Tenacissoside G

Tenacissoside G is a C21 steroidal glycoside. Tenacissoside G inhibits Src and NF-κB, downregulates the activities of PTN and P-gp, induces DNA damage and apoptosis in cancer cells, inhibits their proliferation and migration, and reverses the resistance of ovarian cancer cells to Paclitaxel (HY-B0015). Tenacissoside G inhibits the expression of iNOS, TNF-α, IL-6, MMP-3, and MMP-13, reduces type II collagen degradation, and alleviates articular cartilage damage. Tenacissoside G can be used in studies related to ovarian cancer, colorectal cancer, and osteoarthritis^[1][2][3]. In Vitro:Tenacissoside G (5-160 μM; 24-48 h) shows no significant cytotoxicity against A2780 and A2780/T cells even at concentrations up to 160 μM, and reverses paclitaxel resistance in A2780/T cells in a concentration-dependent manner, with a maximum reversal fold of 6.96 at 20 μM for 24 h. However, it exerts no significant synergistic cytotoxicity on paclitaxel-sensitive A2780 cells^[1].
Tenacissoside G (5-20 μM; 24 h), either used alone or in combination with paclitaxel, downregulates the mRNA and protein expressions of Src, PTN and ABCB1 in A2780/T cells in a dose-dependent manner, and reverses the upregulation of the aforementioned genes and proteins induced by paclitaxel alone^[1].
Tenacissoside G (20 μM; 24 h) inhibits the efflux function of P-gp in A2780/T cells and significantly increases the intracellular accumulation of Rhodamine 123 (HY-D0816) and paclitaxel^[1].
Tenacissoside G (25-400 μM; 48 h) inhibits the proliferation of human colorectal cancer cell lines RKO, LoVo, HCT-8, HCT116 and HT-29 in a concentration-dependent manner, with its 48 h IC₅₀ values ranging from 55.3 μM (LoVo) to 103.1 μM (HT-29)^[3].
Tenacissoside G (50-100 μM; 48 h) reduces DNA replication and inhibits the proliferation of human colorectal cancer cell lines RKO and LoVo^[3].
Combined use of Tenacissoside G (5-20 μM; 24 h) and paclitaxel induces apoptosis of A2780/T cells in a dose-dependent manner^[1].
Tenacissoside G (50-100 μM; 48 h) induces low-level apoptosis in human colorectal cancer cells RKO and LoVo by activating the caspase cascade^[3].
Combination treatment with Tenacissoside G (5-20 μM; 24 h) and paclitaxel induces G2/M cell cycle arrest in A2780/T cells^[1].
Tenacissoside G (50-100 μM; 48 h) induces G0/G1 cell cycle arrest in human colorectal cancer cell lines RKO and LoVo by upregulating p53 and p21, and downregulating CDK2, CDK4, CDK6, cyclin D1 and cyclin E^[3].
Combined treatment with Tenacissoside G (5-20 μM; 24 h) and paclitaxel inhibits the migration of A2780/T cells in a dose-dependent manner^[1].
Tenacissoside G (2.5-160 μM; 24 h) exhibits only extremely low cytotoxicity to primary mouse chondrocytes, with cell viability maintained above 90%^[2].
Tenacissoside G (2.5-10 μM; 26 h) dose-dependently protects primary mouse chondrocytes against IL-1β-induced type II collagen degradation and inhibits MMP-13 protein expression^[2].
Tenacissoside G (2.5-10 μM; 26 h) dose-dependently inhibits IL-1β-induced activation of the NF-κB pathway in primary mouse chondrocytes by suppressing p65 phosphorylation and maintaining IκBα protein levels^[2].
Tenacissoside G (2.5-10 μM; 26 h) dose-dependently maintains the level of type Ⅱ collagen in primary mouse chondrocytes stimulated with IL-1β (detected by immunofluorescence)^[2].
Tenacissoside G (2.5-10 μM; 26 h) dose-dependently inhibits the expression of inflammation-related genes (iNOS, TNF-α, IL-6) and matrix degradation-related genes (MMP-3, MMP-13) in IL-1β-induced primary mouse chondrocytes^[2].
Tenacissoside G (50-100 μM; 24 h) induces DNA damage in human colorectal cancer cells RKO and LoVo, which is evidenced by an increased percentage of comet tail DNA and upregulated expression of γ-H2AX^[3]. In Vivo:Tenacissoside G (4-16 μg/kg; intra-articular; twice weekly; 8 weeks) alleviates osteoarthritis progression in DMM-induced mice in a dose-dependent manner, with 16 μg/kg providing the greatest reduction in articular cartilage damage, OARSI scores, and tibial subchondral bone loss, while increasing collagen II expression^[2].
Tenacissoside G (50 mg/kg; i.p.; every 2 days; 20 days) inhibits colorectal cancer xenograft growth by 28.4% and reduces tumor weight by 33.7% in BALB/c nude mice without causing significant systemic toxicity^[3].