of Biochemistry, Centre for Basic Sciences, Kasturba Medical College, Bejai, Mangalore 575 004, India.

Phyllanthus niruri extract is extensively used in treating liver ailments. Effects of aqueous extract of P. niruri on liver, kidney and testes of CCl4 induced hepatotoxic rats were studied. High levels of malondialdehyde (MDA) were observed in the CCl4 test group with significant reduction of MDA levels in all groups on P. niruri extract administration. Highest levels of glutathione (GSH) were found in P. niruri group. Activities of alanine transaminase, aspartate transaminase and alkaline phosphatase enzymes were significantly reduced in the curative group (P. niruri treatment after CCl4 injection). Histopathology of liver showed lesser degree of inflammation in all P. niruri treated groups while the renal and seminiferous tubules showed eosinophilic protein casts with signs of tubular damage and degeneration. Testes also showed decreased amount of mature spermatozoa. The results suggest that P. niruri has anti-oxidant and hepato-protective activity with associated deleterious effects on kidney and testes.

PMID: 18807755 [PubMed - in process]


6. Ayurvedic medicine and renal calculi.

Kieley S, Dwivedi R, Monga M.

Department of Urologic Surgery, University of Minnesota, Minneapolis, MN 55455, USA.

OBJECTIVE: To explore the supportive evidence for the use of Ayurvedic medicine in the management of existing and recurrent nephrolithiasis. METHOD: Nine Ayurvedic medicines commonly utilized in the management of nephrolithiasis were identified by discussions with Ayurvedic practitioners in India. Mechanistic and clinical studies evaluating the use of these agents were identified using the Medline database and bibliographies suggested by Ayurvedic practitioners. The articles were then critically reviewed and summarized. RESULTS: Four in vitro mechanistic studies, eight animal studies, and seven human trials were identified. Phyllanthus niruri has undergone mechanistic in vitro, animal, and clinical trials that support its impact on calcium oxalate crystallization. Preliminary clinical trials have evaluated the role of Dolichos biflorus and Orthosiphon grandiflorus in the prevention of urolithiasis and fish stone as a method of stone expulsion, yet the treatment effect and mechanism of action remains to be elucidated. CONCLUSION: Ayurvedic medicine holds promise as a complementary approach to the management and prevention of nephrolithiasis. The best studied compound is P. niruri. Further controlled randomized clinical trials are justified to support or refute the potential benefits demonstrated in these initial studies.

PMID: 18620498 [PubMed - indexed for MEDLINE]


7. Symptomatic treatment of acute tonsillo-pharyngitis patients with a combination of Nigella sativa and Phyllanthus niruri extract.

Dirjomuljono M, Kristyono I, Tjandrawinata RR, Nofiarny D.

Department of Ear, Nose, Throat, Faculty of Medicine, University of Airlangga/Dr. Soetomo General Hospital, Surabaya, Jakarta, Indonesia. eleanora.anggiara@dexa-media.com

Acute tonsillopharyngitis is characterized by tonsil or pharyngeal inflammation and mostly is a virus in origin; thus, treatment that covers both the inflammation and inadequate immune response against the pathogenic organism is needed. NSPN extract containing Nigella sativa and Phyllanthus niruri extracts has both antiinflammatory and immunomodulatory effects. A comparative, parallel, randomized, double-blind, placebo-controlled study with a treatment period of 7 days was conducted to examine clinical effectiveness of Nigella sativa and Phyllanthus niruri extract (NSPN extract). Of 200 enrolled patients, 186 patients completed the study, 12 patients withdrew and 2 patients were principally screened failure but inadvertently included. NSPN capsules, each containing 360 mg Nigella sativa and 50 mg Phyllanthus niruri extracts, were orally administered 3 times 1 capsule daily for 7 days. At Hour 5 or 6 of the first dosing of study medication, the sore throat assessed as swallowing pain and difficulty, was markedly alleviated in the NSPN group. In line with the significant alleviation of pain, from Days 0 to 2 of treatment, subjects in the NSPN group also needed significantly less escape âanalgesicâ therapy (paracetamol tablets) than those in the placebo group. At the end of treatment (Day 7), a significantly greater proportion of patients in the NSPN group than in the placebo group had their sore throat completely relieved. NSPN extract was also found to be safe and well tolerated in acute tonsillopharyngitis patients. This study proved significant benefits of NSPN extract in the treatment of acute tonsillopharyngitis as compared to placebo.

PMID: 18541126 [PubMed - indexed for MEDLINE]


8. Chemical and immunological modifications of an arabinogalactan present in tea preparations of Phyllanthus niruri after treatment with gastric fluid.

Mellinger CG, Cipriani TR, Noleto GR, Carbonero ER, Oliveira MB, Gorin PA, Iacomini M.

Departamento de Bioquímica e Biologia Molecular, Universidade Federal do Paraná, Centro Politécnico 81531-980, Curitiba, PR, Brazil.

An arabinogalactan (AG) obtained from tea preparations of Phyllanthus niruri was previously investigated and presented immunological properties when tested with peritoneal mice macrophages. AG was now submitted to acidic and neutral gastric conditions using human gastric fluids and aq. HCl solution. Since the acidic procedures gave rise to the same free monosaccharidic composition, the acid hydrolyzate of AG at pH 2.00 was treated with ethanol to form insoluble (AG-P) and soluble fractions (AG-S). These were analyzed using (13)C NMR, HPSEC, and GC-MS for monosaccharide composition and methylation analyses. The results showed an intense partial degradation, including cleavages of the main chain. AG-S presented the monosaccharides released from the native polymer and some oligosaccharides as shown by methylation data. AG-P contained larger molecular fragments comprising the internal units from AG, which were not attacked by the hydrolysis condition. Both fractions were tested in peritoneal mice macrophages and remained active, promoting an increase of superoxide anion production of 2.0 and 2.3-fold, at 250 microg/mL, for AG-S and AG-P, respectively. When compared to AG, a slight diminished response was observed, revealing a structure-activity relation. The significance of the results is that most plant extracts are orally ingested and will reach the gastrointestinal tract before performing a biological function, so checking these changes is crucial to propose future clinical therapies based on the rational use of phytomedicine.

PMID: 18501421 [PubMed - indexed for MEDLINE]


9. Hepatocytes are protected by herb Phyllanthus niruri protein isolate against thioacetamide toxicity.

Sarkar MK, Sil PC.

Department of Chemistry, Bose Institute, 93/1, Acharya Prafulla Chandra Road, Kolkata 700009, West Bengal, India.

The herb, Phyllanthus niruri has been known to possess protective activity against various drugs and toxins induced hepatic disorders. Present study was conducted to evaluate the role of the protein isolate of the herb against thioacetamide (TAA)-induced cytotoxicity in mice hepatocytes. In vitro cell viability, lactate dehydrogenase (LDH) and alanine amino transferase (ALT) leakage were measured as the indicators of cell damage. In addition, measurement of the level of non-protein thiol, glutathione (GSH); activities of the antioxidant enzymes, superoxide dismutase (SOD), catalase (CAT) and glutathione S-transferase (GST) as well as the extent of lipid peroxidation were carried out to evaluate the prooxidant-antioxidant status of the cell. 2,2-Diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay was performed to determine the radical scavenging activity of the protein isolate. Results showed that the administration of the protein isolate prior to TAA exposure significantly reduced the release of LDH and ALT leakage and enhanced the cell viability in a dose-dependent manner in hepatocytes. Besides, the protein isolate appeared to prevent the alterations in GSH levels and activities of the anti-oxidant enzymes related to prooxidant-antioxidant status of hepatocytes. It also reduced the TAA-induced lipid peroxidation significantly as demonstrated by the reduction of malondialdehyde (MDA) production. DPPH radical scavenging assay showed that the protein isolate possessed radical scavenging activity. Combining, the data suggest that the protein isolate could protect hepatocytes from TAA-induced cellular injury probably by its antioxidative and radical scavenging properties.

PMID: 17913477 [PubMed - in process]


10. Nematicidal prenylated flavanones from Phyllanthus niruri.

Shakil NA, Pankaj, Kumar J, Pandey RK, Saxena DB.

Division of Agricultural Chemicals, Indian Agricultural Research Institute, New Delhi 110 012, India. iamshakil@gmail.com

Two prenylated flavanones have been isolated from the hexane extract of Phyllanthus niruri plant. The structure of these flavanones were established as 8-(3-Methyl-but-2-enyl)-2-phenyl chroman-4-one (1) and 2-(4-hydroxyphenyl)-8-(3-methyl-but-2-enyl)-chroman-4-one (2) on the basis of spectral analysis. These were evaluated for nematicidal activity against root-knot, Meloidogyne incognita, and reniform, Rotylenchulus reniformis, nematodes. Compound 2 exhibited nematicidal activity at par with the standard carbofuran (LC50 3.3 and 3.1ppm, respectively) when tested against reniform nematode. The LC50 value against root-knot nematode was found to be 14.5ppm. Compound 1 however, showed moderate activity against both the test nematodes.

PMID: 17904597 [PubMed - indexed for MEDLINE]


11. In vitro and in vivo antiplasmodial activity and cytotoxicity of extracts of Phyllanthus niruri L. herbs traditionally used to treat malaria in Indonesia.

Mustofa, Sholikhah EN, Wahyuono S.

Department of Pharmacology and Toxicology, Faculty of Medicine, Gadjah Mada University, Yogyakarta, Indonesia. mustofajogja@yahoo.com

In endemic areas where malaria is prevalent, medicinal plants are often used to treat malaria. This study was conducted to evaluate the in vitro and in vivo antiplasmodial activity and cytotoxicity of extracts of meniran (Phyllanthus niruri L.) herb traditionally used to treat malaria in Indonesia. Three extracts viz aqueous, methanolic and chloroformic extracts were obtained by maceration of the herbs. A radioactive method was used to evaluate the in vitro antiplasmodial activity of the extracts on chloroquine-resistant (FCR-3) and chloroquine-sensitive (D-10) strains of Plasmodium falciparum. In vitro antiplasmodial activity was expressed by the concentration inhibiting 50% of parasite growth (IC50). Cytotoxicity was estimated on Hela cells and the Cytotoxicity Index (CI = IC50 on HeLa cells/IC50 on FCR-3 strain) was calculated to evaluate the safety of tested extracts. A standard 4-day test on P berghei infected mice was used to evaluate the in vivo antiplasmodial activity of the extracts showing strong in vitro antiplasmodial activity, for both the methanolic and aqueous extracts. The in vivo antiplasmodial activity was expressed by the dose inhibiting 50% of parasite growth (ED50). The IC50 values obtained for these extracts against P. falciparum ranged from 2.3 to 202.4 microg/ml. The methanolic extract was the most active in vitro extract with an IC50 that ranged from 2.3 to 3.9 microg/ml and a CI that ranged from 41.3 to 57.5. This was also the most in vivo active extract with an ED50 of 9.1 mg/kg/d. Further study will be conducted to isolate and purify active compounds presented in the methanolic extract.

PMID: 17882995 [PubMed - indexed for MEDLINE]


12. Eudragit E as excipient for production of granules and tablets from Phyllanthus niruri L spray-dried extract.

Pereira de Souza T, Martínez-Pacheco R, Gómez-Amoza JL, Petrovick PR.

Departamento de Farmácia, UFRN, Natal, Rio Grande do Norte, Brazil. tpsouza@ufrnet.br

The aim of this study was to investigate the feasibility of using Eudragit E as a granulating agent for a spray-dried extract from Phyllanthus niruri to obtain tablets containing a high dose of this product. The granules were developed by wet granulation and contained 2.5%, 5.0%, and 10.0% Eudragit E in the final product concentration. The tablets were produced on a single-punch tablet press by direct compression of granules using 0.5% magnesium stearate as a lubricant. The tablets were elaborated following a 2 x 3 factorial design, where Eudragit E concentration and compression force were the independent variables, and tensile strength and the extract release of the tablets were the dependent variables. All granules showed better technological properties than the spray-dried extract, including less moisture sorption. The characteristics of the granules were directly dependent on the proportion of Eudragit E in the formulation. In general, all tablets showed high mechanical resistance with less than 1% friability, less moisture sorption, and a slower extract release profile. The Eudragit E concentration and compression force of the tablets significantly influenced both dependent variables studied. In conclusion, Eudragit E was efficient as a granulating agent for the spray-dried extract, but additional studies are needed to further optimize the formulations in order to achieve less water sorption and improve the release of the extract from the tablets.

PMID: 17622112 [PubMed - indexed for MEDLINE]


13. Determination of four lignans in Phyllanthus niruri L. by a simple high-performance liquid chromatography method with fluorescence detection.

Murugaiyah V, Chan KL.

School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia.

A new and simple analytical method using HPLC with fluorescence detection was developed for the simultaneous determination of four lignans (phyllanthin, hypophyllanthin, phyltetralin and niranthin) in Phyllanthus niruri L. plant samples. Optimal separation was achieved with an isocratic mobile phase consisting of acetonitrile-water (55:45 v/v). The method recorded limits of detection (S/N=5) for phyllanthin at 0.61 ng/mL, hypophyllanthin at 6.02 ng/mL, phyltetralin at 0.61 ng/mL and niranthin at 1.22 ng/mL, being 80, 8, 80 and 40 times, respectively, lower when compared with those derived using HPLC-UV detection. The limits of quantification (S/N=12) were 4.88 ng/mL for phyllanthin and phyltetralin, 9.76 ng/mL for niranthin and 24.4 ng/mL for hypophyllanthin showing 40, 8 and 20 times, respectively, lower than those from the UV detection method. The within-day and between-day accuracy for the four lignans were between 98.1% and 102.9% while their precision values were below 2.2%. The mean recovery was between 92.5% and 110.1%. The method was then successfully applied for the quantification of lignans in P. niruri plant samples. The highest amount of lignans was found in the leaves followed by fruits, branches and stem, whilst the roots have the least amount of lignans.

PMID: 17418855 [PubMed - indexed for MEDLINE]


14. Phytochemicals from Phyllanthus niruri Linn. and their pharmacological properties: a review.

Bagalkotkar G, Sagineedu SR, Saad MS, Stanslas J.

Department of Biomedical Sciences, University Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia.

This review discusses the medicinal plant Phyllanthus niruri Linn. (Euphorbiaceae), its wide variety of phytochemicals and their pharmacological properties. The active phytochemicals, flavonoids, alkaloids, terpenoids, lignans, polyphenols, tannins, coumarins and saponins, have been identified from various parts of P. niruri. Extracts of this herb have been proven to have therapeutic effects in many clinical studies. Some of the most intriguing therapeutic properties include anti-hepatotoxic, anti-lithic, anti-hypertensive, anti-HIV and anti-hepatitis B. Therefore, studies relating to chemical characteristics and structural properties of the bioactive phytochemicals found in P. niruri are very useful for further research on this plant as many of the phytochemicals have shown preclinical therapeutic efficacies for a wide range of human diseases, including HIV/AIDS and hepatitis B.

PMID: 17331318 [PubMed - indexed for MEDLINE]


15. Inhibitory effects of methyl brevifolincarboxylate isolated from Phyllanthus niruri L. on platelet aggregation.

Iizuka T, Nagai M, Taniguchi A, Moriyama H, Hoshi K.

Faculty of Pharmaceutical Sciences, Hoshi University, Tokyo, Japan. iizuka@hoshi.ac.jp

A platelet-aggregatory inhibitor was isolated from the 50% MeOH extract of Phyllanthus niruri L. leaf. Its structure was determined to be methyl brevifolincarboxylate on the basis of the 1H-, 13C-NMR, and high-resolution mass spectral data. We compared the antiplatelet aggregatory effects of the constituent with adenosine, a well-known inhibitor of platelet aggregation. Platelet aggregation was induced by collagen or adenosine 5'-diphosphate as an activating agent; the extent of inhibition was monitored with a platelet aggregometer employing a laser-scattering method. The inhibitory effects of methyl brevifolincarboxylate were found to be as potent as adenosine that is known to act on an A2A subtype receptor.

PMID: 17268086 [PubMed - indexed for MEDLINE]


16. Analysis of lignans from Phyllanthus niruri L. in plasma using a simple HPLC method with fluorescence detection and its application in a pharmacokinetic study.

Murugaiyah V, Chan KL.

School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia.

A simple analytical method using HPLC with fluorescence detection was developed for the simultaneous determination of four lignans, phyllanthin (1), hypophyllanthin (2), phyltetralin (3) and niranthin (4) from Phyllanthus niruri L. in plasma. The method recorded limits of detection for 1, 2, 3 and 4 as 1.22, 6.02, 0.61 and 1.22 ng/ml, respectively, at a signal-to-noise ratio of 5:1 whereas their limits of quantification were 4.88, 24.41, 4.88 and 9.76 ng/ml, respectively, at a signal-to-noise ratio of 12:1. These values were comparable to those of other sensitive methods such as gas chromatography-mass spectrometry (GC-MS), high-performance liquid chromatography-MS (HPLC-MS) and HPLC-electrochemical detection (HPLC-ECD) for the analysis of plasma lignans. A further advantage over known methods was its simple protocol for sample preparation. The within-day and between-day accuracies for the analysis of the four lignans were between 87.69 and 110.07% with precision values below 10.51%. Their mean recoveries from extraction were between 91.39 and 114.67%. The method was successfully applied in the pharmacokinetic study of lignans in rats. Following intravenous administration, the lignans were eliminated slowly from the body with a mean clearance of 0.04, 0.01, 0.03 and 0.02 l/kg h and a mean half-life of 3.56, 3.87, 3.35 and 4.40 h for 1, 2, 3 and 4, respectively. Their peak plasma concentration upon oral administration was 0.18, 0.56, 0.12 and 0.62 microg/ml, respectively, after 1h. However, their absorption was incomplete with a calculated absolute oral bioavailability of 0.62, 1.52, 4.01 and 2.66% for 1, 2, 3 and 4, respectively.

PMID: 17261384 [PubMed - indexed for MEDLINE]


17. Protein isolate from the herb, Phyllanthus niruri L. (Euphorbiaceae), plays hepatoprotective role against carbon tetrachloride induced liver damage via its antioxidant properties.

Bhattacharjee R, Sil PC.

Department of Chemistry, Bose Institute, 93/1, Acharya Prafulla Chandra Road, Kolkata 700009, West Bengal, India.

Phyllanthus niruri L. (Euphorbiaceae) (P. niruri) is a well-known hepatoprotective herbal plant. In the present study, hepatoprotective potential of the protein isolate of P. niruri was investigated against carbon tetrachloride (CCl(4)) induced liver damage in vivo. Protein isolate of P. niruri was intraperitoneally injected in mice either prior to (preventive) or after the induction of toxicity (curative). Levels of different liver marker enzymes in serum and different anti-oxidant enzymes, as well as lipid peroxidation products and glutathione (GSH) in liver homogenates were measured in normal, control (toxicity induced) and protein isolate treated mice. Administration of CCl(4) increased the serum glutamate pyruvate transaminase (GPT) and alkaline phosphatase (ALP) levels of mice sera along with increased lipid peroxidation and reduced levels of antioxidant enzymes superoxide dismutase (SOD) and catalase (CAT) in the liver. Treatment with the protein isolate of P. niruri significantly altered these changes to almost normal. The protein isolate also showed protective properties as was evidenced in histopathological studies. Results suggest that the protein isolate of P. niruri protects liver tissues against oxidative damage and somehow helps stimulating repair mechanism present in liver. It could be used as an effective hepatoprotector against CCl(4) induced liver damage.

PMID: 17175085 [PubMed - indexed for MEDLINE]


18. Hepatoprotective effect of aqueous extract of Phyllanthus niruri on nimesulide-induced oxidative stress in vivo.

Chatterjee M, Sil PC.

Department of Chemistry, Bose Institute, 93/1, Acharya Prafulla Chandra Road Kolkata-700009, India.

Nimesulide (NIM), an atypical non-steroidal anti-inflammatory drug (NSAID) is also used as analgesic. In the present study, we evaluated its effect on the prooxidant-antioxidant system of liver and the hepatoprotective potential of aqueous extract of the herb Phyllanthus niruri (PN) on NIM-induced oxidative stress in vivo using a murine model, by determining the activities of hepatic anti-oxidant enzymes superoxide dismutase (SOD) and catalase (CAT), levels of reduced glutathione (GSH) and lipid peroxidation (expressed as malonaldialdehyde, MDA). Aqueous extract of PN at a dose of 50 or 100 mg/kg body wt was administered either intraperitoneally or orally for 7 days, before NIM administration at a dose of 8 mg/kg body wt twice daily for 7 days in mice. Animals were sacrificed 24 h after administration of final dose of NIM. In another set of experiments, both aqueous extract of PN (at a dose of 50 or 100 mg/kg body wt) and NIM (8 mg/kg body wt) were administered simultaneously for 7 days. Animals were sacrificed 24 h after administration of final dose of the extract and NIM, liver tissues were collected, and the activities of SOD and CAT and levels of GSH and lipid peroxidation end-product (as MDA), were determined from the livers of all the experimental animals. Appropriate NIM control was maintained for all sets of experiments. NIM administration (8 mg/kg body wt) for 7 days caused significant depletion of the levels of SOD, CAT and reduced GSH, along with the increased levels of lipid peroxidation. Intraperitoneal administration of the extract at a dose of 50 mg/kg body wt for 7 days,. prior to NIM treatment, significantly restored most of the NIM-induced changes and the effect was comparable to that obtained by administering 100 mg/kg body wt of the extract orally. Thus, results suggested that intraperitoneal administration of the extract could protect liver from NIM-induced hepatic damage more effectively than oral administration. Antioxidant property of the aqueous extract of PN was also compared with that of a known potent antioxidant, vitamin E. The PN extract at a dose of 100 mg/kg body wt along with NIM was more effective in suppressing the oxidative damage than the PN extract at a dose of 50 mg/kg body wt. Results suggested that beneficial effect of the aqueous extract of PN, probably through its antioxidant property, might control the NIM-induced oxidative stress in the liver.

PMID: 17133737 [PubMed - indexed for MEDLINE]


19. Antihyperuricemic lignans from the leaves of Phyllanthus niruri.

Murugaiyah V, Chan KL.

School of Pharmaceutical Sciences, Universiti Sains Malaysia, Malaysia.

The methanol extract from the leaves of Phyllanthus niruri L. showed oral antihyperuricemic activity in potassium oxonate- and uric acid-induced hyperuricemic rats. Fractionation of the extract by resin chromatography led to the isolation of a less polar fraction which exhibited the highest reduction of plasma uric acid. Further antihyperuricemic-guided purification of the fraction afforded three lignans, phyllanthin (1), hypophyllanthin (2) and phyltetralin (3), of which 1 significantly reversed the plasma uric acid level of hyperuricemic animals to its normal level in a dose-dependent manner, comparable to that of allopurinol, benzbromarone and probenecid which are used clinically for the treatment of hyperuricemia and gout. Thus, the lignans of P. niruri are potential antihyperuricemic agents worthy of further investigation.

PMID: 16953466 [PubMed - indexed for MEDLINE]


20. Effect of extract of Phyllanthus niruri on crystal deposition in experimental urolithiasis.

Barros ME, Lima R, Mercuri LP, Matos JR, Schor N, Boim MA.

Department of Medicine, Renal Division, Federal University of São Paulo, São Paulo, SP, Brazil.

Phyllanthus niruri (Pn) is a plant that has been shown to interfere in the growth and aggregation of calcium oxalate (CaOx) crystals. In the present study we evaluated the effect of Pn on the preformed calculus induced by introduction of a CaOx seed into the bladder of male Wistar rats. Pn treatment (5 mg/ rat/day) was initiated immediately or 30 days after CaOx seeding and thus in the presence of a preformed calculus. Animals were sacrificed 50 or 70 days after surgery. The resulting calculi were weighed and analyzed by X-ray diffraction, stereomicroscopy and scanning electronic microscopy. Precocious Pn treatment reduced the number (75%, P < 0.05) and the weight (65%, P < 0.05) of calculi that frequently exhibited a matrix-like material on its surface, compared to the untreated CaOx group. In contrast, Pn treatment in the presence of a preformed calculus did not prevent further calculus growth; rather, it caused an impressive modification in its appearance and texture. Calculi from Pn-treated animals had a smoother, homogeneous surface compared to the spicule shape of calculi found in the untreated CaOx group. XRD analysis revealed the precipitation of struvite crystals over the CaOx seed and Pn did not change the crystalline composition of the calculi. This suggests that Pn interfered with the arrangement of the precipitating crystals, probably by modifying the crystal-crystal and/or crystal-matrix interactions. Results suggest that Pn may have a therapeutic potential, since it was able to modify the shape and texture of calculi to a smoother and probably more fragile form, which could contribute to elimination and/or dissolution of calculi.

PMID: 16896689 [PubMed - indexed for MEDLINE]


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