Mechanistic and therapeutic perspectives of baicalin and baicalein on pulmonary hypertension: A comprehensive review

2023

Front. Pharmacol.

The flavonoids baicalin and baicalein were discovered in the root of Scutellaria baicalensis Georgi and are primarily used in traditional Chinese medicine, herbal supplements and healthcare. Recently, accumulated investigations have demonstrated the therapeutic benefits of baicalin in treating various lung diseases due to its antioxidant, anti-inflammatory, immunomodulatory, antiapoptotic, anticancer, and antiviral effects. In this review, the PubMed database and ClinicalTrials website were searched with the search string “baicalin” and “lung” for articles published between September 1970 and March 2023. We summarized the therapeutic role that baicalin plays in a variety of lung diseases, such as chronic obstructive pulmonary disease, asthma, pulmonary fibrosis, pulmonary hypertension, pulmonary infections, acute lung injury/acute respiratory distress syndrome, and lung cancer. We also discussed the underlying mechanisms of baicalin targeting in these lung diseases.

Section: Methodsmentioning

confidence: 99%

Pharmacological effects of baicalin in lung diseases

2023

Front. Pharmacol.

“…Studies have shown that there is an interconversion between baicalin and baicalein during the absorption process of baicalin [22][23][24]. In particular, after drug administration in animals, baicalin could be hydrolyzed to baicalein by β-glucuronidase derived from intestinal bacteria, and baicalein could be recovered to baicalin by uridine 5 -diphosphate (UDP) glucuronide transferase (UGT) circulating in vivo [25]. This mutual conversion maximizes the full pharmacodynamic functions of baicalin [25].…”

Section: Bioavailability Of Baicalinmentioning

confidence: 99%

“…In particular, after drug administration in animals, baicalin could be hydrolyzed to baicalein by β-glucuronidase derived from intestinal bacteria, and baicalein could be recovered to baicalin by uridine 5 -diphosphate (UDP) glucuronide transferase (UGT) circulating in vivo [25]. This mutual conversion maximizes the full pharmacodynamic functions of baicalin [25]. Due to the better absorption of baicalein compared to baicalin, the conversion of baicalin to baicalein is a key step for the absorption of baicalin in the intestine.…”

Section: Bioavailability Of Baicalinmentioning

confidence: 99%

The Pharmacological Efficacy of Baicalin in Inflammatory Diseases

Wen

Zhao

et al. 2023

IJMS

Baicalin is one of the most abundant flavonoids found in the dried roots of Scutellaria baicalensis Georgi (SBG) belonging to the genus Scutellaria. While baicalin is demonstrated to have anti-inflammatory, antiviral, antitumor, antibacterial, anticonvulsant, antioxidant, hepatoprotective, and neuroprotective effects, its low hydrophilicity and lipophilicity limit the bioavailability and pharmacological functions. Therefore, an in-depth study of baicalin’s bioavailability and pharmacokinetics contributes to laying the theoretical foundation for applied research in disease treatment. In this view, the physicochemical properties and anti-inflammatory activity of baicalin are summarized in terms of bioavailability, drug interaction, and inflammatory conditions.

“…Baicalin and baicalein are flavonoids with a wide range of pharmacological activities isolated from the TCM Scutellaria baicalensis Georgi. Studies have shown that baicalin and baicalein can play a role in the treatment of PH in many aspects, such as anti-inflammatory, inhibition of PASMC proliferation and EndMT, reduction of oxidative stress, and stabilization of extracellular matrix [ 66 ]. The improvement of baicalin on PVR may be achieved through the following pathways alone or together, including the regulating tumor necrosis factor-α (TNF-α)/BMPR2 signaling pathway, downregulating p38 mitogen-activated protein kinase (MAPK)/matrix metalloproteinase-9 (MMP-9) signaling pathway, promoting Akt/eNOS, and inhibiting ERK and the NF-κB signaling pathway [ 67 , 68 , 69 ].…”

Section: Natural Products For the Treatment Of Phmentioning

confidence: 99%

Natural Products for the Treatment of Pulmonary Hypertension: Mechanism, Progress, and Future Opportunities

Zeng

Cui

et al. 2023

CIMB

Self Cite

Pulmonary hypertension (PH) is a lethal disease due to the remodeling of pulmonary vessels. Its pathophysiological characteristics include increased pulmonary arterial pressure and pulmonary vascular resistance, leading to right heart failure and death. The pathological mechanism of PH is complex and includes inflammation, oxidative stress, vasoconstriction/diastolic imbalance, genetic factors, and ion channel abnormalities. Currently, many clinical drugs for the treatment of PH mainly play their role by relaxing pulmonary arteries, and the treatment effect is limited. Recent studies have shown that various natural products have unique therapeutic advantages for PH with complex pathological mechanisms owing to their multitarget characteristics and low toxicity. This review summarizes the main natural products and their pharmacological mechanisms in PH treatment to provide a useful reference for future research and development of new anti-PH drugs and their mechanisms.