Globally, cancer has emerged as a leading health concern. It is estimated that the number of new cancer cases can elevate by 70% over the next two decades. For decades, medicinal plants have been constantly exploited by mankind as sources of cancer-fighting agents. There is an emerging focus on the identification and production of novel bioactive natural compounds as effective, non-toxic alternatives to chemotherapeutic drugs.
Fruits are highly rich in natural antioxidants. Consuming fruits can boost your immune system and may eliminate cancer risk. One such fruit is Gardeniae Fructus that has been utilized in traditional Chinese medicine for centuries. Geniposide, the main compound of Gardenia Fructus, has been found to exhibit an anti-tumor effect.
Geniposide is hydrolyzed into genipin (aglycone form) by β-glucosidase produced by intestinal bacteria. The beneficial effects of geniposide come from their ability to function as antioxidants inside your body and thus playing a crucial role in helping your body scavenge free radicals associated with chronic diseases.
Let us explore how geniposide helps to fight cancer:
- What is geniposide?
- Source of geniposide
- Health benefits of geniposide
- Geniposide and Cancer
What is geniposide?
Geniposide (C17H24O10) is a well-known iridoid glycoside compound.
Source of geniposide
It is primarily isolated from Gardeniae Fructus, the dried ripe fruit of Gardenia jasminoides Ellis (Zhizi in Chinese). It is also present in:
- Achyranthes bidentata Bl. (Niuxi in Chinese)
- Rehmannia glutinosa Libosch. (Dihuang in Chinese)
- Eucommia ulmoides Oliv. (Duzhong in Chinese)
Health benefits of geniposide
Geniposide displays versatile therapeutic benefits such as antioxidant, neuroprotective, hepatoprotective, antidiabetic, anti-inflammatory, analgesic, cardioprotective, antidepressant, immune-regulatory, and antithrombotic.
Geniposide and Cancer
Geniposide may be a potential therapeutic agent for the management of cancer. Geniposide and genipin (the aglycone of geniposide) have demonstrated cytotoxicity in various cancer cell types including HepG2 breast cancer (MDA-MB231cells), pancreatic adenocarcinoma cells, AGS and SNU638 human gastric carcinoma cells, human leukemia (K562, HL-60, U266, U937) cells, prostate (DU151, PC3 cancer cells), tongue squamous carcinoma cells (HSC3), non-small lung cancer H1299 cells, and colorectal cancer.
A study depicted that geniposide could protect gastric cancer cells by diminishing cell migration, viability, invasion, and colony formation in the MKN45 cell line. Geniposide induced apoptosis, inactivated PI3K/AKT (phosphatidylinositol 3′-kinase/ protein kinase B) and JNKN (terminal kinase signal pathway) signal pathways by down-regulating HULC.
In human oral squamous carcinoma cells, geniposide illustrated an anti-proliferative effect. In hepatoma cells, geniposide promoted apoptosis. Geniposide has been reported to suppress the generation of hydroperoxide and myeloperoxidase caused by TPA (12-O-tetradecanaoylphorbol-13-acetate) in addition to suppressing TPA-induced skin tumors in female CD–1 mice in vivo.
In the CAM (chick embryo chorioallantoic membrane) assay, the ethanol extract of Gardenia jasminoides Ellis fruits displayed considerable anti-angiogenic activity. In this study, geniposide illustrated an anti-angiogenic effect in a dose-dependent manner.
Another study depicted that geniposide-based treatment may be utilized for managing patients having metastatic cancer since this glycoside may:
- Suppress the progression of metastatic tumors
- Elevate the expression of metastasis suppressor genes in tumors (TPM1 and TAp63)
- Improve the efficacy of cancer interventions
- Thus, oncologists may consider experimenting geniposide for managing advanced metastatic cancers.
Several treatments such as immunotherapy, chemotherapy, surgery, radiation therapy, endocrine therapy, and targeted therapy are utilized to manage cancer. However, these current interventions are associated with deleterious adverse effects. It is therefore essential to develop robust strategies with fewer side effects and no toxicity.
Plants are extensively exploited as natural sources of drugs for cancer treatment. The contemporary pharmacological studies are steadily drawing substantial attention to geniposide from the gardenia fruit. Owing to the favorable effects, this natural antioxidant serves as a potent weapon against cancer. It yields a novel avenue for the therapeutic strategy in cancer management.
As a bioactive natural product, geniposide may be developed as a candidate drug to fight with cancer. However, future studies will certainly provide more insight into geniposide’s pharmacological benefits and its potential use for cancer prevention and intervention.
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