Nexrutine®: Huáng bǎi (黄栢 or 黃栢 ) or Huáng bò (黄檗): Chemoprotective and Chemopreventive Herb from the Amur Cork Tree

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Huáng bǎi (黄栢 or 黃栢 ) or Huáng bò (黄檗), also known as Cortex Phellodendri, is the bark of one of two species of Phellodendron tree: Phellodendron amurense or Phellodendron chinense.  Phellodendron amurense Rupr. is a species of tree in the family Rutaceae, commonly called the Amur cork tree.

AmurCorktreeBark03

Amur Cork Tree bark

A large number of active molecules have been identified and found in the bark.  They include:

(Source:  Wikipedia – Huáng bǎi)

Nexrutine® is a patented compound extracted from Phellodendron amurense trees.  Next Pharmaceuticals, a research and development company is the formulator of Nexrutine®.

A number of scientific studies have shown the extensive chemoprotective capabilities of Nexrutine®, specifically in the following cancers:

Nexrutine® has been shown to inhibit cancer cell growth as a consequence of mitochondrial damage and mitophagy.  One study revealed that autophagy plays an important role in the inhibition of cancer cell proliferation by Nexrutine®.  1

Breast Cancer

In this study we investigated the anticancer effects of Nexrutine on ER negative breast cancer cell lines that are positive or negative for HER-2. Nexrutine decreased the activities of 2 potential targets of breast cancer, cyclooxygenase (COX)-2, and peroxisome proliferators activated receptor gamma (PPARγ). The antiinflammatory effects of Nexrutine were evident with decreased prostaglandin (PG)E2 production, protein expression of microsomal PGE2 synthase (mPGES), and PPARγ. Nexrutine decreased cell survival and induced a G1 cell cycle arrest in SkBr3 and MDA-MB 231 cells, which were associated with reduced protein expression of Cyclin D1 and cdk2 along with increased protein expression of p21 and p27. The growth-inhibitory effect of Nexrutine was associated with apoptosis in SkBr3 cells and autophagy in MDA-MB231 cells. Based on these findings, we propose that Nexrutine may provide a novel approach for protection against breast cancer.  2

Colon Cancer

Here, we explored the mechanism of chemopreventive/chemotherapeutic efficacy of Nexrutine (NX) against colon cancer. We found that dietary exposure of Nexrutine (NX) significantly reduced the number of azoxymethane (AOM)-induced aberrant crypt foci (ACF) in rats. In addition, significant inhibition in AOM-induced cell proliferation and reduced expression of the inflammatory markers COX-2, iNOS as well as the proliferative markers PCNA and cyclin D1 were also seen. Moreover, Nexrutine (Nexrutine (NX)) exposure significantly enhanced apoptosis in the colon of AOM treated rats.  Based on these in vivo and in vitro findings, we suggest that Nexrutine (NX) could be useful candidate agent for colon cancer chemoprevention and treatment.   3

Pancreatic Cancer

Recent studies from our laboratory have shown that Nexrutine® (Nx), a bark extract from Phellodendron amurense exhibits excellent anticancer activity in human pancreatic cancer cells through inhibition of inflammatory signaling via STAT3/NFκB/Cox-2. Given the apparent high oxidative stress and autophagic activity in pancreatic tumors, we investigated the potential of Nx to modulate autophagy, reactive oxygen species (ROS), and their crosstalk. Our results show that Nx inhibits autophagy and decreases ROS generation.  Overall, our findings reveal an important role for STAT3/LC3/ROS in Nx-mediated anti-pancreatic cancer effects.  4

Prostate Cancer

The current standard of care for prostate cancer includes hormone therapy, radiation therapy and radical prostatectomy, each with its own set of undesirable side effects. In this regard there is an unmet need to develop strategies that can prevent or delay the development of clinical prostate cancer. One potential area involves the use of natural compounds involving botanicals. Along these lines we have found that Nexrutine®, a dietary supplement derived from Phellodendron amurense bark extract, has prostate cancer prevention activity.   5

Skin Cancer

In the present investigation, we explored the mechanism of chemopreventive/chemotherapeutic efficacy of NX against skin cancer. Single application of NX (1.0mg/mouse) prior to 12-O-tetradecanoylphorbol 13-acetate (TPA) application significantly inhibited TPA-induced skin edema, hyperplasia, thymidine incorporation and ornithine decarboxylase (ODC) activity; expression of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS); phosphorylation of extracellular signal-regulated kinases (ERK) 1/2, p38 and c-jun N-terminal kinase (JNK) mitogen-activated protein kinases (MAPKs); and activation of I kappa B kinase (IKK), IκBα and nuclear factor-kappa B (NF-κB) in mouse skin.  Based on our in vivo and in vitro studies, NX could be useful in the management (chemoprevention as well as chemotherapy) of skin cancer.  6


Resources:

Swanson Health Products – Nexrutine

 

Huang Bai, Extract Powder Phellodendron Amurense Bark,黃柏濃縮粉,100 g/bt

 

Nexrutine


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