Chemometric profiling and anti-arthritic activity of aerial parts of Glinus oppositifolius (L.) Aug. DC.

ETHNOPHARMACOLOGICAL RELEVANCE: Glinus oppositifolius (L.) Aug. DC. belongs to the family Molluginaceae, an annual prostrate herb traditionally used to treat inflammations, arthritis, malarial, wounds, fevers, diarrhoea, cancer, stomach discomfort, jaundice, and intestinal parasites. However, the anti-arthritic activity of the aerial part has still not been reported. AIM OF THE STUDY: To investigate the antioxidant and anti-arthritic activity of G. oppositifolius in Complete Freund's Adjuvant (CFA) induced rats. MATERIALS AND METHODS: The dried aerial parts of this plant material were defatted with n-hexane and extracted by methanol using a soxhlet apparatus. The in vitro anti-arthritic activity of methanolic extract of G. oppositifolius (MEGO) was evaluated in protein denaturation, membrane stabilization, and inhibition of proteinase assay at 25, 50, 100, 200, and 400 µg/ml concentrations. Female Wistar rats were immunized sub-dermally into the right hind paw with 0.1 ml of CFA. Rats were administered with MEGO at doses of 200 and 400 mg/kg once daily for fourteen days after arthritis induction. Assessment of arthritis was performed by measuring paw diameter, arthritic index, arthritic score, body weight, organ weight, and hematological and biochemical parameters, followed by the analysis of pro-inflammatory cytokines such as tumor necrosis factor-alpha (TNF-α), interleukin 6 (IL-6), interleukin-1-beta (IL-1ß), cyclooxygenase-2 (COX-2), interleukin 13 (IL-13) and interleukin 10 (IL-10) and histopathological study. In vivo antioxidant effect was investigated in enzymatic assays. The presence of phytoconstituents was analyzed by Gas Chromatography-Mass Spectrometry (GC-MS) and Liquid Chromatography-Mass Spectrometry (LC-MS), respectively. In silico molecular docking study of the compounds was carried out against COX-2, IL-1ß, IL-6, and TNF-α using AutoDock 4.2 and BIOVIA-Discovery Studio Visualizer software. RESULTS: MEGO's in vitro anti-arthritic activity showed dose-dependent inhibition of protein denaturation, membrane stabilization, and proteinase inhibition, followed by significant in vivo anti-arthritic activity. The rats treated with MEGO showed tremendous potential in managing arthritis-like symptoms by restoring hematological, biochemical, and histological changes in CFA-induced rats. MEGO (200 and 400 mg/kg) showed a significant alleviation in the levels of hyper expressed inflammatory mediators (TNF-α, IL-1ß, and IL-6) and oxidative stress (SOD, CAT, GSH, and LPO) in CFA-induced rats. Spergulagenin-A as identified by LC-MS analysis, exhibited the highest binding affinity against COX-2 (-8.6), IL-1ß (7.2 kcal/mol), IL-6 (-7.4 kcal/mol), and TNF-α (-6.5 kcal/mol). CONCLUSIONS: Provided with the comprehensive investigation, methanolic extract of G. oppositifolius against arthritic-like condition is a proof of concept that revalidates its ethnic claim. The presence of Spergulagenin-A might be responsible for the anti-arthritic activity.

FAS and SREBP-1c Inhibition via AMPK Activation in HepG2 Cells by Biovip, Tox-off, and Traphanoside GO1 from Glinus oppositifolius.

Glinus oppositifolius is an endemic herbaceous plant found in tropical Asian countries and is native in Vietnam. It is used in traditional folk medicine because of its flavor and antiseptic and laxative effects. In the current research, the effects of Tox-off, Biovip, and the purified compounds isolated from G. oppositifolius in the previous study were evaluated on the activation of adenosine 5'-monophosphate-activated protein kinase (AMPK)-activated protein kinase (AMPK) and acetyl-coenzyme A carboxylase (ACC) in C2C12 myoblasts. In addition, the most potent active compounds, traphanoside-GO1 (TRA-GO1) and TRA-GO5 have validated the reduction of fatty acid synthase (FAS) and sterol regulatory element binding protein (SREBP)-1c in HepG2 cells. We found that Tox-off and Biovip significantly increased the phosphorylation of AMPK and ACC in C2C12 myoblasts. Furthermore, TRA-GO1 and TRA-GO5 significantly increased the AMPK activation and phosphorylation of its downstream substrate ACC in a concentration-dependent way compared to the dimethyl sulfoxide (DMSO) control. Besides, the protein level of FAS and SREBP-1c decreased by TRA-GO1 and TRA-GO5 in a concentration-dependent manner. Taken together, our results showed that the increased AMPK and ACC phosphorylation by active components of G. oppositifolius may activate the AMPK signaling pathways, which are useful for the anti-obesity and its related metabolic disorders.

Biosynthesis of Co3O4 nanomedicine by using Mollugo oppositifolia L. aqueous leaf extract and its antimicrobial, mosquito larvicidal activities.

Nanotechnology is a relatively revolutionary area that generates day-to-day advancement. It makes a significant impact on our daily life. For example, in parasitology, catalysis and cosmetics, nanoparticles possess distinctive possessions that make it possible for them in a broad range of areas. We utilized Mollugo oppositifolia L. aqueous leaf extract assisted chemical reduction method to synthesize Co3O4 nanoparticles. Biosynthesized Co3O4 Nps were confirmed via UV-Vis spectroscopy, scanning electron microscope, X-ray diffraction, EDX, Fourier-transform infrared, and HR-TEM analysis. The crystallite size from XRD studies revealed around 22.7 nm. The biosynthesized Co3O4 nanoparticle was further assessed for mosquito larvicidal activity against south-urban mosquito larvae Culex quinquefasciatus, and antimicrobial activities. The synthesized Co3O4 particle (2) displayed significant larvicidal activity towards mosquito larvae Culex quinquefasciatus with the LD50 value of 34.96 µg/mL than aqueous plant extract (1) and control Permethrin with the LD50 value of 82.41 and 72.44 µg/mL. When compared to the standard antibacterial treatment, Ciprofloxacin, the Co3O4 nanoparticle (2) produced demonstrates significantly enhanced antibacterial action against the pathogens E. coli and B. cereus. The MIC for Co3O4 nanoparticles 2 against C. albicans was under 1 µg/mL, which was much lower than the MIC for the control drug, clotrimale, which was 2 µg per milliliter. Co3O4 nanoparticles 2, with a MIC of 2 µg/mL, has much higher antifungal activity than clotrimale, whose MIC is 4 µg/mL, against M. audouinii.

Anti-inflammatory Activity of Mollugo cerviana Methanolic Extract in LPS-induced Acute Inflammatory RAW 264.7 Macrophages.

BACKGROUND: The management of acute inflammation, which arises from complex biological responses to harmful stimuli, is an important determinant in the recovery from an otherwise detrimental outcome such as septicemia. However, the side effects and limitations of current therapeutics necessitate the development of newer and safer alternatives. Mollugo cerviana is a common medicinal herb of the Indian subcontinent and has been traditionally used for its fever mitigating anti-microbial and hepatoprotective action. We have already reported the rich presence of radical scavenging phytochemicals in the plant extracts and their strong antioxidant properties. OBJECTIVE: In the present study, we have evaluated the anti-inflammatory effects of methanolic extract (ME) of the areal parts of M. cerviana in a lipopolysaccharide (LPS)-induced acute inflammatory cell culture model. METHODS: RAW 264.7 mouse macrophage cells were stimulated by the bacterial endotoxin LPS at a concentration of 1 µg/mL. Cytotoxicity and anti-inflammatory potential of ME were carried out. RESULTS: The concentration of M. cerviana extract up to 150 µg/ml was found to be non-toxic to cells (MTT and NRU assay). LPS induces acute inflammation by binding to TLR-4 receptors, initiating a downstream signalling cascade that results in pro-inflammatory cytokine secretion. Extract treatment at 100 µg/ml suppressed LPS-induced gene expression (qPCR) and secretion (ELISA) of pro-inflammatory cytokines IL-1ß, IL-6 and TNF-α, and the chemokine CCL2, leading to dampening of the acute inflammatory cascade. LPS-induced elevation of ROS level (DCFDA method) was significantly reduced by extract treatment. Nitric oxide production, as indicated by nitrite level, was significantly reduced post extract treatment. CONCLUSION: This study demonstrated that M. cerviana methanolic extract has a potent antiinflammatory effect in the in vitro acute inflammation model of LPS-stimulated RAW 264.7 cells. There is no reported study so far on the anti-inflammatory properties of M. cerviana in an LPSinduced acute inflammatory model, which closely mimics a human bacteremia response. Hence, this study highlights the therapeutic potential of this extract as a source of anti-inflammatory lead molecules.

Anti-inflammatory and anti-osteoarthritis effect of Mollugo pentaphylla extract.

CONTEXT: Mollugo pentaphylla L. (Molluginaceae) extract (MPE) has been reported to have anti-inflammatory effect on MSU-induced gouty arthritis in a mouse model. OBJECTIVE: This study examined the anti-inflammatory activities of an MPE in vitro and anti-osteoarthritis effects on monosodium iodoacetate (MIA)-induced osteoarthritis (OA) in vivo. MATERIALS AND METHODS: The dried whole plants of M. pentaphylla were extracted with 70% ethanol under reflux. The anti-inflammatory effect of MPE was evaluated in vitro in lipopolysaccharide (LPS)-treated RAW264.7 cells. The anti-osteoarthritic effect of MPE was investigated in a Sprague-Dawley rat model of MIA-induced OA. Each seven male rats were orally administered MPE (75, 150 or 300 mg/kg) or the positive control drug indomethacin (1 mg/kg) 3 days before MIA injection and once daily for 11 days thereafter. After the treatment with MPE, no evidence of systemic adverse effects was observed in any study group. RESULTS: MPE exhibited anti-inflammatory activity via inhibition of the production of NO (57.8%), PGE2 (97.1%) and IL-6 (93.2%) in LPS-treated RAW264.7 cells at 200 µg/mL. In addition, MPE suppressed IL-1ß (60.9%), TNF-α (37.9%) and IL- 6 (40.9%) production and suppressed the synthesis of MMP-2, MMP-9 and COX-2 in the MIA-induced OA rat model. CONCLUSIONS: These results demonstrate that MPE exerts potent anti-inflammatory activities and protects cartilage in an OA rat model. This might be a potential candidate for therapeutic OA treatment.

Effects of Mollugo pentaphylla extract on monosodium urate crystal-induced gouty arthritis in mice.

BACKGROUND: Gout is an inflammatory condition induced by the deposition of monosodium urate (MSU) crystals in joints and soft tissues, and it can lead to acute or chronic arthritis. MSU are pro-inflammatory stimuli that can initiate, amplify and sustain an intense inflammatory response. In this study, we evaluated the anti-inflammatory effect of an extract of Mollugo pentaphylla (MPE) on MSU-induced gouty arthritis in a mouse model. METHOD: An MSU crystal suspension (4 mg/50 µL) was injected intradermally into the right paw. The mice were orally administered MPE (150 mg/kg or 300 mg/kg) or the positive control drug colchicine (1 mg/kg) 1 h before the MSU crystals were injected and then once daily for 3 days. The effects of MPE included inflammatory paw edema and pain upon weight-bearing activity, and we evaluated the inflammatory cytokine expression and paw tissue inflammation-related gene expression. RESULTS: MPE suppressed inflammatory paw edema and pain in the MSU-induced mice. MPE showed anti-inflammatory activity by inhibiting the production of TNF-α, interleukin (IL)-1ß, NLRP3 inflammasome and NF-κB. CONCLUSION: These results suggest that MPE has potent anti-inflammatory activities and may be useful as a therapeutic agent against gouty arthritis.

Preliminary research concerning antinociceptive and antiinflammatory effects of two extracts from Glinus oppositifolius (L.) Aug. DC.

UNLABELLED: In Mali Glinus oppositifolius (L.) Aug. DC. (Aizoaceae) is used to treat inflammations and joint pains. AIM: The present study was designed to evaluate the antinociceptive and anti-inflammatory effects of the aqueous and ethanol extracts obtained from the aerial parts of the plant. MATERIAL AND METHODS: The aqueous and ethanol extracts (G-A1 and G-E1, respectively) were studied regarding their acute toxicity. The extracts were further evaluated in different models using nociceptive (chemical, thermal, mechanical) and inflammatory stimuli. Experimental protocol was implemented according to international regulations in animal experiments. RESULTS AND DISCUSSIONS: No acute toxicity was noticed for these two extracts. ED50 (mg/kg bw) values were determined in different nociception models: the constrictive abdominal response test (G-A1: 229.00 +/- 53.30; G-E1: 146.38 +/- 31.75), hot plate test (G-A1: 278.59 +/- 73.00; G-E1: 383.52 +/- 89.69), Randall-Selitto test (G-A1: 207.14 +/- 26.15), evaluation of the inflammatory edema test (G-A1: 228.31 +/- 13.84; G-E1: 62.55 +/- 89.69). CONCLUSIONS: The results of the inflammatory nociception studies show that G-E1 extract had a higher potency than G-A1 extract in the constrictive abdominal response test. Also, for the same level of anti-inflammatory activity, G-E1 extract was more potent than G-A1 extract. These results encourage further studies to separate, isolate and identify the phytochemicals responsible for the analgesic and anti-inflammatory effects.

Antioxidant activities and phenolic contents of extracts from Glinus oppositifolius aerial parts.

UNLABELLED: In Malian traditional medicine, aerial parts of Glinus oppositifolius are used in the treatment of many disorders, particularly inflammations and joint pains. AIM: The present study was initiated to investigate the antioxidant potential of Glinus oppositifolius. MATERIAL AND METHODS: Aqueous and ethanol extracts were prepared from the dried aerial parts. Both extracts were examined for the phenolic content and antioxidant activity. Total phenolic content was quantified by Folin-Ciocalteu method. Antioxidant activity was studied in vitro by evaluating the ability to scavenge different free radicals (ABTS, superoxide and hydroxyl radicals, nitric oxide) and to chelate ferrous ions. RESULTS: Aqueous extract was found to contain a higher level of total phenols than ethanol extract (1.27 +/- 0.04 vs. 0.94 +/- 0.05 g GAE/100 g extract). Both extracts lacked the ability to scavenge superoxide anion radical but scavenged ABTS and hydroxyl radicals, nitric oxide and chelated ferrous ions in a concentration-dependent manner. According to the EC50 values, aqueous extract showed stronger antioxidant effects than ethanol extract (174.32 +/- 1.49 vs. 276.76 +/- 1.52 microg/mL in ABTS radical cation scavenging assay, 119.91 +/- 1.70 vs. 240.57 +/- 0.97 microg/mL in nitric oxide scavenging assay, 1.99 +/- 0.01 vs. 6.54 +/- 0.08 mg/mL in ferrous ion chelating assay). In hydroxyl radical scavenging assay, aqueous extract had an EC50 value of 0.86 +/- 0.00 mg/mL while the EC50 value of ethanol extract was higher than the highest concentration that was tested (3.75 mg/mL). CONCLUSIONS: Our results clearly indicate the antioxidant potential of Glinus oppositifolius aerial parts and suggest that the antiinflammatory activity might be partly related to the antioxidant potential.

Laboratory assessment of molluscicidal and cercariacidal effects of Glinus lotoides fruits.

BACKGROUND: The negative impact of synthetic molluscicides on the environment and their high cost necessitated search for an alternative approach of using plant extracts for the control of schistosomiasis. The objective of this study was, therefore, to evaluate aqueous and ethyl acetate crude extracts of Glinus lotoides fruits for their cercariacidal activity and molluscicidal effect against schistosome snail intermediate hosts. METHODS: Assessment of the molluscicidal activity against Biomphalaria pfeifferi was made by immersion method in accordance with WHO guideline. The results of mortality were statistically analyzed using probit analysis. The attenuating effect of the plant on Schistosoma mansoni cercariae was determined using establishment of adult worms as a parasitological parameter post exposure. RESULTS: The 24 and 48 hour-LC50 values for the aqueous extract of G. lotoides fruits were 47.1 and 44.1 mg/L, respectively, whereas that of ethyl acetate were 66.1 and 59.6 mg/L, respectively. The 24 and 48 hour LC90 values for the aqueous extract of G. lotoides fruits were 56.96 and 51.0 mg/L, respectively, while that of ethyl acetate were 77.2 and 70.0 mg/L, respectively. The in vitro cercariacidal activity was determined after 2 hrs of exposure to the aqueous plant extract. It was found out that the LC50 and LC90 values were 18.7 and 41.7 mg/L, respectively. Besides, infectivity of Schistosoma mansoni cercariae to mice was determined by exposing mice to cercariae pre-treated with the sub-lethal concentrations (3.7, 11.6 and 18.7 mg/L) of the aqueous extract. A significant reduction in worm burden in mice was obtained at 11.6 mg/L (p < 0.05). Moreover, the reduction in number of worms recovered was highly significant at 18.7 mg/L (p < 0.001). CONCLUSIONS: The results showed that G. lotoides has molluscicidal activity against B. pfeifferi snails and cercariacidal activity against S. mansoni. Yet, further comprehensive evaluation is recommended for the possible use of G. lotoides against B. pfeifferi and the schistosome parasite.

Recent progress in Glinus oppositifolius research.

CONTEXT: Glinus oppositifolius (L.) Aug. DC. (Molluginaceae), a perennial subshrubs herb, grows at low altitudes in the southern part of Taiwan, and is used in traditional Chinese medicine for herpes zoster and herpangina. OBJECTIVE: This study describes nutritional and therapeutic potential of Glinus oppositifolius and summarizes scientific evidence that supports traditional claims; recent progress in research for this plant is reviewed herein. MATERIALS AND METHODS: The literature has been retrieved from the web-based online systems including PubMed, Medline, and Google Scholar. The articles related to phytochemistry, pharmaceutical biology and ethnopharmacology have been excluded. RESULTS AND DISCUSSION: In clinical practice, the plant has been extensively investigated in a broad range of studies to provide scientific evidence for folklore claims or to find new therapeutic uses. The present review may arouse related research and make a more valid display for Taiwanese native medicinal plants.

An in vitro study on the DNA damaging effects of phytochemicals partially isolated from an extract of Glinus lotoides.

An extract of Glinus lotoides, a medicinal plant used in Africa and Asia for various therapeutic purposes, was recently shown to cause DNA damage in vitro. To further explore the potential genotoxicity of this plant, fractionation of the crude extract was performed using reverse phase solid-phase extraction and a stepwise gradient elution of methanol in water. Four fractions were collected and subsequently analysed for their DNA damaging effects in mouse lymphoma cells using an alkaline version of the comet assay. To identify potential genotoxic and non-genotoxic principles, each fraction was then subjected to liquid chromatography coupled to mass spectrometry, LC-MS/MS. 1D and 2D nuclear magnetic resonance analyses were used to confirm the identity of some saponins. Although fractions containing a mixture of flavonoids and oleanane-type saponins or oleanane-type saponins alone produced no DNA damage, those containing hopane-type saponins exhibited a pronounced DNA damaging effect without affecting the viability of the cells. To conclude, even if this study presents evidence that hopane-type of saponins are endowed with a DNA damaging ability, further studies are needed before individual saponins can be cited as a culprit for the previously reported genotoxicity of the crude extract of G. lotoides.

Protective effect of Mollugo nudicaulis Lam. on acute liver injury induced by perchloroethylene in experimental rats.

OBJECTIVE: To evaluate the protective effect of ethanol extract of Mollugo nudicaulis (M. nudicaulis) against perchloroethylene-induced hepatotoxicity. METHODS: The hepatoprotective activity of the ethanol extract of M. nudicaulis (200 mg/kg body wt) was studied in percholoroethylene (1 000 mg/kg body wt) induced hepatotoxicity in Wistar albino rats. The serum levels of AST, ALT, ALP, bilirubin and the liver content of SOD, CAT, GPx, GST, GSH, vitamin C were assessed to evaluate the hepatoprotective and antioxidant activities of the extract. The activity of the extract was compared with silymarin, a standard reference drug. In addition, serum urea, uric acid and creatinine levels were measured to evaluate the kidney function. The histopathological examination of the liver tissues was observed to support the biochemical parameters. RESULTS: The results revealed that the extract significantly (P<0.05) restored the serum levels of AST, ALT, ALP, bilirubin and significantly (P<0.05) increased the antioxidant enzymes SOD, CAT, GPx, GST, GSH, vitamin C in perchloroethylene-induced rats to its normalcy. The biochemical observations were supported by the histopathological studies of the liver tissues. CONCLUSIONS: The results led to the conclusion that M. nudicaulis possess hepatoprotective and antioxidant activities against perchloroethylene-induced hepatotoxicity in rats.

Protective effect of Mollugo nudicaulis Lam. on acute liver injury induced by perchloroethylene in experimental rats

OBJECTIVE@#To evaluate the protective effect of ethanol extract of Mollugo nudicaulis (M. nudicaulis) against perchloroethylene-induced hepatotoxicity.@*METHODS@#The hepatoprotective activity of the ethanol extract of M. nudicaulis (200 mg/kg body wt) was studied in percholoroethylene (1 000 mg/kg body wt) induced hepatotoxicity in Wistar albino rats. The serum levels of AST, ALT, ALP, bilirubin and the liver content of SOD, CAT, GPx, GST, GSH, vitamin C were assessed to evaluate the hepatoprotective and antioxidant activities of the extract. The activity of the extract was compared with silymarin, a standard reference drug. In addition, serum urea, uric acid and creatinine levels were measured to evaluate the kidney function. The histopathological examination of the liver tissues was observed to support the biochemical parameters.@*RESULTS@#The results revealed that the extract significantly (P<0.05) restored the serum levels of AST, ALT, ALP, bilirubin and significantly (P<0.05) increased the antioxidant enzymes SOD, CAT, GPx, GST, GSH, vitamin C in perchloroethylene-induced rats to its normalcy. The biochemical observations were supported by the histopathological studies of the liver tissues.@*CONCLUSIONS@#The results led to the conclusion that M. nudicaulis possess hepatoprotective and antioxidant activities against perchloroethylene-induced hepatotoxicity in rats.

L-(-)-(N-trans-cinnamoyl)-arginine, an acylamino acid from Glinus oppositifolius (L.) Aug. DC.

An amino acid derivative, L-(-)-(N-trans-cinnamoyl)-arginine, was isolated from the whole plant of Glinus oppositifolius (L.) Aug. DC. along with kaempferol 3-O-galactopyranoside, isorhamnetin 3-O-beta-D-xylopyranosyl-(1-->2)-beta-D-galactopyranoside, vitexin, vicenin-2, adenosine and L-phenylalanine. The structure determinations were based on analyses of chemical and spectroscopic methods.

Anticancer activity and nutritional value of extracts of the seed of Glinus lotoides.

The purpose of this study is to determine the anticancer activity and the nutritional values of the seeds of Glinus lotoides, a plant used as a dietary vegetable and medicinal plant in Asia and Africa. To achieve this goal, the seeds were extracted in soxhlet using solvents, namely n-hexane, dichloromethane, methanol and water. The methanol and n-hexane extracts showed differential growth inhibitory responses in carcinoma cell lines (Calu-3 IC(50)=29.7 and 79.8 µg/mL and Caco-2 IC(50)=69.7 and 74.6 µg/mL, respectively) as compared to normal cell lines (MDCK IC(50)=106.1 and 131.1 µg/mL and IEC-6 IC(50)=134.0 and 128.5 µg/mL, respectively). In addition, these extracts induced significant apoptosis in the cancer cells (p<0.05) at 100 µg/mL. The seeds of G. lotoides were found to contain nutritional compounds of well-established chemopreventive activity, including vitamin E, folic acid, selenium and calcium. The hydrophilic oxygen radical absorption capacity (ORAC) value was found to be 123 µM Trolox Equiv./g, indicating the antioxidant activity of the plant. These data suggest that the seeds of G. lotoides could potentially be used in the diet in chemoprevention of cancer and warrant further confirmatory preclinical and clinical studies. The amount of protein, carbohydrate, fat, ash, moisture, sugar profile and fatty acids further support the nutritional value of the seeds.

Potential genotoxicity of plant extracts used in Ethiopian traditional medicine.

AIM OF THE STUDY: Although traditional herbal medicines are widely used in Ethiopia, no information is available on their potential genotoxicity. In the present study, hydroalcoholic extracts of Glinus lotoides, Plumbago zeylanica, Rumex steudelii and Thymus schimperi were evaluated for their DNA damaging effects using the comet assay. MATERIAL AND METHODS: Mouse lymphoma L5178Y cells were exposed to different concentrations of the extracts for 3h with and without metabolic activation (S9-mix) using 4-nitroquinoline-N-oxide and benzo(a)pyrene as positive controls, and vehicles as negative controls. RESULTS: In the absence of S9, all extracts were found to induce significant DNA damage without affecting the cell viability. T. schimperi and R. steudelii were the most potent DNA-damaging extracts, and G. lotoides and P. zeylanica the least potent. The addition of S9 had different effects on the DNA damage induced by the extracts: it lowered the DNA damaging effect of P. zeylanica, did not affect the DNA damaging effect of T. schimperi, and increased the DNA damaging effects of R. steudelii and G. lotoides. CONCLUSION: The findings of the present study suggest that all extracts evaluated have a genotoxic potential in vitro which needs to be substantiated by further studies.

Granulation by roller compaction and enteric coated tablet formulation of the extract of the seeds of Glinus lotoides loaded on Aeroperl 300 Pharma.

The purpose of this research was to improve the hygroscopicity and poor flow properties of the crude dry extract of the seeds of Glinus lotoides and improve the disintegration time of the core-tablets for enteric coated formulation thereof. The liquid crude extract of the plant was adsorbed on granulated colloidal silicon dioxide (Aeroperl 300 Pharma) at 30% w/w and the dry extract preparation (DEP) was dry-granulated with roller-compaction using Micro-Pactor. Hygroscopicity, flow property and disintegration time were improved significantly due to the adsorption and granulation processes. Moreover, the DEP does not become mucilaginous even at higher relative humidity levels (above 65%). Oblong tablets (20 x 8.25 mm) containing 947 mg of the granulated DEP (equivalent to the traditional dose), 363 mg of Avicel PH101 and 90 mg of Ac-di-Sol as disintegrant were formulated using an instrumented eccentric tablet machine at 20 kN. The tablets showed a crushing strength of 195 N, a friability of 0.4% and disintegrated within 9 min. The tablets were then enteric coated using polymethacrylate co-polymers (Eudragit L 100-55 and Kollicoat MAE 100P). The coated tablets resisted disintegration or softening in simulated gastric fluid for a minimum of 2 h and disintegrated within 15 min in intestine simulated fluid at pH 6.8. In addition to controlling the release of the active agents, the enteric coating improved the strength and decreased friability of the core-tablets.

Antibacterial and anti-inflammatory effects of Jeju medicinal plants against acne-inducing bacteria.

Propionibacterium acnes and Staphylococcus epidermidis are pus-forming bacteria that trigger inflammation in acne. The present study was conducted to evaluate the antimicrobial activities of Jeju medicinal plants against these etiologic agents of acne vulgaris. Ethanol extracts of Jeju plants were tested for antimicrobial activities by disc diffusion and broth dilution methods. The results from the disc diffusion assays revealed that four medicinal plants, Mollugo pentaphylla, Angelica anomala, Matteuccia orientalis, and Orixa japonica inhibited the growth of both pathogens. Among these, A. anomala had strong inhibitory effects. Its MIC values were 15.6 microg/ml and 125 microg/ml against P. acnes and S. epidermidis, respectively. The cytotoxic effects of the four extracts were determined by colorimetric MTT assays using two animal cell lines: human dermal fibroblasts and HaCaT cells. Although the M. orientalis root extract had moderate cytotoxicity in HaCaT cells at 200 microg/ml, most extracts exhibited low cytotoxicity at 200 microg/ml in both cell lines. In addition, the extracts reduced the P. acnes-induced secretion of interleukin-8 and tumor necrosis factor-alpha (TNF-alpha) in THP-1 cells, an indication of their anti-inflammatory effects. Based on these results, we suggest that M. pentaphylla, A. anomala, M. orientalis, and O. japonica are attractive acne-mitigating candidates for topical application.

Immunological and structural properties of a pectic polymer from Glinus oppositifolius.

The aim of this paper was to further elucidate the structure and the immunomodulating properties of the pectic polymer GOA2, previously isolated from Glinus oppositifolius. Enzymatic treatment of GOA2 by endo-alpha-d-(1 --> 4)-polygalacturonase led to the isolation of three pectic subunits, GOA2-I, GOA2-II, and GOA2-III, in addition to oligogalacturonides. GOA2-I was shown to consist of 1,2-linked Rhap and 1,4-linked GalpA in an approximately 1:1 ratio, and NMR-analysis showed that the monomers were linked together in a strictly alternating manner. The galactose units in GOA2-I were found as terminal-, 1,3-, 1,6-, 1,4-, 1,3,4-, and 1,3,6-linked residues, while the arabinofuranosyl existed mainly as terminal- and 1,5-linked units. A rhamnogalacturonan-I type structure was suggested being the predominant part of GOA2-I. According to linkage analysis GOA2-II and GOA2-III contained glycosidic linkages characteristic for rhamnogalacturonan-II type structures. GOA2 was shown by sedimentation velocity in the analytical ultracentrifuge, to have a broad degree of polydispersity with a mode s(20,w) value of approximately 1.9 S, results reinforced by atomic force microscopy measurements. The polydispersity, as manifested by the proportion of material with s(20,w) > 3 S, decreased significantly with enzyme treatment. The abilities of GOA2, GOA2-I, GOA2-II, and GOA2-III to induce the proliferation of B cells, and to exhibit complement fixing activities were tested. In both test systems, GOA2-I showed significantly greater effects compared to its native pectin GOA2. GOA2-I was in addition shown to exhibit a more potent intestinal immune stimulating activity compared to GOA2. The ability of GOA2 to induce secretion of proinflammatory cytokines was examined. Marked upregulations in mRNA for IL-1beta from rat macrophages and IFN-gamma from NK cells were found.

Toxicological study on Glinus lotoides: a traditionally used taenicidal herb in Ethiopia.

Seeds of Glinus lotoides L. (Molluginaceae) are used traditionally in the treatment of tapeworm infestation in Ethiopia. Previous studies on its anthelmintic activities confirmed its traditional claims, but data on safety profile were lacking. To this effect, single and repeated dose oral toxicities of the methanolic extracts of seeds of Glinus lotoides were conducted in rats. Doses of 0, 1000 and 5000 mg/kg of crude extract of Glinus lotoides were employed in single dose toxicity studies, while doses of 0, 250, 500, and 1000 mg/kg were used in repeated toxicity studies. In the single dose toxicity test, oral administration of 5000 mg/kg of Glinus lotoides produced mortality in two females and one male on day 4. No significant differences in body and organ weights were observed between controls and treated surviving animals. Moreover, both gross and microscopic examinations of organs did not show detectable differences between controls and treated animals of both sexes. In repeated dose toxicity studies, no mortality was observed when varying doses of the extracts were administered per day for a period of 28 days. There were no significant differences in body weight, absolute and relative organ weights between controls and treated animals of both sexes. Hematological analysis showed no differences in most parameters examined. In the biochemistry parameter analysis, no significant change occurred. Pathologically, neither gross abnormalities nor histopathological changes were observed. These finding suggest that none of the organs appeared to be target and the data could provide satisfactory preclinical evidence of safety to launch clinical trial on standardized formulation of plant extracts.