Baicalein from Scutellaria baicalensis as Natural Therapeutic Agent for Glioblastoma

Abstract

Glioblastoma multiforme (GBM), also known as grade IV astrocytoma, remains one of the most challenging malignancies in neuro-oncology, characterized by an exceptionally poor prognosis and high recurrence rate. The multifactorial nature of glioblastoma progression—including its resistance to apoptosis, diffuse infiltration, and angiogenesis—makes it one of the most treatment-resistant tumors. Standard treatment protocols involving surgical resection followed by radiotherapy and temozolomide chemotherapy have only marginally improved survival outcomes. There is, therefore, a growing demand for novel therapeutic agents that are multi-targeted, effective across glioblastoma molecular subtypes, and capable of penetrating the blood-brain barrier (BBB).

In this context, baicalein, a naturally occurring flavonoid derived from Scutellaria baicalensis (commonly known as Chinese skullcap), has emerged as a promising candidate. With a rich ethnopharmacological history in traditional Chinese medicine, S. baicalensis has been used for centuries to treat inflammatory diseases, viral infections, and cancers. Modern scientific studies have revealed that baicalein exerts diverse pharmacological effects, including anti-inflammatory, antioxidative, neuroprotective, and anticancer properties. In glioblastoma models, baicalein demonstrates a capacity to suppress tumor proliferation, promote apoptosis, inhibit angiogenesis, and impair invasive behavior of glioma cells. The goal of this comprehensive review is to synthesize the current knowledge surrounding baicalein’s pharmacological actions in the context of glioblastoma. We explore its phytochemical composition, its molecular targets within glioblastoma signaling networks, its pharmacokinetic limitations, and the use of advanced drug delivery systems to enhance its therapeutic efficacy. In addition, we examine recent preclinical data supporting its use, the potential for combination with existing chemotherapeutic agents, and the status of clinical development.

We also address the challenges facing baicalein’s clinical translation, including solubility issues, bioavailability, and the need for regulatory oversight. Comparative analysis with other flavonoids (e.g., wogonin, luteolin, quercetin) is included to place baicalein’s unique properties in context. Ultimately, this review aims to provide a platform for further investigation and development of baicalein as a viable adjunct or primary therapeutic option for glioblastoma patients.