Inflammatory bowel disease (IBD) is a group of chronic conditions characterized by inflammation in                    the gastrointestinal tract, which can be categorized into ulcerative colitis (UC) and Crohn's disease (CD).

 Patients with UC often suffer from diarrhea, mucus or blood in the stool. Acute UC patients usually associate with  tenesmus which leads to difficultly in defecating. Patients with CD often suffer from repeated episodes of lower right  abdominal pain and diarrhea. These two diseases are both caused by intestinal inflammation and may increase cancer  risks.

 IBD patients do not respond well to current treatments, such as immunosuppressive agents, steroids, or common  anti-inflammatory drugs. Therefore, there is a great unmet medical need. It is estimated that about 1.4 million people  in the United States have IBD, and approximately 30,000 people are newly diagnosed every year, which in all account  for 700,000 physician visits, 100,000 hospitalizations, and disability in 119,000 patients every year.

 The global revenue of IBD medications was predicted to reach about $9.6 billion in 2017 by Visiongain.

1.   Inhibition of lipopolysaccharide (LPS)-induced serum TNF-α production in mice

     Summary: It is proved that BLI-1006 could act as a TNF-α inhibitor in the LPS-induced mice model.

Figure 1. In vivo TNF-α and IL-6 inhibition by BLI-1006. Mice were treated with LPS alone or with various concentration

of BLI-1006 for 4 h. Control was obtained in the absence of LPS and the test article. The secretion of TNF-α and IL-6 was

determined by ELISA reader. The values are means of triplicate cultures ± S.D.. The results shown represent two experiments.

2. Suppression of cytokines in 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced inflammation in animal model

    Summary: Potent inhibitory activity of BLI-1006 against various cytokines was demonstrated through quantitative analyses.

    The inhibitory effect of BLI-1006 was greater than 5-ASA, an anti-inflammatory drug for treating IBD.

Figure 2. Cytokine profiles with BLI-1006 in TNBS-induced inflammation Model.A: Blank ; B: control; C:BLI-1006;

D: 5-ASA (5-aminosalicylic acid). *P<0.05, vs. normal control; unpaired Student’s t-test.

3.  Effects of dinitrobenzene sulfonic acid (DNBS)-induced inflammation in animal model

A. Suppression of colon weight increase

    Summary : BLI-1006 significantly suppressed increase of colon weight caused by DNBS-induced colitis,

    suggesting BLI-1006 as a potential drug for treating IBD.

Figure 3. Test substances and vehicle were administered once daily (qd) by oral gavage (PO) for 7 consecutive days

and DNBS was instilled intracolonically on day 2. Animals were sacrificed on Day 8.

The colon-to-body weight ratio was calculated (g/100 g body wt). N=6, †P<0.05, vs. normal control; unpaired

Student’s t-test.*P<0.05, vs. vehicle control; one-way ANOVA followed by Dunnett's test.

B.  Improvement of colon morphology

Summary: Inflammatory colons were observed in mice with DNBS induction, but the characteristic redness and swelling

were relieved in the mice with BLI-1006 treatment.