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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).