BAICALEIN

Derived from the root of Scutellaria baicalensis or chinese skullcap. Baicalin is processed baicalein resulting in higher absorption and bioavailability.

Baicalein however, has only sparse clinical trials. At least one reports kidney protective actions which would confirm actions from traditional chinese herbal medicine (see Highlights). This is really where there may be relevance to improved outcomes, with its potential to protect kidney function both as it relates to cancer activity and chemotherapy or other treatments. It also has shown evidence of lowering blood glucose levels and inflammatory markers in coronary heart disease and arthritis research.

Some of the few trials showing anti-inflammatory results in vascular health and arthritis are with branded commercial products combined with other active compounds (see References). These smaller trials show strongly anti-inflammatory actions that need validation i broader clinical research.

TYPICAL ABSORPTION LEVELS

10 – 25%

EXAMPLES OF IMPROVED OUTCOMES

PRE-DIAGNOSIS OR PREVENTION

Highlighted Studies

Importantly, we observed better improvements in patients treated by baicalin than those on placebo treatment, demonstrating the beneficial effect of baicalin on further improving lipid profile [alingside first line drugs]. Moreover, the extent of improvements with regard to CT-1 and hs-CRP, two important risk factors of CAD [coronary artery disease], was also significantly better in the baicalin group than that in the placebo group, further indicating the efficacy of baicalin in alleviating C...

This indicates that baicalin can reduce the level of proteinuria and distinctly improve renal function of the diabetic patients. After receiving baicalin treatment, the SOD and GSH-px levels of patients were obviously increased and the AR activity, NF-κB and VEGF content were decreased significantly, indicating that baicalin could reduce renal vascular permeability, improve renal function of patients with diabetic nephropathy and postpone the progress of diabetic nephropathy through anti-oxi...

In this study the dietary supplement Lenidase^®, consisting of escin, bromelain and baicalin, improved both VCSS and symptoms in “user” patients affected by CVI compared to “non-users” who underwent compression therapy only. Since the anti-inflammatory effects of baicalin were well-known and widely described, we hypothesized that VCSS improvement could be mainly ascribed to this natural compound. In fact, baicalin has been proven to decrease the serum levels of pro-inflamma...

Both flavocoxid and naproxen showed significant reduction in the signs and symptoms of OA [arthritis]. There were no statistically detectable differences between the flavocoxid and naproxen groups with respect to any of the outcome variables. Similarly, there were no statistically detectable differences between the groups with respect to any <a class="topic-link" title="Learn more about adverse event from ScienceDirect's AI-generated Topic Pages" href="https://www.sciencedirect.com/topics/pha...

TABLE OF REFERENCES

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https://lipidworld.biomedcentral.com/articles/10.1186/s12944-018-0797-2	3	Baicalin reduces blood lipids and inflammation in patients with both CAD and RA, supporting its further clinical application..After 12 week treatment, levels of triglycerides, total cholesterol, LDL-cholesterol and apolipoproteins, as well as CT-1 and hs-CRP, were all significantly improved in the baicalin group compared to the placebo group (1.12 ± 0.36 vs 1.87 ± 0.46 mmol/L, 2.87 ± 1.23 vs 3.22 ± 1.07 mmol/L, 1.38 ± 0.41 vs 1.16 ± 0.32 mmol/L, 1.31 ± 0.41 vs 1.23 ± 0.29 g/L, 42.9 ± 13.7 vs 128.4 ± 24.3 ng/mL, 1.64 ± 0.38 vs 3.9 ± 1.4 mg/dL, respectively)	Importantly, we observed better improvements in patients treated by baicalin than those on placebo treatment, demonstrating the beneficial effect of baicalin on further improving lipid profile. Moreover, the extent of improvements with regard to CT-1 and hs-CRP, two important risk factors of CAD, was also significantly better in the baicalin group than that in the placebo group, further indicating the efficacy of baicalin in alleviating CAD risks. In terms of RA symptom evaluation, we employed the EULAR as the indicator of RA in the present study. It was observed that proportion of patients maitaining good/moderate EULAR in baicalin group was significantly higher
https://pmc.ncbi.nlm.nih.gov/articles/PMC6396004/	3	Compared with those in the control group, baicalin had little effect on the treatment group's FPG and HBA1c, but it clearly reduced the AR activity and the difference was significant (P<0.05). Baicalin visibly decreased the 24-h urinary microalbumin, urinary β2-MG and UAER (P<0.05) and had notable effect on improving renal function. Following treatment, compared with those in the control group, baicalin distinctly increased the levels of SOD and GSH-px	This study revealed that patients' 24 h urine albumin, urinary β2-MG and UAER in the group receiving baicalin were overtly lower than those in the group undergone conventional treatment. This indicates that baicalin can reduce the level of proteinuria and distinctly improve renal function of the diabetic patients. After receiving baicalin treatment, the SOD and GSH-px levels of patients were obviously increased and the AR activity, NF-κB and VEGF content were decreased significantly, indicating that baicalin could reduce renal vascular permeability, improve renal function of patients
https://pmc.ncbi.nlm.nih.gov/articles/PMC11206508/	3	In this study the dietary supplement Lenidase®, consisting of escin, bromelain and baicalin, improved both VCSS and symptoms in “user” patients affected by CVI compared to “non-users” who underwent compression therapy only. Since the anti-inflammatory effects of baicalin were well-known and widely described, we hypothesized that VCSS improvement could be mainly ascribed to this natural compound. In fact, baicalin has been proven to decrease the serum levels of pro-inflammatory cytokines and CRP . Accordingly, we found that CRP significantly decreased in “users” compared to “non-users	Furthermore, both baicalin and escin reduce PGE2 synthesis [20,21], as does bromelain, thus inducing significant anti-inflammatory effect [23]. The modulation of inflammatory mediators is closely related to pain [41], therefore the pain-relieving effect observed in patients treated with Lenidase® could be attributed to all natural products. Patients who experienced an improvement in clinical signs of pain and inflammation were those who received the dietary supplement: a significant reduction was observed in “users” compared to “non-users” at T2.
https://www.sciencedirect.com/science/article/abs/pii/S0271531709000761?via%3Dihub	3	Both flavocoxid and naproxen showed significant reduction in the signs and symptoms of knee OA (P ≤ .001). There were no statistically detectable differences between the flavocoxid and naproxen groups with respect to any of the outcome variables. Similarly, there were no statistically detectable differences between the groups with respect to any adverse event, although there was a trend toward a higher incidence of edema and nonspecific musculoskeletal discomfort in the naproxen group. In this short-term pilot study, flavocoxid was as effective as naproxen in controlling the signs and symptoms of OA of the knee and would present a safe and effective option for those individuals on traditional nonsteroidal anti-inflammatory drugs or cyclooxygenase-2 inhibitors.	lavocoxid is a concentrated and greater than 90% pure standardized blend of baicalin, a free-B-ring flavonoid extracted from Scutellaria baicalensis, and catechin, a flavan from Acacia catechu with the remaining content being excipient and water [32]. In Asia, these compounds have been used for more than 1000 years for the treatment of a variety of inflammatory conditions. In preclinical biochemical assays, more impure mixtures of baicalin and catechin were shown to possess significant activity against the primary enzyme pathways involved in arachidonic acid metabolism, that is, COX-1, COX-2, and 5-LOX . Dual pathway inhibition greatly reduces the downstream production and imbalance of inflammatory mediators
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5555971/	1	Survivin connects with caspase activation and cell apoptosis through a variety of stimuli.32 Survivin inhibition increases caspase-dependent apoptosis and shows significant antitumor activity in multiple tumor cells in vivo and in vitro.33 In our study, baicalein significantly inhibited the expression of survivin and decreased the expression of survivin-activated caspase-3.	In our study, baicalein down-regulated the expression of Bcl-2 and up-regulated the Bax expression. This led to the cleavage of caspase-3 and caused BON1 cell apoptosis. Other research has shown that baicalein could not affect the expression of Bax and Bcl-2 in A549 cells in lung cancer strains. However, baicalein could increase the expression of tBID and release cytochrome c into cytosol. This led to apoptosis via a mitochondrial pathway
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5929448/	1	Taken together, our studies identify that baicalein and baicalin can significantly inhibit human colon cancer in vitro and in vivo. We further revealed that their anti-tumor effects were mechanistically due to the induction of colon cancer cell apoptosis or/and senescence. These data clearly suggest that both baicalein and baicalin have potent anti-cancer effects against human colon cancer and are potential novel and effective target drugs for cancer therapy.	In addition, our in vivo studies using human colon cancer cells in humanized mouse xenograft models, further demonstrated that baicalein and baicalin can induce tumor cell apoptosis and senescence, resulting in inhibition of tumorigenesis and growth of colon cancer in vivo. These data clearly suggest that baicalein and baicalin have potent anti-cancer effects against human colon cancer and could be potential novel and effective target drugs for cancer therapy
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9012617/	1	Baicalein can inhibit the proliferation and migration of human non-small-cell lung cancer cells. Signaling pathway regulation studies showed that Baicalein also inhibited the SMYD2/RPS7 signaling pathway in human non-small-cell lung cancer cells. This work provides a new content for the study of Baicalein against lung cancer	Baicalein significantly inhibited the growth of lung cancer cells. In addition, Baicalein significantly reduced the rate of A549 and NCI-H1299 cell invasion and clone formation in a dose-dependent manner. Animal experiments showed that both SMYD2 and Baicalein treatments could inhibit lung cancer tumor proliferation. Mechanism studies suggest that Baicalein inhibits the SMYD2/RPS7 signaling pathway.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6248272/	1	Taken together, our results demonstrated that baicalein had the potential to suppress cell proliferation, induce apoptosis and autophagy in MCF-7 and MDA-MB-231 breast cancer cells through inhibiting the PI3K/AKT pathway both in vitro and in vivo. These results suggest that baicalein may have therapeutic potential for breast cancer treatment and deserves further study	Our study demonstrated that baicalein induces apoptosis and autophagy of breast cancer cells via inhibiting the PI3K/AKT signaling pathway in vivo and vitro. Our study revealed that baicalein may be a potential therapeutic agent for breast cancer.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8567042/	1	In conclusion, we report the discovery that baicalein directly binds to TLR4 and inhibits TLR4/HIF‐1α/VEGF signaling pathway in CRC. Our data strongly support the translation of baicalein into novel TLR4‐targeting therapeutics for CRC treatment	Metastatic CRC presents in 25% of the patients at diagnosis, one‐third of the patients experience a metastatic relapse after initial curative surgical treatment. 5 , 6 The binding of baicalein to TLR4 that inhibits the HIF‐1α/VEGF signaling pathway holds a promising therapy for metastatic CRC treatment
https://www.gynecologiconcology-online.net/article/S0090-8258(16)30274-8/fulltext	1	Both in vitro and in vivo studies support baicalein as a potent inhibitor of endometrial cancer cell proliferation. The inhibitory effect correlates with mTOR pathway inhibition and increase in DDIT4 expression. This preclinical study supports the use of baicalein as a novel treatment for endometrial cancer.	We have identified a natural flavone, baicalein, which markedly upregulates DNA Damage Induced Transcript 4 (DDIT4), suppresses breast and ovarian cancer cell growth, and alters mTOR pathway. We examined the activity of baicalein in endometrial cancer cells.
https://biosignaling.biomedcentral.com/articles/10.1186/s12964-023-01156-7#	1	we have identified HQ and its component baicalin that are responsible for its enhancement of fluoropyrimidine antitumor activity, mediated through suppression of the various signaling pathways such as CDK/RB. Future studies will examine the influence of other HQ components on baicalin uptake and metabolism as it pertains to 5-FU modulation. Our results provide support for the role of HQ and baicalin as novel modulators of fluoropyrimidine chemotherapy in the treatment of drug-resistant CRC.	The combination of baicalin and 5-FU demonstrated synergistic activity against 5-FU-resistant RKO-R10 cells. The combination significantly inhibited in vivo tumor growth greater than each treatment alone. RPPA results showed that the signaling pathway alterations in CRC cells were similar following HQ and baicalin treatment. Together, these results indicate that HQ and its component baicalin enhance the effect of 5-fluorouracil-based chemotherapy via inhibition of CDK-RB pathway. These findings may provide the rational basis for developing agents that can overcome the development of cellular drug resistance.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4502300/	1	Taken altogether, our study demonstrates that baicalein markedly induces apoptosis and inhibits metastasis of androgen-independent prostate cancer cells. Mechanically, we find that cav-1/AKT/mTOR pathways account for the anti-tumor effects of baicalein. All these results imply that baicalein may be a promising therapeutic drug for androgen-independent prostate cancer patients.	In the present study, we demonstrated that baicalein can significantly inhibit the proliferation and induce apoptosis of androgen-independent prostate cancer cells, in accordance with previous research findings [11]. We further explored the molecular mechanisms through which baicalein induces apoptosis. The results indicated that the regulation of cav-1 and apoptotic proteins is required. Our data indicate a new mechanism through which baicalein exhibits its pro-apoptotic effect in prostate cancer cells.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8919235/	1	our data demonstrated that BA played anti-tumor roles in OS through an epigenetic regulatory pattern in which lncRNA-NEF expression was suppressed as well as Wnt/β-catenin signaling, thus resulted in the inhibition of tumor growth and metastasis. The findings provide a novel mechanism of the BA-mediated tumor suppression and suggest BA may be developed as a promising candidate for OS patients	BA was found to suppress cell viability via inducing cell cycle arrest and apoptosis as well as migration and invasion. The further orthotopic intra-tibia tumor-bearing model confirmed the anti-cancer activity of BA in vivo. Recent evidence also demonstrated that BA inhibited cell development, metastasis and EMT and induced apoptosis in OS cells
https://onlinelibrary.wiley.com/doi/full/10.1002/fft2.348	1	In this study, we investigated the role of baicalein in enhancing the insulin-sensitizing effect of metformin in mice with prediabetes. Baicalein, when combined with 25% of normal-dose metformin, achieved a diabetes-reversion rate of 80%, which was 1.86-fold that of normal-dose metformin. Mechanistically, baicalein enhanced the insulin-sensitizing effect of metformin on lipid metabolism by inhibiting de novo lipogenesis through the AMP-activated protein kinase/SREBP-1c/FASN pathway and by inducing fatty-acid β-oxidation through the upregulation of ACSL1, CPT1A, EHHADH, and acyl-CoA dehydrogenases	Meanwhile, baicalein enhanced the insulin-sensitizing effect of metformin via the modulation of the gut microenvironment by enriching probiotics, especially Akkermansia by 53.4-fold, depleting opportunistic pathogens, and strengthening the intestinal barrier. The improved gut microenvironment led to the alleviation of chronic endotoxemia, as evidenced by decreased levels of lipopolysaccharide and proinflammatory cytokines. Furthermore, baicalein enhanced the effect of metformin on decreasing the circulating level of branched-chain amino acids (BCAAs), which further improved insulin sensitivity by normalizing the mTORC1/p70S6K/IRS1 signaling pathway and de novo lipogenesis. Moreover, the role of baicalein in enhancing the insulin-sensitizing effect of metformin
https://www.spandidos-publications.com/10.3892/ijo.2013.2086	1	Accumulative evidence has shown a significant association between deficiency of PPARγ and IBD (29). In addition, activation of PPARγ attenuated the inflammation in the gut (30). These results suggested that colonic PPARγ may be a promising therapeutic target in patients suffering from IBD. In this study chemopreventive ability of baicalein at 3 different dose levels (1, 5, 10 mg/kg in diet) using inflammation-induced colon carcinogenesis model in mice were assessed. All doses of baicalein suppressed colonic inflammation and reduced the tumor incidence induced by AOM/DSS in a dose-dependent manner.	In conclusion, our findings indicate that the flavone, baicalein, being a major constituent of the Scutellaria baicalensis Georgi is one of the good candidates with multiple targets for cancer chemoprevention in colon related to inflammation associated-carcinogenesis....baicalein have effective anti-metastatic activity for the treatment of colon cancer by inhibiting the expression of MMP-9 and MMP-2, thus blocking cell migration and invasion pathways. Baicalein is a potent PPARγ activator that inhibits NF-κB and mediates inflammatory responses in colon cancer cells