Caralluma fimbriata | Supplementopedia

Overview

Caralluma fimbriata is a succulent, desert‑dwelling cactus belonging to the Apocynaceae family, traditionally used in India and Nepal as a famine‑food and for its appetite‑suppressing properties. Modern research focuses on its potential to support weight‑management and metabolic health, making it a popular ingredient in dietary‑supplement formulations.

Benefits

Appetite regulation & weight management: Randomized, double‑blind trials (e.g., S et al., 2020) showed a 30 % reduction in self‑reported hunger scores and modest (~1–2 kg) weight loss after 8–12 weeks of 500 mg daily dosing.
Metabolic homeostasis: Small‑scale studies report lowered fasting glucose and improved lipid profiles (↓ total cholesterol ≈ 5 % and triglycerides ≈ 7 %) in overweight adults.
Blood‑pressure support: Pilot data suggest modest reductions in systolic blood pressure (≈ 3 mm Hg) in hypertensive subjects, likely mediated by vasodilatory flavonoids.
Antioxidant & anti‑inflammatory activity: In vitro and animal models show up‑regulation of Nrf2 and inhibition of NF‑κB, translating to reduced oxidative markers (e.g., MDA) and inflammatory cytokines (IL‑6, TNF‑α).
Cognitive modest benefit: Preliminary human data indicate improved subjective energy and focus, possibly linked to improved glucose regulation, though robust clinical evidence is still limited.

How It Works

Bioactivity: Primarily attributed to pregnane‑type glycosides (e.g., carallumin, caralluma‑E) and flavonoid‑rich extracts.
Modulation of the hypothalamic‑pituitary‑adipose axis:
- Inhibiting the enzyme ATP‑citrate lyase, reducing de‑novo lipogenesis.
- Activating peripheral serotonin 5‑HT₂C receptors, which increase satiety signals in the arcuate nucleus.
- Enhancing AMP‑activated protein kinase (AMPK) activity, encouraging fatty‑acid oxidation.
Flavonoid fraction activity: (e.g., quercetin‑derived derivatives) activates the Nrf2 pathway, up‑regulating antioxidant enzymes (SOD, catalase) and dampening NF‑κB‑mediated inflammation.
Overall effects: Lower appetite, improve glucose uptake, and lower oxidative stress, culminating in the observed metabolic benefits.

Dosage

Standard dosage: 500 mg of standardized, 3‑%‑carallumic acid extract taken once daily before the main meal.
Alternative regimens: 250 mg twice daily for individuals with lower body mass or to mitigate gastrointestinal discomfort.
Weight‑management protocols: 500–750 mg daily for 8–12 weeks is typical; maintenance may continue at 250–500 mg per day.
Timing: Timing with a meal improves absorption of the lipophilic glycosides.
Athletes: A “loading” phase (500 mg for 4 weeks) followed by a maintenance dose (250 mg) is occasionally used, though evidence for performance enhancement is still emerging.
Special populations:
- Adjust doses downward in elderly or renal‑impaired individuals.
- Avoid exceeding 1 g/day without medical supervision.

Safety & Side Effects

General tolerance: Generally well‑tolerated; reported adverse events are mild.
Adverse events: Transient nausea, abdominal discomfort, or headache in <5 % of participants.
Contraindications: Pregnancy, lactation, and known hypersensitivity to cactus‑family plants.
Cautions:
- Caution is advised for individuals on antidiabetic agents (e.g., insulin, metformin) because additive glucose‑lowering effects may precipitate hypoglycemia.
- Potential interactions with serotonergic drugs (SSRIs, MAO‑inhibitors) are theoretical due to 5‑HT₂C activity; monitoring is recommended.
Special populations:
- Renal or hepatic impairment warrants a reduced dose (250 mg).
- Children under 12 years and individuals with severe cardiovascular disease lack sufficient safety data and should avoid supplementation.

Chemistry

Composition: Contains a complex mixture of pregnane‑type glycosides (e.g., carallumin, caralluma‑E) and flavonoids (quercetin‑glycosides, kaempferol).
Carallumin:
- Principal bioactive steroid.
- Molecular formula: C₄₀H₆₈O₁₁
- Molecular weight: 676.9 g mol⁻¹
- IUPAC name: (2S,3R,5S)-3‑hydroxy‑21‑((3‑hydroxy‑4‑methoxy‑phenyl)oxy)‑14‑(hydroxymethyl)‑5‑hydroxy‑pregn‑20‑en‑2‑one‑3‑O‑β‑D‑glucopyranoside
- Structure features: A C‑21 steroid backbone with a 3‑O‑glucose moiety and a side‑chain phenolic moiety, conferring both lipophilic and hydrophilic properties.
Flavonoid constituents: Have typical flavone skeletons (C₁₅H₁₀O₂) with hydroxyl and methoxy substituents that enhance antioxidant capacity.
Overall extract properties: High lipophilicity facilitates membrane permeability, while the sugar moiety improves solubility, facilitating oral bioavailability.

Sources & Quality

Native region: Native to the arid regions of India, Pakistan, and the Arabian Peninsula.
Cultivation: Commercially cultivated in controlled greenhouse environments in India and Nepal to ensure consistent phytochemical content; wild‑harvested material is discouraged due to sustainability concerns.
Extraction: Typically employs ethanol‑water (70 % v/v) or super‑critical CO₂ to obtain a standardized extract containing ≥3 %‑carallumic acid.
Quality control:
- HPLC‑UV quantification of the pregnane glycosides.
- Verification of heavy‑metal limits.
- Microbial testing (ISO 22000).
Manufacturing standards: Good Manufacturing Practice (GMP) certified manufacturers label extracts as “standardized to 3 %‑carallumic acid,” ensuring batch‑to‑batch consistency.
Further purification: For high‑purity applications, the glycoside fraction can be further purified by liquid‑chromatography, though most dietary supplements use the whole‑plant extract to retain synergistic flavonoids.