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| Baicalin is a flavone glycoside, it is a flavonoid. It is the glucuronide of baicalein.
Baicalin is a flavonoid glycoside derived from plants in the genus Scutellaria. It has anxiolytic, anti-cancer and anti-viral properties, and is used in traditional Chinese medicine. Baicalein and baicalin are chemically related, with baicalin being essentially a conjugated (sugar-attached) form of baicalein. This conjugation can modify their biological functions and impacts, making them distinct in certain aspects even though they share several pharmacological properties. baicalin is often hydrolyzed by gut β-glucuronidase to baicalein (aglycone) and then extensively converted to phase-II conjugates (glucuronides/sulfates), which constrains systemic “free” levels after oral dosing. In cancer models, baicalin/baicalein are reported to modulate NF-κB, PI3K/AKT/mTOR, MAPK, and related programs, with downstream effects on cell-cycle arrest, apoptosis, invasion/EMT, and angiogenesis (model-dependent). Baicalein appears to be antioxidant in normal cells (low Cu). In vitro, baicalein can participate in copper-dependent redox cycling under high Cu conditions, leading to ROS generation. Whether this mechanism contributes meaningfully in vivo remains model-dependent. (higher Cu levels) (May applies to other plant polyphenols as well: Ex apigenin, luteolin, EGCG, and resveratrol). Pathways: Apoptosis Pathways (Intrinsic/Mitochondrial): NF-κB Inhibition : PI3K/Akt/mTOR Signaling Pathway downregulate : MAPK/ERK and JNK Signaling Pathways: STAT3 Signaling: (inhibit) Wnt/β-Catenin Signaling Pathway: (suppress) Other Pathways and Effects: • Cell Cycle Arrests (commonly G0/G1 or G2/M) • Anti-angiogenic Effects: By inhibiting VEGF • Modulation of Oxidative Stress: Balancing reactive oxygen species (ROS) levels in cancer cells can also contribute to its antitumor effects. • In normal cells or under conditions of oxidative stress, baicalin has been shown to act as an antioxidant. • In cancer cells, baicalin may increase ROS levels, triggering apoptosis. Lower doses of baicalin might favor antioxidant responses, whereas higher concentrations could lead to ROS accumulation in cancer cells. Redox effects are concentration- and context-dependent; antioxidant behavior predominates in non-tumor oxidative stress models, whereas ROS increases have been reported in some tumor systems at higher concentrations. • If copper levels are elevated in a cancer cell, the additional ROS generated via copper-mediated reactions may synergize with baicalin’s pro-oxidant effects (if observed at higher doses) to exceed the threshold for cancer cell survival. • Conversely, in normal cells with tightly regulated copper levels, baicalin’s antioxidant properties may help in quenching excess ROS or maintaining redox balance. -IC50 in cancer cell lines: Approximately 50–200 µM (with some variability depending on the cell type). • IC50 in normal cell lines: Generally higher, often exceeding 200 µM, though values will vary with experimental conditions. Many in-vitro IC50 values exceed achievable systemic concentrations after oral dosing without advanced formulation. Low oral bioavailability: classic rat PK reports very low absolute BA bioavailability and evidence of enterohepatic cycling
Time-Scale Flag (TSF): P / R / G
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| Glutathione (GSH) is a thiol antioxidant that scavenges reactive oxygen species (ROS), resulting in the formation of oxidized glutathione (GSSG). Decreased amounts of GSH and a decreased GSH/GSSG ratio in tissues are biomarkers of oxidative stress. Glutathione is a powerful antioxidant found in every cell of the body, composed of three amino acids: cysteine, glutamine, and glycine. It plays a crucial role in protecting cells from oxidative stress, detoxifying harmful substances, and supporting the immune system. cancer cells can have elevated levels of glutathione, which may help them survive in the oxidative environment created by the immune response and chemotherapy. This can make cancer cells more resistant to treatment. While glutathione can be obtained from certain foods (like fruits, vegetables, and meats), its absorption from supplements is debated. Some people take N-acetylcysteine (NAC) or other precursors to boost glutathione levels, but the effects on cancer prevention or treatment are still being studied. Depleting glutathione (GSH) to raise reactive oxygen species (ROS) is a strategy that has been explored in cancer research and therapy. Many cancer cells have altered redox states and may rely on GSH to survive. Increasing ROS levels can induce stress in these cells, potentially leading to cell death. Certain drugs and compounds can deplete GSH levels. For example, agents like buthionine sulfoximine (BSO) inhibit the synthesis of GSH, leading to its depletion. Cancer cells tend to exhibit higher levels of intracellular GSH, possibly as an adaptive response to a higher metabolism and thus higher steady-state levels of reactive oxygen species (ROS). "...intracellular glutathione (GSH) exhibits an astounding antioxidant activity in scavenging reactive oxygen species (ROS)..." "Cancer cells have a high level of GSH compared to normal cells." "...cancer cells are affluent with high antioxidant levels, especially with GSH, whose appearance at an elevated concentration of ∼10 mM (10 times less in normal cells) detoxifies the cancer cells." "Therefore, GSH depletion can be assumed to be the key strategy to amplify the oxidative stress in cancer cells, enhancing the destruction of cancer cells by fruitful cancer therapy." The loss of GSH is broadly known to be directly related to the apoptosis progression. |
| 2605- | Ba, | BA, | Potential therapeutic effects of baicalin and baicalein |
| - | Review, | Var, | NA | - | Review, | Stroke, | NA | - | Review, | IBD, | NA | - | Review, | Arthritis, | NA | - | Review, | AD, | NA | - | Review, | Park, | NA |
Query results interpretion may depend on "conditions" listed in the research papers. Such Conditions may include : -low or high Dose -format for product, such as nano of lipid formations -different cell line effects -synergies with other products -if effect was for normal or cancerous cells
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