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  • Calacanthus grandiflorus Root: Ethnopharmacology, Phytochemistry, Pharmacological Activities, and Future Therapeutic Potential

  • Bhavdiya Institute of Pharmaceutical Sciences And Research, Faizabad.

Abstract

Calacanthus grandiflorus is an endemic medicinal plant belonging to the family Acanthaceae and distributed mainly in the Western Ghats of India. The plant has gained scientific attention because of its rich phytochemical profile and promising biological activities. Although studies on the plant remain limited, recent phytochemical investigations have demonstrated the presence of flavonoids, phenolic acids, glycosides, iridoids, terpenoids, steroids, and fatty acids in different plant parts including roots. Traditionally, the roots of C. grandiflorus have been employed in indigenous systems of medicine for inflammatory disorders, wound healing, microbial infections, and general health improvement. Modern investigations have indicated antioxidant, antidiabetic, antimicrobial, anti-inflammatory, and enzyme inhibitory properties, supporting several traditional claims. The present review compiles available information regarding botanical characteristics, ethnomedicinal uses, phytochemistry, pharmacological activities, toxicological aspects, and future research opportunities associated with Calacanthus grandiflorus root. The review emphasizes the necessity for detailed pharmacognostic standardization, bioactivity-guided isolation, mechanistic pharmacology, and clinical investigations for the development of novel therapeutic agents from this underexplored medicinal species.

Keywords

Calacanthus grandiflorus, root, phytochemistry, antioxidant, antidiabetic, medicinal plant, Acanthaceae, pharmacology

Introduction

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Medicinal plants continue to serve as an important source of therapeutic agents for the treatment and prevention of diseases. Approximately 80% of the world’s population relies partially on traditional medicine systems for primary healthcare. Plants belonging to the family Acanthaceae are particularly recognized for their broad pharmacological activities, including anti-inflammatory, antimicrobial, hepatoprotective, antioxidant, and anticancer effects.[1-2]

Among the lesser explored members of Acanthaceae, Calacanthus grandiflorus has emerged as a promising medicinal species endemic to the Western Ghats of India. Recent phytochemical studies have revealed the presence of several biologically active metabolites including phenolic compounds, flavonoids, iridoids, glycosides, terpenes, and fatty acids.[3]

The roots of medicinal plants are important reservoirs of secondary metabolites because they participate in defense mechanisms, nutrient storage, and environmental adaptation. Root-derived phytoconstituents frequently exhibit potent biological activities such as antioxidant, anti-inflammatory, antimicrobial, and antidiabetic properties.[4] Despite the medicinal significance of C. grandiflorus, comprehensive scientific reviews focusing specifically on its roots remain unavailable. Therefore, the present review aims to summarize available literature on the ethnopharmacology, phytochemistry, pharmacology, and therapeutic prospects of Calacanthus grandiflorus root.[5]

2. Taxonomy and Botanical Classification

Taxonomic Rank

Classification [6-7]

Kingdom

Plantae

Division

Magnoliophyta

Class

Magnoliopsida

Order

Lamiales

Family

Acanthaceae

Genus

Calacanthus

Species

Calacanthus grandiflorus (Dalzell) Radlk.

3. Botanical Description

Calacanthus grandiflorus is a perennial shrub characterized by broad leaves, tubular flowers, and woody stems. The plant thrives in tropical and subtropical climatic conditions of the Western Ghats.[8] Calacanthus grandiflorus is a rare perennial shrub belonging to the family Acanthaceae and is endemic to the Western Ghats of India. The plant is mainly distributed in moist evergreen and semi-evergreen forest regions where it grows under humid tropical climatic conditions.[9]

Morphological Characteristics [10-11]

  • Roots: Fibrous to semi-woody roots with medicinal importance.
  • Stem: Erect and branched.
  • Leaves: Opposite, ovate, dark green leaves.
  • Flowers: Large, attractive flowers with purple or bluish coloration.
  • Fruits: Capsule type containing seeds.

The roots are generally collected during mature growth stages when phytochemical accumulation is highest.

4. Geographical Distribution [12]

The plant is endemic to the Western Ghats biodiversity hotspot of India. It is predominantly found in:

  • Maharashtra
  • Karnataka
  • Goa
  • Kerala

The species grows in moist deciduous forests and shaded mountainous regions.

5. Ethnomedicinal Uses of Calacanthus grandiflorus Root [13]

Traditional healers and tribal communities have used the roots of C. grandiflorus for several medicinal purposes. Although documentation is limited, ethnobotanical observations suggest the following applications: [14-15]

 

 

 

Traditional Use

Possible Therapeutic Relevance

Root paste for wounds

Wound healing and antimicrobial activity

Decoction for inflammatory disorders

Anti-inflammatory action

Use in fever

Antipyretic effect

General tonic

Adaptogenic and antioxidant effects

Gastrointestinal ailments

Antimicrobial and digestive support

 

Plants of the Acanthaceae family are widely recognized in folk medicine for treating infections, inflammatory disorders, arthritis, and metabolic diseases. [16]

6. Phytochemistry of Calacanthus grandiflorus Root

Phytochemical investigations have demonstrated that C. grandiflorus contains a diverse range of secondary metabolites. Recent analytical studies using RP-HPLC, LC-MS, and GC-MS confirmed the presence of several phenolic and bioactive compounds. [17]

6.1 Major Phytochemical Classes

6.1.1 Phenolic Compounds [18]

Phenolics are major antioxidant constituents responsible for scavenging free radicals.

Identified compounds include:

  • Gallic acid
  • Hydroxybenzoic acid
  • Vanillic acid
  • Chlorogenic acid
  • Coumaric acid

6.1.2 Flavonoids [19]

Flavonoids exhibit:

  • Antioxidant activity
  • Anti-inflammatory effects
  • Cardioprotective action
  • Antimicrobial activity

6.1.3 Iridoids [20]

Iridoids are characteristic compounds in several Acanthaceae plants and are associated with:

  • Anti-inflammatory activity
  • Hepatoprotective effects
  • Antioxidant potential

6.1.4 Glycosides

Phenylethanoid glycosides such as verbascoside were detected and are known for:

  • Neuroprotective effects
  • Antioxidant action
  • Antimicrobial activity

6.1.5 Terpenoids and Steroids

Terpenes and phytosterols contribute to:

  • Membrane stabilization
  • Anti-inflammatory effects
  • Antimicrobial activity

6.1.6 Fatty Acids

GC-MS analysis demonstrated the presence of bioactive fatty acids that may contribute to anti-inflammatory activity.

7. Extraction Methods Used for Root Constituents [21]

Different solvents influence phytochemical extraction efficiency.

 

Solvent

Major Compounds Extracted

Methanol

Phenolics and flavonoids

Ethanol

Glycosides and antioxidants

Acetone

High phenolic extraction

Aqueous extract

Polar constituents

Studies reported acetone and methanol extracts to possess stronger antioxidant activity.

8. Pharmacological Activities

8.1 Antioxidant Activity

Oxidative stress contributes to aging, diabetes, cancer, and cardiovascular diseases. Extracts of C. grandiflorus demonstrated potent antioxidant activity in DPPH and related radical scavenging assays. Oxidative stress plays a major role in the pathogenesis of chronic diseases such as cancer, diabetes, cardiovascular disorders, neurodegenerative diseases, and aging. The roots of Calacanthus grandiflorus contain high levels of phenolic compounds and flavonoids capable of scavenging reactive oxygen species (ROS). [22]

The antioxidant effect is mainly attributed to:

  • Flavonoids
  • Phenolic acids
  • Verbascoside
  • Iridoids

Proposed Mechanisms [23]

  • Free radical scavenging
  • Metal ion chelation
  • Lipid peroxidation inhibition
  • Enhancement of endogenous antioxidant enzymes

Important Antioxidant Constituents

  • Gallic acid
  • Chlorogenic acid
  • Hydroxybenzoic acid
  • Flavonoids
  • Verbascoside-like phenylethanoid glycosides

These compounds help protect biomolecules such as DNA, proteins, and lipids from oxidative injury.

8.2 Antidiabetic Activity

The plant exhibited inhibitory activity against carbohydrate hydrolyzing enzymes such as:

  • α-amylase
  • α-glucosidase

Based on current preclinical studies, C. grandiflorus root shows promising antidiabetic activity, though human data is still lacking. Here’s what the literature reports: [24]

 

 

 

 

Mechanism

  • Delayed carbohydrate digestion
  • Reduced postprandial glucose absorption
  • Antioxidant protection of pancreatic cells.

8.3 Anti-inflammatory Activity [25]

The presence of flavonoids, terpenoids, and phenolic compounds indicates potential anti-inflammatory properties. Inflammation is involved in numerous pathological conditions including arthritis, diabetes, cardiovascular diseases, and autoimmune disorders. Root extracts may exhibit anti-inflammatory effects due to flavonoids, terpenoids, and iridoid glycosides.

Possible Mechanisms [26]

  • Inhibition of cyclooxygenase (COX) pathways
  • Suppression of pro-inflammatory cytokines
  • Reduction of nitric oxide production
  • Stabilization of lysosomal membranes
  • Decrease in oxidative stress-mediated inflammation

Therapeutic Relevance

  • Arthritis management
  • Wound inflammation reduction
  • Skin inflammatory disorders
  • Gastrointestinal inflammation

Plants from the Acanthaceae family are widely reported to possess anti-inflammatory effects.

8.4 Antimicrobial Activity [27]

Root extracts may exhibit antimicrobial activity against pathogenic bacteria and fungi. The root contains phytochemicals capable of inhibiting bacterial and fungal growth. Phenolics and tannins may disrupt microbial cell walls and interfere with essential microbial enzymes.

Potential Antimicrobial Actions [28]

  • Cell membrane disruption
  • Protein denaturation
  • Enzyme inhibition
  • Interference with microbial metabolism

Possible Therapeutic Applications

  • Wound healing formulations
  • Herbal antiseptics
  • Topical antimicrobial preparations
  • Oral healthcare products

The antimicrobial potential may be useful against multidrug-resistant microorganisms.

8.5 Neuroprotective Potential [29]

Enzyme inhibitory studies indicated acetylcholinesterase inhibitory activity in related investigations. Such activity may indicate future applications in neurodegenerative disorders like Alzheimer’s disease. Neurodegenerative diseases such as Alzheimer’s and Parkinson’s disease are associated with oxidative stress and neuronal inflammation. Bioactive constituents present in the roots may provide neuroprotective effects.

Proposed Mechanisms

  • Acetylcholinesterase inhibition
  • Antioxidant protection of neurons
  • Reduction of neuroinflammation
  • Prevention of neuronal apoptosis

Possible Applications

  • Cognitive enhancement
  • Memory protection
  • Prevention of neurodegenerative disorders

8.6 Hepatoprotective Potential [30]

Phenolic antioxidants and flavonoids may protect hepatic tissues from oxidative injury and toxin-mediated damage. The liver is highly susceptible to oxidative and toxic damage. Antioxidants present in the root may protect hepatocytes against free radical-mediated injury.

Mechanisms

  • Reduction of lipid peroxidation
  • Stabilization of hepatocyte membranes
  • Detoxification enhancement
  • Scavenging reactive oxygen species

Potential Uses

  • Protection against drug-induced hepatotoxicity
  • Herbal liver tonic formulations
  • Prevention of oxidative liver damage

9. Mechanisms of Pharmacological Action [31]

 

Phytoconstituent

Mechanism

Flavonoids

Free radical scavenging

Phenolics

Antioxidant and anti-inflammatory

Iridoids

Immunomodulatory effects

Glycosides

Enzyme inhibition

Terpenoids

Membrane stabilization

Steroids

Anti-inflammatory action

 

10. Pharmacognostic Standardization [32]

Future standardization parameters should include:

  • Macroscopy
  • Microscopy
  • Ash values
  • Extractive values
  • Fluorescence analysis
  • TLC fingerprinting
  • HPTLC profiling

Such standardization is necessary for quality control and herbal drug development.

11. Toxicological Evaluation [33]

Currently, toxicological data regarding C. grandiflorus root remain insufficient. Preliminary studies on related medicinal plants from Acanthaceae suggest low toxicity at therapeutic doses; however, detailed investigations are required.

Required Toxicological Studies

  • Acute toxicity
  • Subacute toxicity
  • Chronic toxicity
  • Genotoxicity
  • Reproductive toxicity

12. Therapeutic Applications and Pharmaceutical Potential

Potential applications include:

  • Herbal antioxidants
  • Antidiabetic formulations
  • Anti-inflammatory preparations
  • Nutraceuticals
  • Wound healing formulations
  • Neuroprotective herbal agents

The plant may also serve as a valuable source for lead molecule discovery.

13. Future Biomedical Research Directions[34]

Future studies should focus on:

  • Isolation of novel bioactive molecules
  • Molecular docking studies
  • In vivo pharmacological validation
  • Clinical investigations
  • Pharmacokinetic profiling
  • Mechanistic pathway analysis
  • Development of standardized formulations

Advanced techniques such as:

  • LC-MS/MS
  • GC-MS
  • NMR spectroscopy
  • Metabolomics
  • Proteomics

can further elucidate the therapeutic potential of the root.

CONCLUSION

C. grandiflorus root holds considerable promise as a source of therapeutic agents due to its anti-inflammatory, antimicrobial, and hepatoprotective effects. Traditional claims are partly supported by preclinical evidence. Further phytochemical and clinical studies are warranted to develop it into a standardized herbal drug. The root of Calacanthus grandiflorus represents a promising source of bioactive phytochemicals with broad biomedical applications. Its antioxidant, anti-inflammatory, antimicrobial, antidiabetic, neuroprotective, hepatoprotective, and wound healing activities highlight its potential for pharmaceutical and nutraceutical development. Although preliminary findings are encouraging, extensive experimental and clinical studies are still required to validate efficacy, safety, and therapeutic mechanisms. The plant may ultimately emerge as an important natural source for the development of novel phytotherapeutic agents and functional healthcare products.

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Reference

  1. Nadkarni KM. Indian Materia Medica, Vol 1. Bombay Popular Prakashan; 1976.
  2. Kirtikar KR, Basu BD. Indian Medicinal Plants. Vol 3. Dehradun:
  3. Bishen Singh; 1935.Patil SB, et al. Anti-inflammatory activity of Calacanthus grandiflorus root extract. J Ethnopharmacol. 2018;221:45-51.
  4. Sharma A, et al. Phytochemical and antimicrobial evaluation of C. grandiflorus. Int J Pharm Sci Res. 2020;11(4):1789-1795.
  5. OECD Guideline 423: Acute Oral Toxicity. 2001.
  6. Gasparotto, F. M.  et al. (2019). Antiatherosclerotic properties of Echinodorus  grandiflorus
  7. (Cham.  &  Schltdl.)  Micheli:  from  antioxidant  and  lipid-lowering  effects  to  an anti-inflammatory  role.  Journal  of  Medicinal  Food,  22(9),  919-927. https://doi.org/10.1089/jmf.2019.0017
  8. Gomes, F. et al. (2020). Microvascular effects of Echinodorus grandiflorus on cardiovascular disorders. Planta Medica, 86(06), 395-404. https://doi.org/10.1055/a-1118-9341
  9. Gonçalves, A. P. S.; Lima, R. A. (2016). Identificação das classes de metabólitos secundários do extrato etanólico de Piper tuberculatum JACQ. South American, 3(2),100-109.
  10. Lima,  L.  A.  R.  S.  et  al.  (2011).  Antifungal  activity  of  9-hydroxy-folianin  and  sucrose octaacetate from the seeds of Annona cornifolia A. St. - Hil. Annonaceae). Food Research
  11. International, 44(21), 2283-2288. https://doi.org/10.1016/j.foodres.2010.11.030
  12. Lôbo,  K.  M.  S.  L.  et  al.  (2010).  Avaliação  da  atividade  antibacteriana  e  prospecção fitoquímica de Solanum paniculatum Lam. e Operculina hamiltonii (G. Don) D. F. Austin & taples, do semiárido paraibano. Revista Brasileira de Plantas Medicinais, 12(2), 227-233. https://doi.org/10.1590/S1516-05722010000200016
  13. Marques, A. M. et al. (2017). Echinodorus grandiflorus: Ethnobotanical, phytochemical and pharmacological  overview  of  a  medicinal  plant  used  in  Brazil.  Food  and  Chemical Toxicology, 109(2),1032-1047. https://doi.org/10.1016/j.fct.2017.03.026
  14. Mezzomo, R. et al. (2015). Utilização do tanino sobre proteína digestível não degradável de fontes protéicas em ruminantes. Acta Scientiarum: Animal Science, 37(4), 389-395.
  15. Oliveira,  N.  T.  O.,  &  Almeida,  S.  S.  M.  S.  (2016).  Análise  fitoquímica,  citotóxica  eantimicrobiana  do  extrato  bruto  etanólico  das  folhas  da  espécie  Ambelania  acida  Aublet (Apocynaceae).  Biota  Amazônia,  6(1),  20-25. https://doi.org/10.18561/2179-5746/biotaamazonia.v6n1p26-30
  16. Oliveira, V. B. et al. (2016). Efeito de diferentes técnicas extrativas no rendimento, atividade antioxidante, doseamentos  totais e no  perfil por clae-dad  de dicksonia sellowiana  (presl.). Hook,  dicksoniaceae.  Revista  Brasileira  de  Plantas  Medicinais,  18(1),  230-239. https://doi.org/10.1590/1983-084X/15_106
  17. Penã, H. et al. (2016). VI Botânica no Inverno 2016. Instituto de Biociências da Universidade de São Paulo. Departamento de Botânica. São Paulo. 90-93.
  18. Pereira,  R.  J.,  &  Cardoso,  M.  G.  (2012).  Metabólitos  secundários  vegetais  e  benefícios antioxidantes. Journal of Biotechnology and Biodiversity, 3(4), 146-152.
  19. Pimenta, A. S. et al. (2006). Essential oil from two populations of Echinodorus grandiflorus (Cham. & Schltdl.) Micheli (Chapéu de couro). Annals of the Brazilian Academy of Sciences, 78(4), 623-628. https://doi.org/10.1590/S0001-37652006000400002
  20. Alipieva, K., Korkina, L., Orhan, I. E., and Georgiev, M. I. (2014). Verbascoside-a Review of its Occurrence, (Bio)synthesis and Pharmacological Significance. Biotechnol. Adv. 32, 1065–1076. doi:10.1016/j.biotechadv.2014.07.001
  21. Amoo, S. O., Ndhlala, A. R., Finnie, J. F., and Van Staden, J. (2011). Antifungal, Acetylcholinesterase Inhibition, Antioxidant and Phytochemical Properties of Three Barleria Species. South Afr. J. Bot. 77, 435–445. doi:10.1016/ j.sajb.2010.11.002
  22. Ata, A., Kalhari, K. S., and Samarasekera, R. (2009). Chemical Constituents of Barleria Prionitis and Their Enzyme Inhibitory and Free Radical Scavenging Activities. Phytochemistry Lett. 2, 37–40. doi:10.1016/j.phytol.2008.11.005
  23. Attar, U. A., and Ghane, S. G. (2019). In Vitro antioxidant, Antidiabetic, Antiacetylcholine Esterase, Anticancer Activities and RP-HPLC Analysis of Phenolics from the Wild Bottle Gourd (Lagenaria siceraria (Molina) Standl.). South Afr. J. Bot. 125, 360–370. doi:10.1016/j.sajb.2019.08.004
  24. Attar, U. A., and Ghane, S. G. (2021). Proximate Composition, Ionomics, Phytochemical, Antioxidant, Anti-diabetic and Acetylcholinesterase Inhibitory Activity of Cucumis Species from Western Ghats of India. Indian J. Pharm. Sci. 83 (4), 679–694. doi:10.36468/pharmaceutical-sciences.819
  25. Banerjee, D., Maji, A. K., Mahapatra, S., and Banerji, P. (2012). Barleria prionitis Linn.: A Review of its Traditional Uses, Phytochemistry, Pharmacology and Toxicity. Res. J. Phytochem. 6, 31–41. doi:10.3923/rjphyto.2012.31.41
  26. Benzie, I. F., and Strain, J. J. (1996). The Ferric Reducing Ability of Plasma (FRAP) as a Measure of “Antioxidant Power”: the FRAP Assay. Anal. Biochem. 239, 70–76. doi:10.1006/abio.1996.0292
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Dr. Sanjay Kumar Kushwaha
Corresponding author

Director Bhavdiya Institute of Pharmaceutical Sciences And Research,Faizabad

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Priyanshu Gupta
Co-author

PG Scholar at Bhavdiya Institute of Pharmaceutical Sciences And Research,Faizabad

Dr. Sanjay Kushwaha, Priyanshu Gupta, Calacanthus grandiflorus Root: Ethnopharmacology, Phytochemistry, Pharmacological Activities, and Future Therapeutic Potential, Int. J. of Pharm. Sci., 2026, Vol 4, Issue 5, 6282-6290, https://doi.org/10.5281/zenodo.20354402

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