A Review on the Phytochemical Profile and Multifaceted Pharmacological Effects of Leucas Cephalotes.

Abstract

Leucas cephalotes (Roth) Spreng is a versatile medicinal herb traditionally used across India for treating a wide range of ailments. Tribes and local communities use its leaves, flowers, stems, and roots to manage fever, cough, diarrhoea, mouth ulcers, skin infections, snake bites, and inflammatory conditions. Phytochemical studies have identified several bioactive compounds in the plant, including diterpenes (leucasdins A–C), triterpenes (leucastrins A and B, oleanolic acid), sterols (?-sitosterol, stigmasterol), flavonoids, and essential fatty acids, which are responsible for its diverse therapeutic effects. Scientific research has demonstrated that Leucas cephalotes exhibits hepatoprotective, antioxidant, antimicrobial, anti-inflammatory, analgesic, anthelmintic, anti-diabetic, and anti-filarial activities. These findings support its traditional uses and highlight its potential as a source of natural bioactive compounds for drug development. This review aims to provide a comprehensive overview of the ethnomedicinal applications, chemical composition, and pharmacological properties of Leucas cephalotes, emphasizing its relevance for future therapeutic research..

Keywords

Introduction

Leucas cephalotes (Roth) Spreng., a member of the Lamiaceae family (formerly Labiatae), is a widely distributed annual herb found predominantly in tropical and subtropical regions of Asia and Africa. In India, it commonly grows as a rainy-season weed, especially in northern parts of the country. The plant is popularly known as Dronapushpi in Sanskrit and Kubo or Kubi in the traditional medicine practices of Gujarat. It holds a significant place in indigenous systems of medicine due to its broad spectrum of therapeutic applications.₁

In Ayurveda, Leucas cephalotes is described as a mild stimulant, diaphoretic, and emmenagogue. It is traditionally used in the management of fever, liver disorders, and inflammatory conditions. The plant is also recognized for its usefulness in treating dermatological disorders such as psoriasis, scabies, and chronic skin eruptions, where it is often considered a blood purifier. Additionally, it is employed in the treatment of respiratory ailments including bronchitis, asthma, and cough. The flowers, when mixed with honey, are commonly used as a household remedy for colds and throat infections.₂

Ethnomedicinal reports suggest that different parts of the plant possess diverse biological activities. The leaves are used in fever and urinary conditions, while preparations of the plant are also utilized in dyspepsia, paralysis, and eye disorders₃. Notably, it has been used as a traditional remedy for snakebite and as a supportive treatment in chronic malaria and asthma in homeopathic practices.₄

Phytochemical studies indicate that L. cephalotes contains a variety of bioactive constituents such as triterpenes, flavonoids, sterols, and oleanolic acid, which are responsible for its pharmacological effects.₅ The plant is also reported to contain fatty acids like lauric acid, adipic acid, and glutaric acid, along with essential oil components including caryophyllene oxide and other volatile compounds. These constituents contribute to its antimicrobial, anti-inflammatory, and antioxidant properties.₆

Recent scientific investigations have validated several traditional claims, demonstrating antifilarial, antidiabetic, and hepatoprotective activities of the plant₇. Given its rich phytochemical composition and wide range of biological activities, Leucas cephalotes has emerged as a promising candidate for further pharmacological research and drug development.

Scientific classification

Table No.: 01

Distribution

Leucas cephalotes is widely distributed across India, where it commonly occurs as a weed in cultivated fields, along roadsides, and in wastelands. It typically grows at low altitudes ranging from about 30–100 m and extends up to nearly 1,800 m in the Himalayan regions. The plant is also reported in several Asian countries, including Nepal, Pakistan, Bhutan, Bangladesh, China, and Afghanistan, as well as in regions like Java, the Philippines, Malaysia, and Mauritius.₉

3.Preliminary phytochemical screening

Table No. 02: Phytochemicals tests in Methanolic, and Aqueous extract of whole plant of Leucas cephalotes_.10

Present (+), Absent (-)

Table No.03: Macroscopy study of leucas cephalotes species. ₁₆

Traditional uses

Leaves

Leaves are widely used in traditional medicine by various tribal communities across India. The Kol tribes of Uttar Pradesh apply a paste made from leaves to treat chronic boils on the head. In the Rewa district of Madhya Pradesh, tribal people chew or massage leaf paste on the gums and teeth to relieve mouth ulcers and headaches. In Northern Gujarat, tribal groups prepare a decoction of leaves combined with Boerhavia diffuse to manage burning sensations and painful urination. In Almora district of Uttarakhand, leaf paste is used to treat stomachache, diarrhea, and abdominal colic. In several regions, including Chhattisgarh, the leaves are also consumed as herbal tea or cooked as a leafy vegetable (bhaji).₁₁ Dried leaves are sometimes mixed with tobacco in a 1:3 ratio and smoked to alleviate bleeding and itching piles. Additionally, in the Tarkeshwar Sacred Grove of Garhwal, leaf poultices are applied to wounds and sores. The leaves are also considered beneficial in chronic rheumatism, and in southern parts of Tamil Nadu, their paste is traditionally used as a remedy for snake bites.₁₂

Flowers

Flowers are also valued for their medicinal properties in traditional practices. The juice extracted from flowers, when mixed with a small amount of honey, is commonly used to treat cold and cough. They are known to possess stimulant, expectorant, diaphoretic, and emmenagogue properties.₁₃ A decoction prepared from flowers and leaves along with black pepper is often administered as an expectorant and to expel intestinal worms. Flower extracts are also considered helpful in treating burns. In the Hazaribagh district of Bihar, tribal communities use a paste made from flowers and seeds mixed with mustard oil to treat ear infections associated with pus formation. Additionally, the flowers of Leucas cephalotes, when combined with a small quantity of powdered date palm fruits, are traditionally used to manage intestinal catarrh in children.₁₄

Other uses

Various other parts of the plant are also used in traditional medicine by different tribal communities. In the Buldhana district of Maharashtra, dried roots wrapped in a betel leaf are used to help manage fever and pneumonia. According to Ayurvedic practices, multiple parts of the plant are utilized to treat a range of health conditions. In the Almora district, tribal groups use roots ground with black pepper to address liver enlargement, while in Jaunpur district of Uttar Pradesh, plant parts are used in the treatment of asthma. The shrub is also known for its effectiveness in reducing inflammation and managing conditions such as jaundice and digestive disorders. In Ayurveda, Dronapushpi is recognized as an important medicinal plant and is also used in homeopathic preparations for chronic malaria and asthma. Additionally, it is consideredbeneficial in treating bronchitis, dyspepsia, paralysis, leucoma, and other inflammatory conditions.₁₅

Chemical constituent of leucas cephalotes plant

The whole plant of Leucas cephalotes (Roth) Spreng is rich in a variety of phytochemicals. It contains different types of diterpenes, including labdane, norlabdane, and abietane derivatives, which have been identified as leucasdins A, B, and C. Additionally, two protostane-type triterpenes, leucastrins A and B, have been isolated along with a known triterpene, oleanolic acid. The plant also possesses several sterols such as 7-oxositosterol, 7-oxostigmasterol, 7α-hydroxysitosterol, 7α-hydroxystigmasterol, and stigmasterol.A number of flavonoids have also been reported from the plant, including 5-hydroxy-7,4-dimethoxyflavone, pillion, gonzalitosin, tricin, cosmosin, apigenin 7-O-β-D-(6-O-p-coumaroyl) glucopyranoside, anisofolin A, and luteolin 4-O-β-D-glucuronopyranoside. The chemical structures of the major compounds, namely leucasdins (A–C) and leucastrins (A–B), have been elucidated in detail through structural studies. Furthermore, the seed oil of the plant contains various fatty acids such as laballenic acid (octadeca-5,6-dienoic acid), lauric acid, glutaric acid, tridecanoic acid, and adipic acid. Among the sterols present, β-sitosterol and stigmasterol are considered the principal constituents of the plant._17,18

Pharmacological activities

Hepatoprotective activity

The methanolic extract of the whole plant has been investigated for its protective effects on the liver. In experimental studies, liver damage was induced in rats using carbon tetrachloride, and the extract was administered orally at doses of 100 and 200 mg/kg body weight for 24 hours. The results showed a significant decrease in serum markers such as serum glutamic oxaloacetic transaminase (SGOT), serum glutamic pyruvic transaminase (SGPT), alkaline phosphatase, total bilirubin, and total cholesterol. At the same time, there was a notable increase in albumin levels. Overall, the treated groups exhibited considerable protection against liver damage compared to the control group, indicating the hepatoprotective potential of the plant extract.₁₉

Anthelmintic activity

The anthelmintic potential of Leucas cephalotes was evaluated using both alcoholic and aqueous leaf extracts. The study tested the extracts against earthworms (Pheretima posthuma) and roundworms (Ascaridia galli) at concentrations ranging from 10 to 100 mg/ml. The results indicated that the plant extracts exhibited significant anthelmintic activity, with the strongest effect observed at the highest concentration of 100 mg/ml.₂₀

Antimicrobial activity

The antimicrobial effects of Leucas cephalotes were examined using toluene and methanolic extracts of the powdered plant material. The extracts were tested against bacterial strains (Bacillus cereus and Shigella flexneri) as well as the fungal strain (Candida albicans). Among the two, the methanolic extract exhibited a broader and more effective antimicrobial activity compared to the toluene extract at the same concentration (5 mg/disc). However, the zones of inhibition produced by the methanolic extract were smaller than those observed with standard antimicrobial agents for all tested microorganisms.₂₁

Antioxidant , analgesic and anti-inflammatory activity

The powdered whole plant of Leucas cephalotes was subjected to continuous extraction using methanol, and the resulting crude extract was evaluated for several biological activities. Its antioxidant potential was assessed using the DPPH (Diphenyl picryl hydrazyl) scavenging method, showing an IC50 value of 421.3 µg/ml. Analgesic activity was tested using the hot plate method in both young and aged mice, with methanolic extract administered at doses of 200 and 400 mg/kg orally. The 200 mg/kg dose produced a significant analgesic effect (p<0.05), while the 400 mg/kg dose exhibited the highest analgesic activity, comparable to the standard drug pentazocine. Additionally, the anti-inflammatory effect of the methanolic extract was evaluated in Wistar albino rats using carrageenan-induced paw edema. At doses of 200 and 400 mg/kg orally, the extract significantly reduced paw volume compared to the control group, indicating notable anti-inflammatory activity.₂₂

Anti- filarial activity

The alcoholic extract of the flowers and stems of Leucas cephalotes has been shown to possess anti-filarial properties. It was found to be effective against both adult worms and microfilariae of Setaria cervi, demonstrating its potential as a natural filaricidal agent.₂₃

Anti-diabetic activity

The ethanolic extract of Leucas cephalotes leaves has been reported to exhibit antidiabetic, antihyperlipidemic, and antioxidant activities. When administered at doses of 150, 300, and 450 mg/kg body weight, the extract not only lowered blood glucose levels but also improved lipid profiles in both normal and diabetic rats induced with alloxan or streptozotocin. The highest dose of 450 mg/kg showed the most pronounced effect, comparable to standard antidiabetic drugs such as glibenclamide and metformin. These findings suggest that the ethanolic leaf extract of Leucas cephalotes may be effective in managing both insulin-dependent (IDDM) and non-insulin-dependent diabetes mellitus (NIDDM).₂₄

Antibacterial activity

The organic leaf extract of Leucas cephalotes demonstrated notable antibacterial activity against several pathogenic bacteria, including Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Proteus vulgaris, and Klebsiella pneumoniae. However, the zones of inhibition produced by Leucas cephalotes were smaller compared to those observed with other plant extracts tested under similar conditions.₂₅

Anti dengue activity

The study titled “Anti-dengue activity of supercritical extract and isolated oleanolic acid of Leucas cephalotes using in vitro and in silico approach” explores a natural way to fight dengue, a disease spread by mosquitoes that still lacks a reliable antiviral treatment. Because of this gap, researchers are increasingly turning toward medicinal plants for possible solutions. In this research, Leucas cephalotes, a plant known for its healing properties, was carefully studied. Scientists used an advanced extraction method called supercritical fluid extraction to obtain high-quality compounds from the plant. From this extract, they isolated oleanolic acid, a naturally occurring compound with known biological benefits. The effectiveness of both the plant extract and oleanolic acid was tested in laboratory conditions using dengue-infected cells. The findings were very encouraging. The extract almost completely stopped the virus from multiplying, while oleanolic acid showed nearly the same level of effectiveness. Importantly, the treated cells remained healthy, suggesting that these substances are not harmful at working doses. Computer-based analysis further showed that oleanolic acid can strongly bind to important viral proteins, potentially blocking the virus’s growth. Overall, the study highlights the promise of plant-based compounds as future dengue treatments, although more research is needed to confirm their use in humans.₂₆ (Kaushik S et al., 2021)

Recent articles are published in on leaves of leucas cephalotes plant

1. Priyanka Singh, Amar Kumar Mishra, Pragati Singh.

Medicinal plants have been widely investigated for their potential in treating neurological disorders such as epilepsy. Leucas cephalotes is traditionally used in herbal medicine and contains important phytochemicals like flavonoids, alkaloids, terpenoids, and phenolic compounds that may affect the nervous system. Previous experimental studies on animal seizure models have reported that leaf extracts of Leucas cephalotes can delay seizure onset and decrease seizure severity. Toxicity evaluations have also suggested that the extract is relatively safe at experimental doses. These findings indicate that Leucas cephalotes may serve as a potential natural source for anti-epileptic therapy. However, more detailed pharmacological and clinical studies are required to confirm its effectiveness (Singh P, Mishra AK, Singh P, Singh R. 2023)₂₆.

2.Anjali Verma, Anil Kumar, Dalip Kumar Upreti1, Veena Pande, Mahesh Pal

Research on the antidiabetic potential of medicinal plants has focused on their ability to inhibit carbohydrate-hydrolyzing enzymes such as α-amylase and α-glucosidase, which help regulate postprandial blood glucose levels. Leucas cephalotes, a medicinal plant from the Lamiaceae family, has been traditionally used in herbal medicine for various therapeutic purposes. A study by Anjali Verma and colleagues reported that extracts of Leucas cephalotes showed significant α-amylase inhibitory activity, indicating potential antihyperglycemic effects. The study also identified several fatty acids through GC–MS analysis, including palmitic, oleic, and linoleic acids, which may contribute to its biological activity. These findings suggest that Leucas cephalotes could serve as a promising natural source for developing plant-based antidiabetic agents (Verma et al., 2017).₂₇

3.Jasmin H. Bavarva, A.V.R.L. Narasimhacharyab

A study by Jasmin H. Bavarva and A. V. R. L. Narasimhacharya reported the antidiabetic potential of Leucas cephalotes in experimental diabetic rats. The ethanol extract of the plant leaves was administered to both insulin-dependent and non-insulin-dependent diabetic models. The results showed a significant reduction in plasma glucose and lipid levels after treatment. In addition, the extract improved antioxidant status and increased hepatic glycogen levels in diabetic rats. The study also observed a decrease in lipid peroxidation and improvement in metabolic enzyme activity. These findings suggest that Leucas cephalotes may help regulate carbohydrate and lipid metabolism and could be useful in the management of diabetes.₂₈

4.Katara Antariksh, Pradhan Chandan Kumar, Tyagi Amit Kumar, Singh Pradeep

A study by Katara Antariksh and colleagues investigated the phytochemical profile and antimicrobial activity of Leucas cephalotes whole herb. The researchers analyzed the powdered plant using pharmacognostic and phytochemical methods and identified important constituents such as tannins and flavonoids. Extracts prepared using methanol and toluene were evaluated for antimicrobial activity against different bacterial and fungal strains. The methanolic extract showed comparatively higher inhibitory activity, indicating the presence of bioactive compounds with antimicrobial potential. These findings suggest that Leucas cephalotes may serve as a natural source of therapeutic agents for treating microbial infections. The study supports the traditional medicinal use of this plant and highlights its pharmacological importance.₂₉

5. Dhruva Kumar, Dr. Munesh Mani

A study conducted by Dhruva Kumar and Munesh Mani investigated the antidiabetic and liver protective effects of Leucas cephalotes leaves in streptozotocin-induced diabetic rats. The ethanolic leaf extract was administered at doses of 200 and 400 mg/kg, and blood glucose levels were monitored for 21 days. The results showed a significant reduction in blood glucose levels compared with the diabetic control group. In addition, liver function parameters such as bilirubin, serum proteins, albumin, and globulin were improved after treatment. Acute toxicity studies also indicated that the extract was safe at higher doses. These findings suggest that Leucas cephalotes possesses promising antidiabetic and hepatoprotective properties due to its phytochemical constituent.₃₀

6. Reena Bhoriaand Sushma Kainsa

A review by Reena Bhoria and Sushma Kainsa summarized the phytochemical and pharmacological properties of Leucas cephalotes. The plant is widely distributed in India and traditionally used in Ayurvedic medicine for treating inflammation, infections, diabetes and liver disorders. Phytochemical investigations have reported the presence of important compounds such as diterpenes (Leucasdins A–C), sterols and flavonoids. These constituents contribute to several biological activities including antimicrobial, antioxidant and hepatoprotective effects. The review highlights that the plant possesses significant therapeutic potential and supports its traditional medicinal use. However, further experimental studies are required to confirm its safety and clinical effectiveness.₃₁

7.Sachin Chavan, Nishteswar K

A review by Sachin Chavan and K. Nishteswar discussed the medicinal importance of Leucas cephalotes and Leucas aspera, which are commonly known as Dronpushpi. These plants are widely distributed in India and are traditionally used in Ayurvedic and Unani medicine for treating fever, jaundice, cough and inflammatory disorders. Phytochemical studies revealed the presence of important constituents such as β-sitosterol, terpenoids, phenolic compounds and glucosides. These bioactive compounds contribute to various pharmacological activities including antioxidant, antimicrobial and hepatoprotective effects. The review concluded that both species possess significant therapeutic potential and support their traditional medicinal applications.₃₂

CONCLUSION

Leucas cephalotes is a valuable medicinal plant with a long history of use in traditional healthcare systems. The wide range of ethnomedicinal applications, from treating common infections to managing chronic conditions, reflects its importance in folk medicine. Scientific studies have confirmed that the plant contains diverse bioactive compounds such as flavonoids, triterpenes, and sterols, which contribute to its multiple pharmacological effects.

Experimental research supports its antioxidant, anti-inflammatory, antimicrobial, hepatoprotective, antidiabetic, and other therapeutic activities, validating many of its traditional uses. Recent findings also suggest its potential in emerging areas like antiviral and neurological disorders, further expanding its medicinal relevance.

Despite these promising results, most studies are still limited to experimental models. Therefore, more detailed investigations, including clinical trials and safety evaluations, are necessary to establish its effectiveness in humans. Overall, Leucas cephalotes holds strong potential as a natural source for future drug development and deserves further scientific exploration.

REFERENCES

1. Chowdhury AR, Tripathi S. Indian Perfumer. 2001;45(2):81–82.
2. Nadkarni KH. Indian Materia Medica. Mumbai: Popular Prakashan; 2007. p. 739.
3. Kirtikar KR, Basu BD. Indian medicinal plants. Vol. 3. Dehradun: National Book Distributor; 1999. p. 2017–2018.
4. Anonymous. The Ayurvedic pharmacopoeia of India. Vol. 3, Part 1. 1st ed. New Delhi: Controller of Publications, Ministry of Health and Family Welfare, Government of India; 2001. p. 35–37.
5. Anonymous. The wealth of India: a dictionary of Indian raw materials and industrial products. Vol. 6. New Delhi: NISCAIR, CSIR; 2003. p. 79–80.
6. Oudhia P. Dronpushpi or Guma (Leucas cephalotes): a useful weed [Internet]. 2001 [cited year unknown]. Available from: http://www.celestine-india.com/pankajoudhia
7. Khanam M, Hassan A. Banglades J Plant Taxon. 2005;12(1):1–10.
8. Chopra RN, Nayar SC, Chopra IC. Glossary of Indian medicinal plants. New Delhi: NISCAIR; 2002. p. 153.
9. Aminuddin RD, Girach G, Khan SA. Hamdard. 2000;37(2):67–72.
10. Itoria P, Jain S, Jain G, Dubey BK. Pharmacognostic evaluation and phytochemical screening of Leucas cephalotes. 2015
11. Shukla AN, Srivastava S, Rawat AKS. Indian J Tradit Knowl. 2010;9:191–202.
12. Kumari P, Joshi GC, Tewari LM. Int J Biodivers Conserv. 2011;3(7):298–326.
13. Khare CP. Indian medicinal plants. 2nd ed. New Delhi: Springer Pvt Ltd; 2007. p. 372.
14. Anonymous. The Wealth of India: a dictionary of Indian raw materials and industrial products. Vol. 6. New Delhi: NISCAIR, CSIR; 2003. p. 79–80.
15. Samy RP, Thwin MM, Gopalakrishnakone P, Ignacimuthu S. J Ethnopharmacol. 2008;115(2):302–312.
16. Itoria P, Jain S, Jain G, Dubey BK. Pharmacognostic evaluation and phytochemical screening of Leucas cephalotes. 2014.
17. Greca MD, Monaco P, Previtera L. J Nat Prod. 1990;53(6):1430–1435.
18. Pettit GR, Numata A, Cragg GM, Herald DL, Takada T, Iwamoto C, Riesen R, Schmidt JM, Doubek DL. Isolation and structure of leucasdin, a novel cytotoxic compound from Leucas cephalotes. J Nat Prod. 1990;53(6):1406–1410.
19.  Sailor GU, Dudhrejiya AV. Pharmacologyonline. 2010;1:30–38.
20.   Shind RB, Jagtap VA. Int J Drug Discov Herb Res. 2011;1(1):25–26.
21. Antariksh K, Kumar PC. J Nat Prod Plant Resour. 2010;2(4):284–296.
22.   Baburao B, Reddy ARN. Braz J Pharm Sci. 2010;46:525–529.
23.   Qamaruddin, Parveen N. J Nat Remedies. 2002;2(2):155–163.
24.   Bavarva JH, Narasimhacharya AVRL. J Ethnopharmacol. 2010;127:98–102.
25.   Madhukiran BL, Lakshmi Vijaya K, Devi PUM. Anc Sci Life. 2002;21(4):1–3.
26. Singh P, Mishra AK, Singh P, Singh R. Evaluation of anti-epileptic activity of leaves of Leucas cephalotes
27. Verma A, Kumar A, Kumar D, Upreti DK, Pandey V, Pal M. Fatty acid profiling and in vitro antihyperglycemic effect of Leucas cephalotes (Roth) Spreng via carbohydrate hydrolyzing enzyme inhibition. Pharmacogn Mag. 2017;13(Suppl 1):S30–S36.
28. Bavarva JH, Narasimhacharya AVR. Leucas cephalotes regulates carbohydrate and lipid metabolism and improves antioxidant status in IDDM and NIDDM rats. J Ethnopharmacol. 2010;127(1):98–102.
29. Katara A, Chandan P, Kumar A, Tyagi A, Kumar S. Phytochemical investigation and antimicrobial activity of Leucas cephalotes (Roth) Spreng whole herb. Der Pharmacia Lettre. 2010;2(4):284–296.
30. Katara A, Chandan P, Kumar A, Tyagi A, Kumar S. Phytochemical investigation and antimicrobial activity of Leucas cephalotes (Roth) Spreng whole herb. Der Pharmacia Lettre. 2010;2(4):284–296.
31. Bhoria R, Kainsa S. Leucas cephalotes (Roth) Spreng: review at a glance. International Journal of Pharmacy and Pharmaceutical Sciences. 2013;3(1):77–81.
32. Chavan S, Nishtewar K. A review on source plants of Dronpushpi – Leucas cephalotes (Roth) Spreng and Leucas aspera Spreng. Int J Ayurvedic Med. 2013;4(3):290–303.