AI Article Synopsis
- The dried root of Tetrastigma hemsleyanum is traditionally used in southern China for treating cancer and gastrointestinal issues, primarily due to its bioactive flavonoids.
- Research showed that THTF significantly inhibited growth and promoted apoptosis in colorectal cancer cells (HCT-116 and HT-29) in lab studies, and delayed tumor growth in live models without affecting overall health.
- The mechanism of THTF's antitumor effects appears to involve the inhibition of the PI3K/AKT/mTOR signaling pathway, with specific compounds in THTF strongly binding to key proteins in this pathway, suggesting its potential as a colorectal cancer treatment.
Article Abstract
The dried root of Tetrastigma hemsleyanum Diels et Gilg is used as a traditional Chinese medicine in southern China, as a folk remedy for carcinomas and gastrointestinal diseases. The total flavonoids of T. hemsleyanum (THTF) provide its main bioactive constituents. However, the mechanisms underlying its potential activity on colorectal cancer are still unknown. Here, we investigated the antitumor effect of THTF on colorectal cancer in vitro and in vivo. It was found that THTF inhibited HCT-116 and HT-29 cell growth, with an IC of 105.60 and 140.80 μg/mL, respectively. THTF suppressed clonogenicity and promoted apoptosis in HCT-116. In vivo, THTF (120 mg/kg) delayed tumor growth in HCT-116 xenografts without influencing on body weight, organ pathology and indexes, and blood routine level. Mechanistically, THTF inhibited the expression of PI3K, AKT, and mTOR at the protein level and transcriptional levels. Molecular docking indicated eight compounds in THTF (kaempferol 3-rutinoside, rutinum, isoquercitrin, L-epicatechin, quercetin, astragalin, kaempferol 3-sambubioside, and catechin) strongly bound with amino acid sites of PI3K and mTOR proteins, indicating a high affinity. The results suggest that THTF delayed colorectal tumor growth by inhibiting the PI3K/AKT/mTOR pathway and might be a potential candidate for colorectal cancer prevention.
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| http://dx.doi.org/10.1002/ptr.7561 | DOI Listing |
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