Unigen Pharmaceuticals Inc.

Lacey, WA, United States

Unigen Pharmaceuticals Inc.

Lacey, WA, United States
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Tseng-Crank J.,Unigen Pharmaceuticals Inc. | Sung S.,Unigen Inc. | Jia Q.,Unigen Pharmaceuticals Inc. | Zhao Y.,Unigen Pharmaceuticals Inc. | And 3 more authors.
Journal of Dietary Supplements | Year: 2010

A standardized, combined flavonoid extracts of Scutellaria baicalensis and Acacia catechu, UP446, demonstrates favorable anti-inflammatory properties. In this study, DNA microarray, quantitative polymerase chain reaction (QPCR), and enzyme-linked immunosorbent assay (ELISA) were used to study the effect of UP446 on the lipopolysaccharide (LPS)-induced pro-inflammatory gene regulation of both animal and human immortalized cell lines and also primary human cells. One consistent result from microarray was that the gene expression levels stimulated or suppressed by LPS were returned to normal levels by the UP446 co-treatment. This normalization effect from UP446 was also shown for pro-inflammatory genes cyclooxygenase (COX)-2, tissue necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6 using QPCR, and TNF-α using ELISA. The controlling transcriptional factor of these genes, NFκB, was also down-regulated by UP446 in the LPS-induced cell models. Microarray analysis for numerous genes, including cytokines, chemokines, receptors, transcriptional factors, caspase, growth factors, and phosphatases, suggests not only a genomic anti-inflammatory activity for UP446 but also signaling pathways of cell proliferation, cell death, and lipid metabolism demonstrated on different types of cells. © 2010 Informa Healthcare USA, Inc. All rights reserved.


Yimam M.,Unigen Pharmaceuticals Inc. | Zhao Y.,Unigen Pharmaceuticals Inc. | Ma W.,Unigen Pharmaceuticals Inc. | Jia Q.,Unigen Pharmaceuticals Inc. | And 2 more authors.
Food and Chemical Toxicology | Year: 2010

A standardized plant composition-UP446 with primarily baicalin from the roots of Scutellaria baicalensis and (+)-catechin from the heartwoods of Acacia catechu has been used in both joint supplements and a prescription medical food. The in vitro and in vivo safety evaluations of UP446 have been reported previously. A supplemental 90-day oral toxicity study was conducted in Hsd:SD® rats to determine the potential of UP446 to produce toxicity. Four groups (10 males and 10 females per group) of dose levels of 250, 500, and 1000. mg/kg/day of the test article, as well as a control (0.5% carboxymethylcellulose) were tested. There were no test article related mortalities or ophthalmological, neurological (Functional Observational Battery and motor activity), body weight, feed consumption, clinical observation, organ weight changes, gross finding, clinical or histopathological alterations. Normal sperm count and comparable estrus staging were observed. A dose of 1000. mg/kg/day was identified as the NOAEL (no-observed-adverse-effect-level) in this study. © 2010 Elsevier Ltd.


Zhang S.-Q.,National Institutes for Food and Drug Control | Zhu L.,National Institutes for Food and Drug Control | Wen N.,National Institutes for Food and Drug Control | Yu M.,National Institutes for Food and Drug Control | And 4 more authors.
Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences | Year: 2011

UP302 is a novel natural antioxidant isolated from Dianella ensifolia (Liliaceae). In the investigation, a specific and sensitive ultra-high performance liquid chromatography-tandem mass spectrometry for quantitative determination of UP302 in rat plasma was developed and validated. UP302 and the internal standard daidzein were extracted from 100. μL aliquots of rat plasma using methanol. Detection of UP302 and IS was done by tandem mass spectrometry, operating in negative ion and selected reaction monitoring acquisition mode. The precursor-product ion transitions monitored for UP302 and daidzein were m/. z 301.1. → 135.2 and 252.9. → 132.0, respectively. The linearity of the method was observed within the concentration range of 5-2000. ng/mL. Intra- and inter-day assay variations were less than 15%, and the accuracy values were between 99.2% and 107.3%. The method was successfully applied to stability investigation of UP302 incubated in rat plasma at 37. °C and measurement of UP302 in plasma after intravenous administration of UP302 to rats at a single dose of 5. mg/kg. Incubation stability revealed that within first one hour, UP302 was rapidly declined approximately 35% and remained stable after 4. h. Pharmacokinetic values of half-life, volume of distribution, systemic clearance and mean residence time were 0.87. ± 0.58. h, 6.90. ± 3.35. L/kg, 5.89. ± 1.21. L/h. kg and 0.34. ± 0.13. h, respectively. © 2011 Elsevier B.V.


Nesterov A.,Unigen Pharmaceuticals Inc. | Mei Hong,Unigen Pharmaceuticals Inc. | Hertel C.,Unigen Pharmaceuticals Inc. | Ping Jiao,Unigen Pharmaceuticals Inc. | And 2 more authors.
Journal of Biomolecular Screening | Year: 2010

This study describes the screening of a plant extract library for inhibitors of signal transduction pathways mediated by the cholecystokinin receptor, CCK1. CCK1 receptors are coupled to Gαq/11-proteins, localized mainly in the gastrointestinal tract, and implicated in the regulation of various digestive functions. A primary screen was performed using a cell-based assay that used the β-lactamase gene reporter controlled by the transcriptional activator NFAT. The assay was validated with the CCK1 receptor antagonist, lorglumide, and automated by the use of a liquid-handling robot MultiProbe II. Off-target hits were triaged by counterscreening against gene reporter cells activated by a combination of thapsigargin and phorbol ester. Purification of active compounds was guided by the β-lactamase gene reporter and Ca2+ mobilization assays. Pure compounds were characterized by Ca2+ mobilization, radioligand binding, inositol-1 phosphate formation, and Eu-GTP binding assays. The selectivity of inhibition was tested against a panel of Gαq/11, Gαs, and Gαi/0-coupled receptors. These studies led to the identification of a novel Gαq/11-selective inhibitor. © 2010 Society for Biomolecular Sciences.


Yimam M.,Unigen Pharmaceuticals Inc. | Brownell L.,Unigen Pharmaceuticals Inc. | Hodges M.,Unigen Pharmaceuticals Inc. | Jia Q.,Unigen Pharmaceuticals Inc.
Journal of Dietary Supplements | Year: 2012

Anti-inflammatory properties of both baicalin and catechins have been widely reported. However, the reports of analgesic effects of baicalin and catechins are limited. Three commonly used pain-related animal models were employed to evaluate the analgesic activity of UP446, a standardized bioflavonoid composition of baicalin and catechins. Carrageenan-induced paw edema, formalin test, and abdominal constriction assays were used to evaluate antinociceptive activity of 150 mg/kg or 100 mg/kg oral doses of UP446. Ibuprofen was used as a reference compound in each test. Pretreatment of carrageenan-induced hyperalgesic animals with UP446 at 150 mg/kg oral dosage reduced the hypersensitivity of pain by 39.5. Similarly, a single dose of UP446, given orally at 100 mg/kg, exhibited 58 and 71.9 inhibition in pain sensitivity compared to vehicle-treated control in writhing and formalin tests, respectively. These findings suggest that the standardized anti-inflammatory bioflavonoid composition, UP446, could also be employed to inhibit nociception. © 2012 Informa Healthcare USA, Inc.


Pillai L.,Primus Pharmaceuticals Inc. | Levy R.M.,Primus Pharmaceuticals Inc. | Yimam M.,Unigen Pharmaceuticals Inc. | Zhao Y.,Unigen Pharmaceuticals Inc. | And 2 more authors.
Advances in Therapy | Year: 2010

Introduction: Flavocoxid, a botanical, antiinflammatory agent, nonspecifically inhibits the peroxidase activity of cyclooxygenase (COX-1 and COX-2) enzymes and 5-lipooxygenase (5-LOX). Due to the concomitant use of aspirin or warfarin in many osteoarthritis (OA) patients with increased cardiovascular risk, we felt it necessary to assess the anticoagulation properties of flavocoxid. Methods: Three different studies were used: 1) a mouse model to assess effects on bleeding times when combined with aspirin; 2) the effect on platelet function as evaluated by platelet aggregation and bleed times in healthy human subjects; and 3) the effect on international normalized ratio in previously warfarinized patients with OA. Results: Flavocoxid at a human equivalent dose (HED) of 569 mg (within the standard humandosing range of 500 mg) produced no significant increases in bleeding time in mice. There was also no inhibition or synergistic increase in bleed times when flavocoxid was combined with aspirin (370 mg HED). Flavocoxid did not significantly inhibit thromboxane production or platelet aggregation, and did not increase bleeding times in healthy volunteers. Finally, flavocoxid did not inhibit or potentiate the anticoagulant effect of warfarin. Conclusion: These results suggest that flavocoxid does not affect the primary or extrinsic pathways of secondary hemostasis and, by not inhibiting the anticoagulation effects of aspirin, may have utility in cardiovascular patients with OA. © Springer Healthcare 2010.


Patent
Unigen Pharmaceuticals Inc. | Date: 2010-06-11

The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compoundsdiarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.


Patent
Unigen Pharmaceuticals Inc. | Date: 2010-03-10

The present invention describes the identification and purification of 7-hydroxychromes that exhibit potent antioxidant activity. In one embodiment the present invention includes a method for providing an antioxidant to a host in need thereof, comprising administering an effective amount of a 7-hydroxychrome or a mixture of 7-hydroxychromones. The present invention includes methods that are effective in inhibiting free radical and oxidation caused damage through the simultaneous suppression of free radical generation and the suppression of the production of reactive oxygen species (ROS). The present invention also includes methods for preventing and treating ROS mediated diseases and conditions and diseases and conditions associated with other oxidative processes. The method for preventing and treating ROS mediated diseases and conditions and diseases and conditions associated with other oxidative processes is comprised of administering to a host in need thereof an effective amount of a composition comprised of a 7-hydroxychrome or a mixture of 7-hydroxychromones and a pharmaceutically acceptable carrier. Included in this invention is an improved method to isolate and purify 7-hydroxychromones from plant sources.


PubMed | Unigen Pharmaceuticals Inc.
Type: Journal Article | Journal: Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association | Year: 2010

A standardized plant composition--UP446, with primarily baicalin from the roots of Scutellaria baicalensis and (+)-catechin from the heartwoods of Acacia catechu--has been used in both joint supplements and a prescription medical food. The in vitro and in vivo safety evaluations of UP446 have been reported previously. A supplemental 90-day oral toxicity study was conducted in Hsd:SD(R) rats to determine the potential of UP446 to produce toxicity. Four groups (10 males and 10 females per group) of dose levels of 250, 500, and 1000 mg/kg/day of the test article, as well as a control (0.5% carboxymethylcellulose) were tested. There were no test article related mortalities or ophthalmological, neurological (Functional Observational Battery and motor activity), body weight, feed consumption, clinical observation, organ weight changes, gross finding, clinical or histopathological alterations. Normal sperm count and comparable estrus staging were observed. A dose of 1000 mg/kg/day was identified as the NOAEL (no-observed-adverse-effect-level) in this study.


A standardized, combined flavonoid extracts of Scutellaria baicalensis and Acacia catechu, UP446, demonstrates favorable anti-inflammatory properties. In this study, DNA microarray, quantitative polymerase chain reaction (QPCR), and enzyme-linked immunosorbent assay (ELISA) were used to study the effect of UP446 on the lipopolysaccharide (LPS)-induced pro-inflammatory gene regulation of both animal and human immortalized cell lines and also primary human cells. One consistent result from microarray was that the gene expression levels stimulated or suppressed by LPS were returned to normal levels by the UP446 co-treatment. This normalization effect from UP446 was also shown for pro-inflammatory genes cyclooxygenase (COX)-2, tissue necrosis factor (TNF)-, interleukin (IL)-1, IL-6 using QPCR, and TNF- using ELISA. The controlling transcriptional factor of these genes, NFB, was also down-regulated by UP446 in the LPS-induced cell models. Microarray analysis for numerous genes, including cytokines, chemokines, receptors, transcriptional factors, caspase, growth factors, and phosphatases, suggests not only a genomic anti-inflammatory activity for UP446 but also signaling pathways of cell proliferation, cell death, and lipid metabolism demonstrated on different types of cells.

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