LOBELIA’S MECHANISMS OF ACTION ON THE PULMONARY SYSTEM A Modern Look at a Classic Lung Herb

LOBELIA’S MECHANISMS OF ACTION ON THE PULMONARY SYSTEM
A Modern Look at a Classic Lung Herb
Copyright Dr Jillian Stansbury

The Lobelia genus includes nearly 400 species, making up a major group in the Lobelioideae branch of the Campanulaceae Family. The name Lobelia derives from a Belgian botanist Matthias de Lobel, Flemish botanist and physician to King James I. Many Lobelia species are used medicinally in Asia with a growing body of published research, while Lobelia inflata and siphylitica are the main North American species mentioned in traditional folkloric herbal literature with fairly scant research to date. For example the Asian species Lobelia nicotianaefolia is being explored for antiepileptic activity due to lobeline’s ability to promote GABAnergic activity.(1) Lobelia cardenalis has one of the showier flowers and is sometimes used as an ornamental. Lobelia inflata is probably the species most used North American medicinal species and has something of a colorful past. Lobelia inflata goes by the common names Indian Tobacco or occasionally “Pukeweed” because of the powerful emetic effect of the fresh buds. Lobelia was even referred to as the “Demon Herb” due to the occasional cult-like followers of a “puke and purge” approach to medicine that employed Lobelia, not well received by those outside the practice.

Lobelia inflata in North American Traditional Medicine
North American Native people used Lobelia for wheezing and respiratory problems in inhalant powders and even smoking blends giving rise to the common name “Indian Tobacco”. Dried Lobelia leaves were sprinkled over burning coals to inhale the vapors in cases of acute wheezing, and early American pioneer medicine included the use of Lobelia in teas and tinctures for respiratory constriction, spastic coughing, and acute and chronic asthma. A Modern Herbal, a classic herbal formulary and therapeutic book written by Maude Greive and published in the 1930s, described a chest poultice for wheezing using Lobelia and Ulmus bark powers combined with a weak lye solution. Because of broader muscle relaxing effects, Lobelia was also included in formulas for nervous tension and muscle spasm. Midwives are known to have used Lobelia oil rubbed directly onto the cervix in cases of failure to dilate during labor and Lobelia is credited with relaxing effects on the both uterine and cardiac muscle. Case reports in medical journals from the 1800s and early 1900s include Lobelia in formulas for diphtheria. Samuel Thompson reportedly got an early start as an herbalist when he learned that just a few fresh L. inflata flower pods could induce vomiting, a fact which he kept to himself while coaxing childhood friends to eat them. Samuel Thompson went on to become the superintendent of Indian affairs in North America from 1756 to 1774 and promoted his herbal remedies on the side as he traveled extensively.

Lobelia inflata’s Chemical Constituents
A group of piperidine alkaloids are among the most powerful and most studied of Lobelia’s constituents and include lobeline, lobelanine, and lobelanidine, with the seeds having the greatest concentration. Lobelia inflata is reported to have the highest piperidine alkaloid content of any other Lobelia species. Additional alkaloids continue to be identified in the present era.(2) Lobelia inflata also contains the nerve calming beta-amyrin palmitate, as well as lobelic acid, gums, resin, fixed oils and mineral salts including calcium, potassium and ferric oxide.
Lobeline is a lipophilic alkaloidal molecule which researchers have long reported to act as both an agonist and antagonist to beta nicotinic receptors.(3) Animal studies have suggested that piperidine alkaloids such as lobeline are able to cross the blood brain barrier, and similar to nicotine, promote the release of the neurotransmitters dopamine and norepinephrine, thus giving many Lobelia species central nervous system effects.(4) Lobelia inflata also contains beta-amyrin palmitate, shown to reduce the affects amphetamines in animal studies and overall exert a mild sedative effect.(5)
Some Lobelia species contain protostane, a group of tetracyclic triterpenes with very limited distribution in plants. Protostanes are credited with numerous anti-microbial and hepatoprotective effects.(6) Lobelia inflata constituents may also reduce the ability of P-glycoprotein receptors to excrete various chemotherapy drugs that leads to multidrug resistance. (7) [cut this paragraph if needed for space considerations]

Lobeline’s Action on Pulmonary Catecholamines
The pyridine alkaloid lobeline is a respiratory stimulant due to excitant effects on pulmonary afferent nerves.(8) Higher and repetitive doses of Lobelia are well known to have emetic effects, while lesser dosages provoke the nausea and increased salivary flow that typically precede vomiting. This pulmonary stimulation may also promote hyperventilation and hyperpnoea on occasion(9), but is usually a beneficial effect employed by herbalists to help free thick or stagnant respiratory secretions in cases of humid asthma and excessive secretions in the bronchi.

Lobelia, Smoking Cessation and Amphetamine Addiction
Although molecularly quite different from nicotine, lobeline has been shown to act as both an agonist and antagonist at nicotinic receptors. Lobeline inhibits the nicotine-triggered release of dopamine and the binding of various nicotinic agents to nicotinic receptors. Because of adrenergic blockade, lobeline is also being explored as a possible tool to reduce and treat addiction to amphetamines and psychostimulants. Lobeline’s activity at nicotinic receptors may help reduce smoking craving, as well as interact with the vesicular monoamine transport system and reduce the pleasurable effects of smoking.(10) Effect on both monoamine transport and nicotinic receptors lends lobeline modulatory effects on the neurochemical and behavioral responses to amphetamine use.(11) Animal studies have shown that rats dosed with lobelane, a naturally occurring lobeline analogue that can also be synthesized, will spontaneously self-administer less methamphetamine.(12)
Beta-amyrin palmitate is another unusual compound found in Lobelia inflata leaves credited with a calming effect due to central nervous system effects. (13) One group of researchers found that beta-amyrin palmitate promoted noradrenaline activity(14), and others propose an anti-depressant effect via this same mechanism.(15)
Lobeline may also inhibit the flow of calcium ions into adrenal chromaffin cells but not inhibit calcium ion release from the cytoplasmic calcium store.(16) This mechanism helps to block adrenalin-like responses, making Lobelia appropriate in herbal formulas for those who experience wheezing and respiratory symptoms due to psychological stress and nervous tension.

Carotid Sinuses, Chemoreceptors and the Cough Reflex
Although Lobelia is one of the most classic “cough” herbs, it will also commonly induce a cough and pressure sensations in the chest.(17) The ingestion of Lobelia or tincture will almost immediately provoke sensation of fumes or pressure in the throat and upper chest, and if the dosing is repeated frequently, choking sensations and emesis will often ensue. With small, physiologically appropriate dosages, Lobelia can rapid acting expectorant via more gentle effects that will not be emetic or even nauseating when properly formulated and dosed. Like many of the strongest medicinal herbs, Lobelia may display a notable biphasic effect, where it may suppress respiration at some dosages or scenarios while stimulating it in others.
Although known empirically to affect respiration and respiratory secretions for well over a century, the mechanisms of these pulmonary effects have not been well understood until the last several decades. Animal studies show that lobeline’s stimulatory effect on breathing can be abolished by denervation of the carotid sinuses suggesting that lobeline may act on pressure receptors in the carotids and other blood vessels.(18) Research suggests that lobeline may both stimulate chemoreceptors(19) in the carotid sinuses, as well as well as have general adrenergic effects that promote neural firing in the phrenic nerve.(20,21) which innervates the diaphragm and may also stimulate the muscular vigor of coughing. (22) Lobelia also supports the cough reflex via effects on J receptors further described below. Veterinary medicine is exploring lobeline for chronic obstructive pulmonary disease in horses.(23)
Despite all these stimulating effects on various cough reflex mechanisms, Lobelia ultimately helps alleviate pressure and congestion in the lungs which triggers wheezing or a problematic cough. For best results, Lobelia should be formulated with herbs that are soothing to the throat and lung mucosa (Tussilago, Ulmus, Mentha, Glycyrrhiza), and have a relaxing antispasmodic effect to complement and balance to the harsh stimulating effects of Lobelia (Thymus, Khella, Drosera)

HERBS AND THE MECHANICS OF COUGHING
In addition to chemoreceptors in the carotid arteries, the smooth muscles of the upper airways receive excitatory input from peripheral chemoreceptors and pressure receptors including the so called C fibers or J receptors, short for juxtapulmonary capillary receptors. The larynx and trachea contain the greatest number of J receptors found in association with “rapidly adapting receptors” and stimulating these pathways will trigger coughing. Animals that do not possess these do not cough. Rapidly adapting receptors can respond to inhaled irritants as well as dissolved chemicals and trigger the cough reflex to help expel the irritant or compound. The laryngeal and tracheal tissues also possess “slowly adapting stretch receptors” which may also be involved initiating coughing. J receptors are known to be activated by capsaicin, lobeline, bradykinin, sulpher gases, and mechanical manipulation.(24,25) Many of Dr Christopher’s, Jethro Kloss’ and other classic herbal formulas commonly used Lobelia and Capsicum, the source of capsaicin, in tandem reporting the duo together to be more effective than either alone.

Lobelia’s Effect on J Receptors in the Lungs
Research is revealing that the throat and chest symptoms produced by Lobelia occur due to direct effects on juxtapulmonary capillary receptors.(26,27) abbreviated as J receptors. Lobeline binds and activates J Receptors. So called “cardiac coughs” may involve J receptor stimulation when the persistent interstitial edema in patients with left ventricular heart failure or mitral valve stenosis stimulates the J receptors. Lobeline may trigger coughing due to a similar phenomenon where very temporary pulmonary congestion stimulates the J receptors stimulating respiration, secretions, and coughing.(28) In cases of asthma and excessive respiratory secretions, Lobelia may act as something like an internal “counter irritant” supporting productive coughing. The term counter irritant is from herbal folklore and most often in used to refer to irritating agents such as pine tar or Sanguinaria resin used in small amounts topically on the skin to gently irritate the skin and trigger an immune and inflammatory response. In this case, small amounts of Lobelia used internally can gently irritate the J chemoreceptors and trigger respiratory responses.

Examples of Herbal Formulas Using Lobelia inflata
These tincture formulas are based on dram measures where there are 8 drams per 1 oz. The formula can be converted to mls where 1 dram equals 4 mls.

Formula for Acute Wheezing
Ammi visnaga 3
Thymus 2
Lobelia 1
Prunus 1
Zingiber 1
Take 1 tsp every 5 to 15 minutes, reducing as symptoms improve.

Expectoration Formula for Acute Humid Asthma
Grindelia 2
Armoracia 2
Lobelia 1
Cayenne 1
Iris 1
Xanthoxyllum 1
Combine equal parts and take an entire dropperfull every 3-5 minutes for a half an hour while breathing steam when possible. Reduce frequency should nausea occur.

Tight Dry Cough with Scant Sticky Mucous Expectoration
Petasites 2
Grindelia 2
Stillingia 2
Lobelia 1
Capsicum 1
Take one tsp every 15 minutes to an hour, reducing as symptoms improve. Breathe steam when possible to complement the herbs. Reduce frequency should nausea occur.

Hot Lobelia Pack
1 Cup dry Lobelia leaves
2 cups water
2 cups vinegar
Combine the water and vinegar and bring to a simmer. Turn off the heat and add the Lobelia leaves, allowing to steep for 15 minutes. Strain out the herbs and use the fluid to prepare a moist hot pack. Soak a small towel in the infusion, and place over the most painful area of the chest and lungs, cover with plastic wrap and heat, such as heating pad, another hot moist towel or hydroculator pack. The Lobelia pack combines well with a topical oil from plain castor oil to a medicinally infused oil. Oil the person’s skin directly first, apply the hot Lobelia pack, then cover with heat. Repeat every few hours during the acute phases of pleurisy, pneumonia, or spastic coughing.

Plaster Base for Lung Plasters
This formula can be used as a waxy base that other medicinal substances can be stirred into. This formula is not too runny and not to stiff, neither is it sticky like pure lanolin or greasy like pure oil. Once prepared and left to cool, it will harden, but can be stored indefinitely and reheated when needed. The beeswax is first melted in a double boiler and the lanolin, paraffin, and oil are then stirred in. It is applied to a patients oiled chest or back by painting or spooning the plaster base onto a thin oiled piece of muslin (cotton) fabric. The muslin is placed on the patient’s oiled torso and covered with plastic sheeting and a hot pack and towel
Beeswax 4 oz
Castor oil 2 oz
Anhydrous lanolin 2 oz
Soft paraffin 8 oz

Topical Lung Plaster
16 oz Plaster Base (as above)
4 oz Lobelia powder
1 oz Capsicum powder
Heat the plaster base until soft and then stir in the powder herbs. When thoroughly blended, spread the medicated plaster on a piece of muslin or other suitable fabric about 1 foot square in size. Apply this directly to the chest or back, medicine side down, and cover with a hot towel or heating pad. Note that too much Capsicum is capable of inducing severe burns if not properly diluted. Use no more than what is shown here.

Morning Hydrotherapy for Emphysema
Breathe steam through the mouth for 10 to 15 minutes upon arising while taking an expectorating herbal tincture every few minutes, nearly to the point of nausea. Induction of vomiting with herbal emetics is one folkloric method of helping to purge mucous accumulation from the lungs, but is too harsh and debilitating for some elderly or weak patients. For others however, this can support easier breathing for the day and reduce the risk of opportunistic lung infections, thus improving quality of life and even longevity for those with emphysema.
The use of potentially emetic herbs such as Lobelia and Capsicum at a dosage below the nausea and vomiting threshold can help stimulate saliva flow and the mucocilliary apparatus of the lungs and facilitate expectoration without actually vomiting. Gentle but vigorous pounding of the back and chest by a family member may also help loosen settled and stuck mucous plugs and enhance the therapy. This whole procedure is best carried out in the bathroom so that the person can spit or even vomit into the toilet as secretions are freed and able to be expectorated. Carry a big pot of steaming water into the bathroom and set in the bathroom sink. The person might also take a hot shower immediately upon arising to help start the process and get the bathroom humid and steamy. Complement with an expectorating tincture as exemplified above.

Tincture for Pleurisy
Lomatium 2
Allium 2
Hypericum 2
Lobelia 1
Bryonia 1
Take 1 tsp every ½ to 1 hour, reducing frequency as symptoms improve.



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