Iridoid glycosides are natural products occurring widely in many herbal plants. Geniposide (C17H24O10) is a well-known one, present in nearly 40 species belonging to various families, especially the Rubiaceae. Along with this herbal component, dozens of its natural derivatives have also been isolated and characterized by researchers. Furthermore, a large body of pharmacological evidence has proved the various biological activities of geniposide, such as anti-inflammatory, anti-oxidative, anti-diabetic, neuroprotective, hepatoprotective, cholagogic effects and so on. However, there have been some research articles on its toxicity in recent years. Therefore, this review paper aims to provide the researchers with a comprehensive profile of geniposide on its phytochemistry, pharmacology, pharmacokinetics and toxicology in order to highlight some present issues and future perspectives as well as to help us develop and utilize this iridoid glycoside more efficiently and safely.

A Review on the Phytochemistry, Pharmacology, Pharmacokinetics and Toxicology of Geniposide, a Natural Product

Ethnobotanical study of Loloh: Traditional herbal drinks from Bali (Indonesia)

Tinospora species: An overview of their modulating effects on the immune system

Plants contain a much greater diversity of bioactive compounds than any man-made chemical library. Heart-shaped Piper betel leaves are magnificent reservoirs of phenolic compounds with antiproliferative, antimutagenic, antibacterial, and antioxidant properties. Widely consumed in South Asian countries, the glossy leaf contains a multitude of biophenolics such as hydroxychavicol, eugenol, chavibetol, and piperols. Convincing data underscore the remarkable chemotherapeutic and chemopreventive potential of betel leaves against a variety of cancer types. The leaf constituents modulate an extensive array of signaling molecules such as transcription factors as well as reactive oxygen species (ROS) to control multiple nodes of various cellular proliferation and death pathways. Herein, we provide an overall perspective on the cancer-fighting benefits of the phenolic phytochemicals in betel leaves and a comprehensive overview of the mechanisms responsive to dose-driven ROS-mediated signaling cascades conscripted by bioactive phenolics to confer chemotherapeutic and chemopreventive advantages. Intriguingly, these ROS-triggered responses are contextual and may either elicit a protective xenohormetic antioxidant response to premalignant cells to constitute a chemopreventive effect or generate a curative chemotherapeutic response by pro-oxidatively augmenting the constitutively elevated ROS levels in cancer cells to tip the balance in favor of selective apoptosis induction in cancer cells while sparing normal ones. In conclusion, this review provides an update on how distinct ROS levels exist in normal versus cancer cells and how these levels can be strategically modulated and exploited for therapeutic gains. We emphasize the yet untapped potential of the evergreen vine, betel leaf, for chemopreventive and chemotherapeutic management of cancer.

https://cancerpreventionresearch.aacrjournals.org/content/canprevres/7/5/477.full.pdf

Piper Betel Leaf: A Reservoir of Potential Xenohormetic Nutraceuticals with Cancer-Fighting Properties

Objective To examine the anti–bacterial activity of leaf extracts of Morus alba L. ( Moraceae ) and Piper betel L. ( Piperaceae ), and seed extracts of Bombax ceiba L. ( Borabacaceae ). Methods We have partially purified plant extracts by solvent extraction method, and evaluated the effect of individual fractions on bacterial growth using Escherichia coli ( E. coli ), Pseudomonas aeruginosa ( P. aeruginosa ) and Staphylococcus aureus ( S. aureus ) bacterial strains. Results Compared with Morus and Bombax fractions, Piper fractions showed significant growth inhibition on all the three types of bacteria studied. The EtOAc-hexane fractions of Piper leaves exhibited significant anti–bacterial activity with minimum inhibitory concentrations (MIC) of 50 μg/ml culture against both gram-positive and gram-negative bacteria. The EtOAc-fractions I, II, and IV inhibited bacterial colony formation on soft agar in addition to growth inhibition. A combination treatment of piper fractions with ampicillin resulted in significant growth inhibition in E. coli and P. aeruginosa , and combination with anticancer drug geldanamycin (2μg/ml) showed selective growth inhibition against P. aeruginosa and S. aureus . Three major compounds, i.e., eugenol, 3-hexene-ol and stigmasterol, were primarily identified from Piper betel leaf extractions. Among the individual compounds, eugenol treatment showed improved growth inhibition compared with stigmasterol and 3-hexene-ol. Conclusions We are reporting potential anti–bacterial compounds from Piper betel against both gram-positive and gram-negative bacteria either alone or in combination drug treatment.

Anti-microbial principles of selected remedial plants from Southern India

OBJECTIVE To study the chemical constituents from the stems of Piper betle. METHODS Various chromatographic techniques were used to isolate and purify the constituents. The structures of these compounds were elucidated on the basis of spectral analysis. RESULTS Nine compounds were isolated from the petroleum ester and ethyl acetate soluble fractions of the 70% acetone extract and their structures were identified as 6beta-hydroxystigmast-4-en-3-one (1), beta-sitosterol (2), stigmasterol (3), oleanolic acid (4), 23-hydroxyursan-12-en-28-oic acid (5), beta-sitosterol-3-O-beta-D-glucoside-6'-O-palmitate (6), beta-daucosterol (7), (2S) -4'-hydroxy- 2,3-dihydroflavonone-7-O-beta-D-glucoside (8) and alpha-ethyl glucoside (9). CONCLUSION Among these compounds, 1, 3 -9 are isolated from this plant for the first time.

Studies on the chemical constituents of the stems of Piper betle

Objective To study the chemical constituents from the roots of Tinospora sagittata var yunnanensis Methods Various chromatographic techniques were used to isolate and purify the constituents The structures of these compounds were elucidated on the basis of spectral analysis Results Seven compounds were isolated from the plant and their structures were identified as tinophylloloside (1), epitinophylloloside (2), 2-deoxycrustecdysone (3), polypodine B (4) , (+)-5'-methoxyisolariciresinol 3alpha-O-beta-D-glucopyranoside (5), geniposide (6), adenine (7) Conclusion All compounds are isolated from the plant for the first time,and compounds 4, 5, 6 and 7 are isolated firstly from the genus

Hui Liang

Papers

Studies on the chemical constituents of the stems of Piper betle

Studies on the chemical constituents from the roots of Tinospora sagittata var. yunnanensis (II)