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| Baicalein is a flavone, a type of flavonoid, originally isolated from the roots of Scutellaria baicalensis and Scutellaria lateriflora. It is also a constituent of Oroxylum indicum and thyme. Baicalein, a flavonoid found in several medicinal plants (notably Scutellaria baicalensis), has been investigated for its anticancer properties. Its activities involve modulation of multiple cellular pathways, including those that regulate cell proliferation, apoptosis, metastasis, and oxidative stress. Here are some of the key pathways and mechanisms implicated in its anticancer effects: -Apoptosis and Cell Cycle Regulation -Reactive Oxygen Species ROS↑ Generation and Oxidative Stress - ROS↑ related: MMP↓(ΔΨm), ER Stress↑, Ca+2↑, Cyt‑c↑, Caspase-3↑, Caspase-9↑, DNA damage↑, -Baicalein’s effects on ROS are context-dependent. In some cancer cells, it promotes ROS production to a degree that overwhelms the antioxidant defenses. Elevated ROS levels can damage cellular components and promote apoptosis, essentially tipping the balance toward cell death. -Conversely, in normal cells, baicalein may exhibit antioxidant properties and reduce ROS↓ under conditions of oxidative stress, highlighting its dual role. - Lowers AntiOxidant defense in Cancer Cells: NRF2↓, GSH↓, HO-1↓, - Raises AntiOxidant defense in Normal Cells: NRF2↑, SOD↑, GSH↑, Catalase↑, HO-1↑, -MAPK, ERK Pathway: -PI3K/Akt Pathway: Inhibition of the PI3K, Akt pathway by baicalein. -NF-κB Pathway: Baicalein can inhibit -Inhibition of Metastasis and Invasion: Baicalein can downregulate MMPs, MMP2, MMP9 -Angiogenesis Suppression: VEGF -Baicalein is a well-known inhibitor of 12-lipoxygenase -inhibitor of Glycolysis↓ and HIF-1α↓, PKM2↓, cMyc↓, PDK1↓, GLUT1↓, LDHA↓, HK2↓ - promoting PTEN -chemo-sensitization, chemoProtective, RadioSensitizer, RadioProtective, neuroprotective, Cognitive, Renoprotection, Hepatoprotective, cardioProtective, - Selectivity: Cancer Cells vs Normal Cells -low bioavailability but liposomal highly improves bioavailability In summary, baicalein affects cancer cells by modulating multiple pathways—promoting apoptosis, causing cell cycle arrest, generating or modulating ROS levels, inhibiting survival and proliferative signaling (such as MAPK, PI3K/Akt, and NF-κB pathways), and reducing angiogenesis and metastasis. Many animal studies, doses have been reported in the range of approximately 10 to 200 mg/kg body weight. For example, some studies exploring anticancer or anti-inflammatory effects in rodent models have used doses around 50–100 mg/kg. However, these doses do not directly translate to human dosages. Some human studies or formulations (where they are used as nutraceuticals or supplements) may suggest dosing in the range of a few hundred milligrams per day of the extract, but it is often not standardized to a specific amount of baicalein or baicalin. -mix with oil? -ic50 cancer cells 10-30uM, normal cells 50-100uM -Animal studies, 10 to 100 mg/kg. -Reported to induce apoptosis, cause cell cycle arrest, inhibit angiogenesis, and modulate various signaling pathways (e.g., STAT3, NF-κB, MAPK). |
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| The selectivity of cancer products (such as chemotherapeutic agents, targeted therapies, immunotherapies, and novel cancer drugs) refers to their ability to affect cancer cells preferentially over normal, healthy cells. High selectivity is important because it can lead to better patient outcomes by reducing side effects and minimizing damage to normal tissues. Achieving high selectivity in cancer treatment is crucial for improving patient outcomes. It relies on pinpointing molecular differences between cancerous and normal cells, designing drugs or delivery systems that exploit these differences, and overcoming intrinsic challenges like tumor heterogeneity and resistance Factors that affect selectivity: 1. Ability of Cancer cells to preferentially absorb a product/drug -EPR-enhanced permeability and retention of cancer cells -nanoparticle formations/carriers may target cancer cells over normal cells -Liposomal formations. Also negatively/positively charged affects absorbtion 2. Product/drug effect may be different for normal vs cancer cells - hypoxia - transition metal content levels (iron/copper) change probability of fenton reaction. - pH levels - antiOxidant levels and defense levels 3. Bio-availability |
| 2615- | Ba, | The Multifaceted Role of Baicalein in Cancer Management through Modulation of Cell Signalling Pathways |
| - | Review, | Var, | NA |
| 1523- | Ba, | Baicalein induces human osteosarcoma cell line MG-63 apoptosis via ROS-induced BNIP3 expression |
| - | in-vitro, | OS, | MG63 | - | in-vitro, | Nor, | hFOB1.19 |
| 1533- | Ba, | Baicalein, as a Prooxidant, Triggers Mitochondrial Apoptosis in MCF-7 Human Breast Cancer Cells Through Mobilization of Intracellular Copper and Reactive Oxygen Species Generation |
| - | in-vitro, | BrCC, | MCF-7 | - | in-vitro, | Nor, | MCF10 |
| 2479- | Ba, | Baicalein Overcomes Tumor Necrosis Factor–Related Apoptosis-Inducing Ligand Resistance via Two Different Cell-Specific Pathways in Cancer Cells but not in Normal Cells |
| - | in-vitro, | HCC, | SW480 | - | in-vitro, | Pca, | PC3 |
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