intestinal tumor

GA-017 is a potent, selective inhibitor of LATS1 and LATS2 (large tumor suppressor kinase 1/2), exhibiting IC50 values of 4.10 and 3.92 nM, respectively. This compound simultaneously acts as an activator of cell proliferation by promoting YAP/TAZ activation and their nuclear translocation. Additionally, GA-017 enhances cell growth in 3D culture conditions and augments the ex vivo formation of mouse intestinal organoids [1].

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

3'- O- Acetylhamaudol, isolated from the roots of Angelica japonica, exhibits anti-tumor activity through dual actions, anti-angiogenesis and intestinal intraepithelial lymphocyte activation.

CRX 527 is a TLR4 ligand and serves as an adjuvant for peptide cancer vaccines, enhancing anti-tumor immune responses. CRX 527 also induces hematopoietic stem cell (HSC) differentiation, increasing the proportion and number of LSK cells, and promotes their differentiation into macrophages. This activation bolsters immune defense and protects intestinal epithelium from radiation damage.

1. 7-Ethylcamptothecin has the superior antitumor activity than CPT. (a). 7-Ethylcamptothecin has a stronger growth-inhibiting activity against tumor cells. (b). 7-Ethylcamptothecin remains in the intestinal tract for a longer time and in higher amounts when administered in vivo.

1. Crotonoside (Isoguanosine) has much more active than adenosine in reducing the blood pressure in rabbits and cats, in decreasing the tone of isolated intestinal strips of the rabbit, guinea pig and hamster and in stimulating the isolated uterus of guinea pigs and hamsters. 2. Crotonoside inhibits the growth of S-18 and Ehrlich solid tumor in mice at the optimal doses of 96 mg kg day x 12 and 48 mg kg day x 12, with 1-T C values of 65% and 6%, respectively.

GB-6, a short linear peptide that selectively binds to the gastrin releasing peptide receptor (GRPR), shows potential as a high-contrast imaging probe due to its tumor selectivity and specific accumulation. Overexpression of GRPR in pancreatic cancer enables GB-6, when labeled with near-infrared (NIR) fluorescent dyes or the radionuclide technetium-99m (99mTc), to serve as an effective agent for tumor visualization. Demonstrating excellent in vivo stability, GB-6 yields tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW1990 subcutaneous xenograft models. Its rapid tumor targeting capability and precise tumor boundary delineation signify GB-6's extensive potential for clinical applications [1].

TP4 (Nile tilapia piscidin) is an orally active, piscidin-like antimicrobial peptide that inhibits various gram-positive and gram-negative bacterial strains with a minimum inhibitory concentration (MIC) ranging from 0.03 to 10 μg mL. It demonstrates hemolytic activity and promotes immune response, antioxidant activity, and intestinal health in the presence of bacterial infections. Additionally, TP4 has an anti-tumor effect and induces necrosis in cancer cells by triggering mitochondrial dysfunction [1] [2] [3].

Phellamurin inhibits intestinal P-glycoprotein in a dose-dependent manner, there is a serious interaction occurred between Phellamurin with cyclosporin, to ensure the efficacy of cyclosporin, we suggest that the coadministration of Phellamurin or Phellode